protein tyrosine kinase/rtk 1 inhibitors, agonists, screening libraries protein tyrosine kinase/rtk...

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Inhibitors, Agonists, Screening Librarieswww.MedChemExpress.com

Protein Tyrosine Kinase/RTK

Protein-tyrosine kinases (PTKs) catalyze the transfer of the -phosphate of ATP to tyrosine residues of protein substrates,are critical components of signaling pathways that control cellular proliferation and differentiation. Two classes of PTKsare present in cells: the transmembrane receptor PTKs and the nonreceptor PTKs.The RTK family includes the receptors for insulin and for many growth factors, such as EGF, FGF, PDGF, VEGF, and NGF.RTKs are transmembrane glycoproteins that are activated by the binding of their ligands, and they transduce theextracellular signal to the cytoplasm by phosphorylating tyrosine residues on the receptors themselves(autophosphorylation) and on downstream signaling proteins. RTKs activate numerous signaling pathways within cells,leading to cell proliferation, differentiation, migration, or metabolic changes. In addition, nonreceptor tyrosine kinases(NRTKs), which include Src, JAKs, and Abl, among others, are integral components of the signaling cascades triggered byRTKs and by other cell surface receptors such as GPCRs and receptors of the immune system. NRTKs are criticalcomponents in the regulation of the immune system.RTKs and NRTKs have been implicated in the progression of diseases such as cancer, diabetic retinopathy, atherosclerosis,and psoriasis. Protein kinases, including RTKs, are one of the most frequently mutated gene families implicated in cancer,which has prompted numerous studies on their role in cancer pathogenesis. There are four main mechanisms of RTKdysregulation in human cancers: genomic rearrangements, autocrine activation, overexpression and gain- orloss-of-function mutations. Currently, there are several clinically available small molecule inhibitors and monoclonalantibodies against specific RTKs.References:[1] Hubbard SR, et al. Annu Rev Biochem. 2000;69:373-98.[2] Robinson DR, et al. Oncogene. 2000 Nov 20;19(49):5548-57.
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RET 95

ROS 98

Src 100

Syk 106

TAM Receptor 109

Trk Receptor 112

VEGFR 116

Ack1 3

ALK 5

Bcr-Abl 10

BMX Kinase 16

Btk 18

c-Fms 23

c-Kit 27

c-Met/HGFR 32

Discoidin Domain Receptor 38

DYRK 40

EGFR 42

Ephrin Receptor 54

FAK 56

FGFR 59

FLT3 66

IGF-1R 72

Insulin Receptor 75

IRAK 78

Itk 81

PDGFR 83

PKA 90

Pyk2 93

Inhibitors, Agonists, Screening Librarieswww.MedChemExpress.com

Target List in Protein Tyrosine Kinase/RTK

2 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]
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Ack1Activated CDC42 kinase 1;TNK2

Ack1 (Activated CDC42 kinase 1) is an enzyme that in humans isencoded by the TNK2 gene. Ack1 binds to multiple receptor tyrosinekinases e.g. EGFR, MERTK, AXL, HER2 and insulin receptor (IR). Ack1also interacts with Cdc42Hs in its GTP-bound form and inhibits boththe intrinsic and GTPase-activating protein (GAP)-stimulated GTPaseactivity of Cdc42Hs. Ack1 is a survival kinase and shown to beassociated with tumor cell survival, proliferation, hormone-resistanceand radiation resistance. Ack1 has emerged as a new cancer targetand multiple small molecule inhibitors have been reported.
https://www.MedChemExpress.com/Targets/Ack1.html

Purity: 96.72%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 50 mg, 100 mg

Purity: 99.95%Clinical Data: No Development ReportedSize: 10mM x 1mL in DMSO,

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Ack1 Inhibitors & Modulators

Bioactivity: AIM-100 is a small molecule inhibitor of Ack1 with an IC50 of24 nM

Bioactivity: KRCA-0008 is a potent and selective ALK/Ack1 inhibitor withIC50 of 12 nM/4 nM for ALK and Ack1 respectively; displaysdrug-like properties without hERG liability.


AIM-100 Cat. No.: HY-15290

KRCA-0008 Cat. No.: HY-12331
https://www.MedChemExpress.com/Targets/Ack1.htmlhttps://www.MedChemExpress.com/AIM-100.htmlhttps://www.MedChemExpress.com/KRCA-0008.html


ALKAnaplastic lymphoma kinase;ALK tyrosine kinase receptor;CD246;Cluster of differentiation 246

ALK (Anaplastic lymphoma kinase) is encoded by the ALK gene. ALK isa membrane associated tyrosine kinase receptor of the insulinreceptor superfamily. The function of the full-length ALK receptor ispoorly understood. It has a probable role in the central and peripheralnervous system development and maintenance. ALK is a dependencereceptor, which may exert antagonist functions, proapoptotic orantiapoptotic, depending on the absence or presence of a ligand.Dependence receptors have a potential role in cancer anddevelopment. Ligands available for this demonstration were agonistanti-ALK antibodies. ALK is still an orphan receptor, given the highlevel of controversy about pleiotrophin and midkine.
https://www.MedChemExpress.com/Targets/ALK.html


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Purity: 99.76%Clinical Data: Phase 1Size: 10mM x 1mL in DMSO,

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Purity: >98%Clinical Data: No Development ReportedSize: 100 mg, 250 mg, 500 mg



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Purity: 99.95%Clinical Data: LaunchedSize: 10mM x 1mL in DMSO,

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Purity: >98%Clinical Data: No Development ReportedSize: 250 mg, 500 mg

ALK Inhibitors & Modulators

Bioactivity: 2-Keto Crizotinib (PF-06260182) is an active lactam metaboliteof crizotinib.

Bioactivity: Alectinib (CH5424802) is a potent, selective, and orallyavailable inhibitor with an of 1.9 nM.ALK IC50

Bioactivity: Alectinib Hydrochloride (CH5424802 Hydrochloride) is a potent,selective, and orally available inhibitor with ofALK IC501.9 nM, the dissociation constant ( ) value for ALK in anKDATP-competitive manner is 2.4 nM using a competition-b

Bioactivity: ALK inhibitor 1 is a novel and selective inhibitor for the ALKkinase.

Bioactivity: ALK inhibitor 2 is a novel and selective inhibitor for the ALKkinase.

Bioactivity: ALK-IN-1 is a potent and selective active inhibitor ofanaplastic lymphoma kinase(ALK), Patent US20140066406 A1.

Bioactivity: ALK-IN-5 is a potent, selective, and brain-penetrant inhibitorof , with an of 2.9 nManaplastic lymphoma kinase (ALK) IC50

.[1]

Bioactivity: ALK-IN-6 (compound 11) is an orally bioavailable inhibitor of, with values of 71 nM,anaplastic lymphoma kinase (ALK) IC50

18.72 nM and 36.81 nM for ALK wild, ALK F1196M and ALK F1174L,respectively .[1]

Bioactivity: ASP3026 is a novel and selective inhibitor for ALK (anaplasticlymphoma kinase) with IC50 of 3.5 nM.

Bioactivity: AZD-3463 is an ALK/IGF1R inhibitor which overcomes multiplemechanisms of acquired resistance to crizotinib. IC50 Value:Target: ALK/IGF1R


2-Keto Crizotinib (PF-06260182) Cat. No.: HY-13320

Alectinib (CH5424802; RO5424802; AF802) Cat. No.: HY-13011

Alectinib Hydrochloride (CH5424802 (Hydrochloride); RO5424802 (Hydrochloride); AF-802 Hydrochloride (Hydrochloride)) Cat. No.: HY-13011A

ALK inhibitor 1 Cat. No.: HY-15357

ALK inhibitor 2 Cat. No.: HY-15358

ALK-IN-1 Cat. No.: HY-13464



ASP3026 Cat. No.: HY-13326

AZD-3463 (ALK/IGF1R inhibitor) Cat. No.: HY-15609
https://www.MedChemExpress.com/Targets/ALK.htmlhttps://www.MedChemExpress.com/PF-06260182.htmlhttps://www.MedChemExpress.com/CH5424802.htmlhttps://www.MedChemExpress.com/CH5424802-Hydrochloride.htmlhttps://www.MedChemExpress.com/ALK-inhibitor-1.htmlhttps://www.MedChemExpress.com/ALK-inhibitor-2.htmlhttps://www.MedChemExpress.com/ALK-IN-1.htmlhttps://www.MedChemExpress.com/alk-in-5.htmlhttps://www.MedChemExpress.com/alk-in-6.htmlhttps://www.MedChemExpress.com/ASP3026.htmlhttps://www.MedChemExpress.com/azd-3463.html




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Purity: 99.86%Clinical Data: LaunchedSize: 10mM x 1mL in Water,

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Purity: >98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 50 mg, 100 mg

Purity: 99.98%Clinical Data: LaunchedSize: 5 mg, 10 mg, 50 mg, 100 mg


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Bioactivity: Belizatinib is an oral, dual, potent inhibitor of ALK andTRKA, TRKB, and TRKC, with of 0.7nM for wild-typeIC50recombinant ALK kinase.

Bioactivity: Brigatinib is a highly potent and selective inhibitor,ALKwith an of 0.6 nM.IC50

Bioactivity: CEP-28122 is a highly potent and selective orally active ALKinhibitor with IC50 of 1.9 0.5 nM in an enzyme-based TRFassay.

Bioactivity: CEP-28122 mesylate salt is a highly potent and selectiveorally active ALK inhibitor with IC50 of 1.9 0.5 nM in anenzyme-based TRF assay. IC50 value: 1.9 0.5 nM Target: ALKin vitro: CEP-28122 is a potent inhibitor of recombinant ALKactivity and cellular ALK tyrosine phosphorylation. CEP-28122

Bioactivity: CEP-37440 is a novel potent and selective Dual FAK/ALKinhibitor with IC50 s of 2.3 nM (FAK) and 120 nM(ALK cellularIC50 in 75% human plasma). IC50 value: 2.3 nM (FAK); 120 nM(ALK cellular IC50 in 75% human plasma) Target: Dual FAK/ALKPreparation of fused bicyclic 2,4-diaminopyrimidine

Bioactivity: Ceritinib (LDK378) is a potent and specific inhibitorALKwith an of 0.2 nM.IC50

Bioactivity: Ceritinib dihydrochloride (LDK378 dihydrochloride) is potentinhibitor against ALK with IC of 0.2 nM, shows 40- and5035-fold selectivity against IGF-1R and InsR, respectively.

Bioactivity: Crizotinib is a potent inhibitor of and with anc-Met ALK of 11 nM and 24 nM in cell-based assays, respectively.IC50

Bioactivity: Crizotinib hydrochloride is a potent inhibitor of andc-Met with s of 11 nM and 24 nM in cell-based assays,ALK IC50

respectively.

Bioactivity: EML4-ALK kinase inhibitor 1 is a potent oral active inhibitorof echinoderm microtubule-associated protein-like 4-anaplasticlymphoma kinase , with an of 1 nM .(EML4-ALK) IC50

[1]

Belizatinib (TSR-011) Cat. No.: HY-17603

Brigatinib (AP-26113) Cat. No.: HY-12857

CEP-28122 Cat. No.: HY-18030

CEP-28122 mesylate salt Cat. No.: HY-18030A

CEP-37440 Cat. No.: HY-15841

Ceritinib (LDK378) Cat. No.: HY-15656

Ceritinib dihydrochloride (LDK378 (dihydrochloride)) Cat. No.: HY-15656A

Crizotinib (PF-02341066) Cat. No.: HY-50878

Crizotinib hydrochloride (PF-02341066 hydrochloride) Cat. No.: HY-50878A

EML4-ALK kinase inhibitor 1 Cat. No.: HY-111752
https://www.MedChemExpress.com/Belizatinib.htmlhttps://www.MedChemExpress.com/Brigatinib.htmlhttps://www.MedChemExpress.com/CEP-28122.htmlhttps://www.MedChemExpress.com/CEP-28122-mesylate-salt.htmlhttps://www.MedChemExpress.com/CEP-37440.htmlhttps://www.MedChemExpress.com/LDK378.htmlhttps://www.MedChemExpress.com/LDK378-dihydrochloride.htmlhttps://www.MedChemExpress.com/Crizotinib.htmlhttps://www.MedChemExpress.com/Crizotinib-hydrochloride.htmlhttps://www.MedChemExpress.com/EML4-ALK_kinase_inhibitor_1.html



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Purity: 98.51%Clinical Data: No Development ReportedSize: 2 mg, 5 mg, 10 mg


Bioactivity: Ensartinib (X-396) is a potent and dual / inhibitorALK METwith s of



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Bioactivity: MS4078 is an anaplastic lymphoma kinase ( ) ALK PROTAC(degrader) with a of 19nM for binding affinity to ALKKd

.[1]

Bioactivity: NVP-TAE 684 is a highly potent and selective inhibitor,ALKwhich blocks the growth of ALCL-derived and ALK-dependent celllines with values between 2 and 10 nM.IC50

Bioactivity: Repotrectinib (TPX-0005) is a potent inhibitor,ALK/ROS1/TRKwith of 5.3 nM, 1.01 nM, 1.26 nM and 1.08 nM for SRC, WTIC50ALK, ALK G1202R and ALK L1196M, respectively.

Bioactivity: WY-135 is a ( =1.4 nM) and ( =1.1 nM) dualALK IC50 ROS1 IC50inhibitor.

Bioactivity: X-376 is a potent and dual / inhibitor with sALK MET IC50of 0.61 nM and 0.69 nM, respectively.

MS4078 Cat. No.: HY-112155

NVP-TAE 684 (TAE 684) Cat. No.: HY-10192

Repotrectinib (TPX-0005) Cat. No.: HY-103022

WY-135 Cat. No.: HY-111416

X-376 Cat. No.: HY-16590
https://www.MedChemExpress.com/MS4078.htmlhttps://www.MedChemExpress.com/NVP-TAE-684.htmlhttps://www.MedChemExpress.com/TPX-0005.htmlhttps://www.MedChemExpress.com/WY-135.htmlhttps://www.MedChemExpress.com/Ensartinib.html

Bcr-Abl

Bcr-Abl tyrosine-kinase inhibitors (TKI) are the first-line therapy formost patients with chronic myelogenous leukemia (CML). More than90% of CML cases are caused by a chromosomal abnormality thatresults in the formation of a so-called Philadelphia chromosome. Thisabnormality is a consequence of fusion between the Abelson (Abl)tyrosine kinase gene at chromosome 9 and the break point cluster(Bcr) gene at chromosome 22, resulting in a chimeric oncogene(Bcr-Abl) and a constitutively active Bcr-Abl tyrosine kinase that hasbeen implicated in the pathogenesis of CML. Compounds have beendeveloped to selectively inhibit the tyrosine kinase.

https://www.MedChemExpress.com/Targets/Bcr-Abl.html



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Bcr-Abl Inhibitors & Modulators

Bioactivity: Asciminib (ABL001) is a potent and selective allosteric Bcr-Ablinhibitor; inhibits Ba/F3 cells grown with an of 0.25 nM.IC50

Bioactivity: AST 487 is a kinase inhibitor with of 880 nM,RET IC50inhibits RET autophosphorylation and activation of downstreameffectors, also inhibits with of 520 nM.Flt-3 IC50

Bioactivity: Bafetinib is a tyrosine kinase inhibitor withLyn and Bcr-Ablpotential antineoplastic activity.

Bioactivity: BCR-ABL-IN-1 is an inhibitor of tyrosine kinase, withBCR-ABLa of 6.46, and may be used in the research of chronicpIC50myelogenous leukemia.

Bioactivity: BCR-ABL-IN-2 is an inhibitor of tyrosine kinase,BCR-ABL1with of 57 nM, 773 nm for ABL1 and ABL1 ,IC s50

native T315I

respectively.

Bioactivity: Bosutinib is a dual inhibitor with s of 1.2 nM andSrc/Abl IC501 nM, respectively.

Bioactivity: CHMFL-ABL-039 is a type II native kinase andABLdrug-resistant V299L mutant inhibitor with the sBCR-ABL IC50of 7.9 nM and 27.9 nM, respectively. CHMFL-ABL-039 is used inthe research of chronic myeloid leukemia .[1]

Bioactivity: CHMFL-ABL-121 is a highly potent type II inhibitorABL kinasewith s of 2 nM and 0.2 nM against purified inactive ABL wtIC50and T315I kinase protein, respectively .[1]

Bioactivity: CZC-8004 is a pan-kinase inhibitor and binds a range oftyrosine kinases, including kinase.ABL

Bioactivity: Dasatinib (BMS-354825) is a dual and familyBcr-Abl Srctyrosine kinase inhibitor with s of 0.6, 0.8, 79 and 37 nMIC50for Abl, Src, c-Kit and c-Kit , respectively.D816V

Asciminib (ABL001) Cat. No.: HY-104010

AST 487 (NVP-AST 487) Cat. No.: HY-15002

Bafetinib (INNO-406; NS-187) Cat. No.: HY-50868

BCR-ABL-IN-1 Cat. No.: HY-100314

BCR-ABL-IN-2 Cat. No.: HY-18819

Bosutinib (SKI-606) Cat. No.: HY-10158

CHMFL-ABL-039 Cat. No.: HY-126143

CHMFL-ABL-121 Cat. No.: HY-119370

CZC-8004 (CZC-00008004) Cat. No.: HY-111138

Dasatinib (BMS-354825) Cat. No.: HY-10181
https://www.MedChemExpress.com/Targets/Bcr-Abl.htmlhttps://www.MedChemExpress.com/Asciminib.htmlhttps://www.MedChemExpress.com/AST-487.htmlhttps://www.MedChemExpress.com/Bafetinib.htmlhttps://www.MedChemExpress.com/BCR-ABL-IN-1.htmlhttps://www.MedChemExpress.com/BCR-ABL-IN-2.htmlhttps://www.MedChemExpress.com/Bosutinib.htmlhttps://www.MedChemExpress.com/chmfl-abl-039.htmlhttps://www.MedChemExpress.com/chmfl-abl-121.htmlhttps://www.MedChemExpress.com/CZC-8004.htmlhttps://www.MedChemExpress.com/Dasatinib.html



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Purity: 95.0%Clinical Data: Phase 3Size: 10mM x 1mL in Water,

500 mg


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10 mg, 50 mg


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Bioactivity: Dasatinib hydrochloride is a potent and dual / AblWT Srcinhibitor of 0.6 nM/0.8 nM respectively; also inhibitsIC50

/ with of 79 nM/37 nM.c-KitWT c-KitD816V IC50

Bioactivity: Degrasyn (WP1130) is a cell-permeable deubiquitinase (DUB)inhibitor, directly inhibiting DUB activity of USP9x, USP5,USP14, and UCH37. Degrasyn has been shown to downregulate theantiapoptotic proteins and .Bcr-Abl JAK2

Bioactivity: DPH is a potent cell permeable activator, which displaysc-Ablpotent enzymatic and cellular activity in stimulating c-Ablactivation.

Bioactivity: Flumatinib (HHGV678) is a multi-kinase inhibitor with IC50Values of 1.2 nM, 307.6 nM and 2662 nM for c-Abl, PDGFR andc-Kit respectively.

Bioactivity: Flumatinib mesylate (HH-GV-678 mesylate), a derivative ofimatinib, is a multi-kinase inhibitor with IC50 Values of 1.2nM, 307.6 nM and 2662 nM for c-Abl, PDGFR and c-Kitrespectively. IC50 Value: 1.2 nM (c-Abl); 307.6 nM(PDGFR);2662 nM (c-Kit) [1] Target: c-Abl; c-Kit; PDGRF in vitro:

Bioactivity: GNF-2 is a highly selective non-ATP competitive inhibitor ofoncogenic Bcr-Abl activity (IC50 = 0.14 M). IC50 value: 0.14uM [1] Target: Bcr-Abl in vitro: Ba/F3 cells harboring nativeor T315I mutated Bcr-Abl constructs were treated with GNF-2and AKIs. We monitored the effect of GNF-2 with AKIs on the

Bioactivity: GNF-5, an analogue of GNF-2 with improved pharmacokineticproperties, is a selective non-ATP competitive inhibitor ofBcr-Abl with an IC50 value of 0.220.1 uM (Wild type Abl).IC50 Value: 0.220.1 uM (Wild type Abl) [1] Target: Abl GNF-5is a cell-permeable GNF-2 N-hydroxyethyl carboxamide analog

Bioactivity: GNF-7 inhibits Bcr-Abl WT and Bcr-Abl T315I with IC50 of 133nM and 61 nM, respectively.

Bioactivity: GZD824 is a novel orally bioavailable Bcr-Abl inhibitor forBcr-Abl(WT) and Bcr-Abl(T315I) with IC50 of 0.34 nM and 0.68nM, respectively.

Bioactivity: GZD856 is a novel and orally bioavailable inhibitorPDGFR/with s of 68.6 and 136.6 nM, respectively. Anti-lungIC50cancer activities . Also a inhibitor with[1] Bcr-AblT315I

s of 19.9 and 15.4nM for Bcr-Abl and T315I mutant .IC50[2]


Dasatinib hydrochloride (BMS 354825 hydrochloride) Cat. No.: HY-10181A

Degrasyn (WP1130) Cat. No.: HY-13264

DPH Cat. No.: HY-12070

Flumatinib (HHGV678) Cat. No.: HY-13904

Flumatinib mesylate (HHGV678 mesylate) Cat. No.: HY-13905

GNF-2 Cat. No.: HY-11007



GZD824 Cat. No.: HY-15666

GZD856 Cat. No.: HY-101489
https://www.MedChemExpress.com/Dasatinib-hydrochloride.htmlhttps://www.MedChemExpress.com/WP1130.htmlhttps://www.MedChemExpress.com/DPH.htmlhttps://www.MedChemExpress.com/Flumatinib.htmlhttps://www.MedChemExpress.com/flumatinib-mesylate.htmlhttps://www.MedChemExpress.com/GNF-2.htmlhttps://www.MedChemExpress.com/GNF-5.htmlhttps://www.MedChemExpress.com/GNF-7.htmlhttps://www.MedChemExpress.com/gzd824.htmlhttps://www.MedChemExpress.com/GZD856.html



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Bioactivity: Imatinib (STI571) is a tyrosine kinases inhibitor thatinhibits , , and ( =100 nM) tyrosinec-Kit Bcr-Abl PDGFR IC50kinases.

Bioactivity: Imatinib Mesylate (STI571 Mesylate) is a tyrosine kinasesinhibitor that inhibits , , and ( =100c-Kit Bcr-Abl PDGFR IC50nM) tyrosine kinases.

Bioactivity: KW-2449 is a multi-targeted kinase inhibitor of , ,FLT3 ABL and with s of 6.6, 14, 4 and 48 nM,ABLT315I Aurora kinase IC50

respectively.

Bioactivity: Lyn-IN-1 is a potent and selective dual Bcr-Abl/Lyn inhibitor,extracted from patent WO2014169128A1.

Bioactivity: Nilotinib is an orally available tyrosine kinaseBcr-Ablinhibitor with antineoplastic activity.

Bioactivity: Nilotinib monohydrochloride monohydrate is a second generationtyrosine kinase inhibitor (TKI), is significantly more potentagainst than Imatinib, and is active against manyBCR-ABLImatinib-resistant BCR-ABL mutants.

Bioactivity: Nocodazole is a rapidly-reversible inhibitor of. Nocodazole binds to -tubulin and disruptsmicrotubule

microtubule assembly/disassembly dynamics, which preventsmitosis and induces apoptosis in tumor cells. Nocodazoleinhibits , activates .Bcr-Abl CRISPR/Cas9

Bioactivity: ON 146040 is a potent and ( 14 and 20 nM,PI3K PI3K IC50respectively) inhibitor. ON 146040 also inhibits (Abl1











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Bioactivity: Rebastinib (DCC-2036) is a conformational control Bcr-Ablinhibitor for and with of 0.8 nM andAbl1WT Abl1T315I IC504 nM, also inhibits SRC, KDR, FLT3, and Tie-2, and lowactivity to seen towards c-Kit.

Bioactivity: SNIPER(ABL)-013, conjugating GNF5 (ABL inhibitor) to Bestatin(IAP ligand) with a linker, induces the reduction of BCR-ABLprotein with a DC of 20 M .50

[1]

Bioactivity: SNIPER(ABL)-015, conjugating GNF5 (ABL inhibitor) to MV-1 (IAPligand) with a linker, induces the reduction of BCR-ABLprotein with a DC of 5 M .50

[1]

Bioactivity: SNIPER(ABL)-019, conjugating Dasatinib (ABL inhibitor) to MV-1(IAP ligand) with a linker, induces the reduction of BCR-ABLprotein with a DC of 0.3 M .50

[1]

Bioactivity: SNIPER(ABL)-020, conjugating Dasatinib (ABL inhibitor) toBestatin (IAP ligand) with a linker, induces the reduction ofBCR-ABL protein .[1]

Bioactivity: SNIPER(ABL)-024, conjugating GNF5 (ABL inhibitor) to LCL161derivative (IAP ligand) with a linker, induces the reductionof BCR-ABL protein with a DC of 5M .50

[1]

Bioactivity: SNIPER(ABL)-033, conjugating HG-7-85-01 (ABL inhibitor) toLCL161 derivative (IAP ligand) with a linker, induces thereduction of BCR-ABL protein with a DC of 0.3 M .50

[1]

Bioactivity: SNIPER(ABL)-039, conjugating Dasatinib (ABL inhibitor) toLCL161 derivative (IAP ligand) with a linker, induces thereduction of BCR-ABL protein with a DC of 10 nM. s are50 IC500.54 nM, 10 nM, 12 nM, and 50 nM for , cIAP1, cIAP2, XIABL

Bioactivity: SNIPER(ABL)-044, conjugating HG-7-85-01 (ABL inhibitor) toBestatin (IAP ligand) with a linker, induces the reduction ofBCR-ABL protein with a DC of 10 M .50

[1]

Bioactivity: SNIPER(ABL)-047, conjugating HG-7-85-01 (ABL inhibitor) toMV-1 (IAP ligand) with a linker, induces the reduction ofBCR-ABL protein with a DC of 2 M .50

[1]


Rebastinib (DCC-2036) Cat. No.: HY-13024

SNIPER(ABL)-013 Cat. No.: HY-111860








https://www.MedChemExpress.com/DCC-2036.htmlhttps://www.MedChemExpress.com/sniper-abl-013.htmlhttps://www.MedChemExpress.com/sniper-abl-015.htmlhttps://www.MedChemExpress.com/sniper-abl-019.htmlhttps://www.MedChemExpress.com/sniper-abl-020.htmlhttps://www.MedChemExpress.com/sniper-abl-024.htmlhttps://www.MedChemExpress.com/sniper-abl-033.htmlhttps://www.MedChemExpress.com/sniper-abl-039.htmlhttps://www.MedChemExpress.com/sniper-abl-044.htmlhttps://www.MedChemExpress.com/sniper-abl-047.html



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Bioactivity: SNIPER(ABL)-049, conjugating Imatinib (ABL inhibitor) toBestatin (IAP ligand) with a linker, induces the reduction ofBCR-ABL protein with a DC of 100 M .50

[1]

Bioactivity: SNIPER(ABL)-050, conjugating Imatinib (ABL inhibitor) to MV-1(IAP ligand) with a linker, induces the reduction of BCR-ABLprotein .[1]

Bioactivity: SNIPER(ABL)-058, conjugating Imatinib (ABL inhibitor) toLCL161 derivative (IAP ligand) with a linker, induces thereduction of protein with a DC of 10 M .BCR-ABL 50

[1]

Bioactivity: SNIPER(ABL)-062, in which an ABL inhibitor is linked to aligand of cIAP1 via a linker containing a variablepolyethylene glycol (PEG) unit, shows a potent activity todegrade the protein .BCR-ABL [1]

Bioactivity: XL228 is a multi-targeted tyrosine kinase inhibitor with sIC50of 5, 3.1, 1.6, 6.1, 2 nM for , , , Bcr-Abl Aurora A IGF-1R Srcand , respectively.Lyn





XL228 Cat. No.: HY-15749
https://www.MedChemExpress.com/sniper-abl-049.htmlhttps://www.MedChemExpress.com/sniper-abl-050.htmlhttps://www.MedChemExpress.com/sniper-abl-058.htmlhttps://www.MedChemExpress.com/sniper-abl-062.htmlhttps://www.MedChemExpress.com/XL228.html

BMX Kinase

Bmx is a non-receptor tyrosine kinase belonging to the Tec kinasefamily. The protein contains a PH-like domain, which mediatesmembrane targeting by binding to phosphatidylinositol3,4,5-triphosphate (PIP3), and a SH2 domain that binds totyrosine-phosphorylated proteins and functions in signaltransduction. The protein is implicated in several signal transductionpathways including the Stat pathway, and regulates differentiationand tumorigenicity of several types of cancer cells. Bmx ischaracterized by an N-terminal pleckstrin homology domain and hasbeen shown to be a downstream effector of phosphatidylinositol3-kinase. P21-activated kinase 1 (Pak1), another well characterized

effector of phosphatidylinositol 3-kinase, has been implicated in the progression of breast cancer cells.

https://www.MedChemExpress.com/Targets/BMX Kinase.html



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BMX Kinase Inhibitors & Modulators

Bioactivity: BMX-IN-1 is a selective, irreversible inhibitor of bone that targetsmarrow tyrosine kinase on chromosome X (BMX)

Cys in the BMX ATP binding domain with an of 8 nM,496 IC50also targets the related Brutons tyrosine kinase w(BTK)

Bioactivity: CHMFL-BMX-078 is a highly potent and selective type IIirreversible kinase inhibitor with an of 11 nM.BMX IC50

BMX-IN-1 (BMX kinase inhibitor) Cat. No.: HY-80002

CHMFL-BMX-078 (CHMFL-BMX 078) Cat. No.: HY-101267
https://www.MedChemExpress.com/Targets/BMX Kinase.htmlhttps://www.MedChemExpress.com/BMX-IN-1.htmlhttps://www.MedChemExpress.com/CHMFL-BMX-078.html

BtkBruton tyrosine kinase

Bruton tyrosine kinase (Btk) is a member of the Tec family kinaseswith a well-characterized role in B-cell antigen receptor(BCR)-signaling and B-cell activation.Btk plays a crucial role in B cell development and activation throughthe BCR signaling pathway and represents a new target for diseasescharacterized by inappropriate B cell activity. Btk is a kinase expressedexclusively in B cells and myeloid cells and has a well characterized,vital role in B cells highlighted by the human primary immunedeficiency disease, X-linked agammaglobulinemia (XLA), which resultsfrom mutation in the Btk gene. Btk plays an essential role in the BCRsignaling pathway. Antigen binding to the BCR results in B cell

receptor oligomerization, Syk and Lyn kinase activation, followed by Btk kinase activation. Once activated, Btk forms asignaling complex with proteins such as BLNK, Lyn, and Syk and phosphorylates phospholipase C (PLC)2. This leadsto downstream release of intracellular Ca stores and propagation of the BCR signaling pathway through2+

extracellular signal-regulated kinase and NF-B signaling, ultimately resulting in transcriptional changes to foster B cellsurvival, proliferation, and/or differentiation.

https://www.MedChemExpress.com/Targets/Btk.html




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Btk Inhibitors & Modulators

Bioactivity: ()-Zanubrutinib is a potent, selective and orally availableBruton's tyrosine kinase ( ) inhibitor.Btk

Bioactivity: Acalabrutinib is a novel, potent, and highly selective BTKinhibitor, with an of 3 nM and of 8 nM in IC50 EC50 in vitro

assay.

Bioactivity: ARQ 531 is a reversible non-covalent inhibitor of BrutonsTyrosine Kinase ( ), with of 0.85 nM and 0.39 nM forBTK IC s50WT-BTK and C481S-BTK, respectively.

Bioactivity: BMS-935177 is a potent and selective reversible inhibitor ofBrutons tyrosine kinase ( ) with an of 3 nM.Btk IC50

Bioactivity: BMS-986142 is a potent and highly selective reversibleinhibitor of ( ) with an IC Bruton's tyrosine kinase BTK 50of 0.5 nM.

Bioactivity: BMS-986195 is a potent, covalent, irreversible inhibitor ofBrutons tyrosine kinase , with an of


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Bioactivity: Btk inhibitor 1 R enantiomer is a pyrazolo[3,4-d]pyrimidinederivative as a Btk kinase inhibitor. IC50 value: Target: BtkFrom PCT Int. Appl. (2012), WO 2012158843 A2 20121122.

Bioactivity: Btk inhibitor 1R enantiomer Hcl is a pyrazolo[3,4-d]pyrimidinederivative as a Btk kinase inhibitor.

Bioactivity: Btk inhibitor 2 is a ( )Bruton's tyrosine kinase BTKinhibitor extracted from patent US 20170224688 A1.

Bioactivity: CG-806 is a pan Multi-Kinase inhibitor.FLT3/BTK

Bioactivity: CGI-1746 is a potent and highly selective inhibitor ofthe with of 1.9 nM.Btk IC50

Bioactivity: CNX-774 is a potent, selective, and orally available smallmolecule inhibitor of Btk (IC50< 1 nM) that forms aligand-directed covalent bond with Cys-481, a non-conservedamino acid within the active site of the enzyme.

Bioactivity: Evobrutinib is an inhibitor of Bruton's tyrosin kinase ( )Btkinhibitor extracted from patent US20140162983 example 0174.

Bioactivity: Fenebrutinib (GDC-0853) is a potent, selective, andnoncovalent bruton's tyrosine kinase ( ) inhibitor with aBtk

of 0.91 nM.Ki

Bioactivity: G-744 is a highly potent, selective inhibitor with anBtk of 2 nM.IC50

Bioactivity: GDC-0834 is a potent and selective inhibitor. GDC-0834BTKinhibits BTK with an in vitro of 5.9 and 6.4 nM inIC50biochemical and cellular assays, respectively, and in vivo

of 1.1 and 5.6 M in mouse and rat, respectively.IC50


Btk inhibitor 1 R enantiomer Cat. No.: HY-13036A

Btk inhibitor 1 R enantiomer hydrochloride Cat. No.: HY-13036B

Btk inhibitor 2 Cat. No.: HY-101766

CG-806 Cat. No.: HY-112646

CGI-1746 Cat. No.: HY-11999

CNX-774 Cat. No.: HY-13943

Evobrutinib (M2951; MSC2364447C) Cat. No.: HY-101215

Fenebrutinib (GDC-0853) Cat. No.: HY-19834

G-744 Cat. No.: HY-102036

GDC-0834 Cat. No.: HY-15427
https://www.MedChemExpress.com/Btk-inhibitor-1-R-enantiomer.htmlhttps://www.MedChemExpress.com/btk-inhibitor-1-r-enantiomer-hydrochloride.htmlhttps://www.MedChemExpress.com/Btk_inhibitor_2.htmlhttps://www.MedChemExpress.com/CG-806.htmlhttps://www.MedChemExpress.com/CGI-1746.htmlhttps://www.MedChemExpress.com/CNX-774.htmlhttps://www.MedChemExpress.com/Evobrutinib.htmlhttps://www.MedChemExpress.com/GDC-0853.htmlhttps://www.MedChemExpress.com/G-744.htmlhttps://www.MedChemExpress.com/GDC-0834.html



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Purity: >98%Clinical Data: No Development ReportedSize: 5 mg


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Purity: >98%Clinical Data: No Development ReportedSize: 10mM x 1mL in DMSO,

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Bioactivity: GDC-0834 Racemate is the racemate form of GDC-0834, which is apotent and selective BTK inhibitor with in vitro IC50s of 5.9and 6.4 nM in biochemical and cellular assays, respectively.IC50 value: 5.9 nM/6.4 nM(biochemical/cellular assay) [1]Target: BTK in vitro: GDC-0834 inhibited BTK with an in vitro

Bioactivity: GDC-0834 (S-enantiomer) is the S-enantiomer of GDC-0834.GDC-0834 is a potent and selective BTK inhibitor.

Bioactivity: Ibrutinib (PCI-32765) is a selective, irreversible Btkinhibitor with an of 0.5 nM.IC50

Bioactivity: Ibrutinib-biotin is a probe that consists of Ibrutinib linkedto biotin via a long chain linker, extracted from patentWO2014059368A1 Compound 1-5, has an of 0.755-1.02 nM forIC50

.BTK

Bioactivity: LFM-A13 is a potent , , inhibitor, inhibitsBTK JAK2 PLKrecombinant BTK, Plx1 and PLK3 with s of 2.5 M, 10 M andIC5061 M; LFM-A13 shows no effects on JAK1 and JAK3, Src familykinase HCK, EGFR and IRK.

Bioactivity: The product is the analog of ONO-4059, ONO-4059 is a highlypotent and selective Btk inhibitor with an IC50 in the sub-nMrange.

Bioactivity: PCI 29732 is a selective and irreversible Btk inhibitor withIC50 of 8.2 nM in a FRET based biochemical enzymology assay.

Bioactivity: PCI-33380 is an irreversible Bruton's Tyrosine Kinase (BTK)inhibitor (fluorescent probe).

Bioactivity: PF-06250112 is a potent, highly selective, orally bioavailable inhibitor with an of 0.5 nM, shows inhibitory effectBTK IC50

toward and with sBMX nonreceptor tyrosine kinase TEC IC50of 0.9 nM and 1.2 nM, respectively .[1]

Bioactivity: PRN1008 is a reversible covalent, selective and oral activeinhibitor of Brutons Tyrosine Kinase , with an of(BTK) IC501.3 nM.

GDC-0834 Racemate Cat. No.: HY-15427A

GDC-0834 S-enantiomer Cat. No.: HY-15427B

Ibrutinib (PCI-32765) Cat. No.: HY-10997

Ibrutinib-biotin Cat. No.: HY-100342

LFM-A13 Cat. No.: HY-18009

ONO-4059 analog Cat. No.: HY-18951

PCI 29732 Cat. No.: HY-18010

PCI-33380 Cat. No.: HY-100335

PF-06250112 Cat. No.: HY-117900

PRN1008 Cat. No.: HY-112166
https://www.MedChemExpress.com/GDC-0834-Racemate.htmlhttps://www.MedChemExpress.com/GDC-0834-S-enantiomer.htmlhttps://www.MedChemExpress.com/PCI-32765.htmlhttps://www.MedChemExpress.com/Ibrutinib-biotin.htmlhttps://www.MedChemExpress.com/LFM-A13.htmlhttps://www.MedChemExpress.com/ONO-4059-analog.htmlhttps://www.MedChemExpress.com/PCI-29732.htmlhttps://www.MedChemExpress.com/PCI-33380.htmlhttps://www.MedChemExpress.com/pf-06250112.htmlhttps://www.MedChemExpress.com/PRN1008.html


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Purity: >98%Clinical Data: Phase 2Size: 5 mg, 10 mg, 50 mg, 100 mg


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Bioactivity: QL47 is a potent, selective and irreversible BTK kinaseinhibitor with IC50 of 7 nM. IC50 Value: 7 nM Target: Btk invitro: QL47 inhibits BTK kinase activity with an IC50 of 7 nM,inhibits autophosphorylation of BTK on Tyr223 in cells with anEC50 of 475 nM and inhibits phosphorylation of a downstream

Bioactivity: RN486 is a selective Btk inhibitor with an IC50 Value of 4.0nM.

Bioactivity: Spebrutinib (AVL-292; CC-292) is a covalent, orally active,and highly selective with an of 0.5 nM.IC50

Bioactivity: Spebrutinib besylate (AVL-292 benzenesulfonate; CC-292besylate) is a potent inhibitor of kinase activity (Btk


c-FmsCSF-1 receptor;colony stimulating factor 1 receptor;CSF-1R;CSF1R

c-FMS (CSF1R, CSF-1R) is located at the cell plasma membrane. c-FMSis the receptor for the ligand colony stimulating factor-1 (CSF1).c-FMS is an integral transmembrane glycoprotein that exhibitsligand-induced tyrosine-specific protein kinase activity, which triggersa signaling cascade eventually affecting transcription ofCSF1-responsive genes. c-FMS tyrosine phosphorylation is inducedupon binding of CSF1, leading to activation of Ras/Erk and class I-Aphosphatidylinositol 3-kinase signaling pathways, which in turnactivate the signal transducers and activators of transcription (STATs)pathways, specifically STAT1, STAT3, and STAT5. c-FMS activation byCSF1 results in increased growth, proliferation and differentiation.
https://www.MedChemExpress.com/Targets/c-Fms.html


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c-Fms Inhibitors & Modulators

Bioactivity: AZD7507 is a potent and orally active inhibitor, withCSF-1Rantitumor activity.

Bioactivity: BLZ945 is a potent, selective and brain-penetrant CSF-1Rinhibitor with an of 1 nM, showing more than 1,000-foldIC50selectivity against its closest receptor tyrosine kinasehomologs.

Bioactivity: c-Fms-IN-1 is a inhibitor with an of 0.0008FMS kinase IC50M .[1]

Bioactivity: c-Fms-IN-2 is a inhibitor with an of 0.024FMS kinase IC50M.

Bioactivity: c-Fms-IN-3 is a novel c-Fms kinase inhibitor with a potentialas anti-inflammatory agent and antirheumatic agent.

Bioactivity: c-Fms-IN-6 is a potent inhibitor of , with an ofc-FMS IC5010 nM for unphosphorylated c-FMS, also weakly inhibitsunphosphorylated c-KIT and PDGFR ( , > 1 M). Used inIC50the research of autoimmune diseases .[1]

Bioactivity: c-Fms-IN-7 is a inhibitor extracted from patentcFMSWO2011079076A1, example159, has an of 18.5 nM .IC50

[1]Bioactivity: c-Fms-IN-8 (compound 4a) is a colony stimulating factor-1

Type II inhibitor, with an ofreceptor (CSF-1R, c-FMS) IC509.1 nM .[1]

Bioactivity: c-Fms-IN-9 is a inhibitor extracted from patentc-FMSWO2014145023A1, Compound Example 7. c-Fms-IN-9 inhibitsunphosphorylated c-FMS kinase ( ) and with s ofuFMS uKIT IC50



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Bioactivity: CSF1R-IN-1 is a inhibitor with an with an of 0.5CSF1R IC50nM.

Bioactivity: CSF1R-IN-2 (compound 5) is an oral-active inhibitor of ,SRC and , with values of 0.12 nM, 0.14 nM andMET c-FMS IC50

0.76 nM for SRC, MET and c-FMS respectively .[1]

Bioactivity: Edicotinib is a selective and orally available inhibitor,colony-stimulating factor-1 (CSF-1) receptor

and has entered phase IIA clinical trial to study rheumatoidarthritis (RA) despite disease.

Bioactivity: GENZ-882706 is a potent colony stimulating factor-1 receptor () Inhibitor extracted from patent WO 2017015267A1.CSF-1R

Bioactivity: GENZ-882706(Raceme) is the racemate of GENZ-882706. Bioactivity: GW2580 is an orally bioavailable inhibitor of c-Fms kinasewhich completely inhibits human cFMS kinase at 0.06 M.in vitro

Bioactivity: JTE-952 is a potent, oral active and selective Type IIinhibitor of ( colony stimulating factor-1 receptor CSF-1R or

, type III receptor tyrosine kinase), with valuescFMS IC50of 13 nM and 261 nM for CSF1R and TrkA , respectively.Effective against a mouse collagen-induced model of arthritis

Bioactivity: Ki-20227 is a highly selective c-Fms tyrosine kinase(CSF1R)inhibitor with IC50 value of 2 nM; 6 fold and > 100 foldselectivity over VEGFR2(IC50=12 nM) andc-Kit/PDGFR(IC50=451/217 nM), respectively. IC50 value:Target: CSF1R in vitro: Ki20227 did not inhibit other kinases

Bioactivity: OSI-930 is a potent inhibitor of Kit, KDR and CSF-1R with IC50of 80 nM, 9 nM and 15 nM, respectively; also potent to Flt-1,c-Raf and Lck and low activity against PDGFR/, Flt-3 andAbl. IC50 value: 9 nM(VEGFR2); 15 nM(CSF1R); 80 nM (Kitactivated) [1] Target: VEGFR2/Kit/CSF1R in vitro: OSI-930

Bioactivity: Pazopanib Hydrochloride (GW786034 Hydrochloride) is a novelmulti-target inhibitor of , , , ,VEGFR1 VEGFR2 VEGFR3 PDGFR

, , and with an of 10, 30, 47, 84, 74,c-Kit FGFR1 c-Fms IC50140 and 146 nM, respectively.

CSF1R-IN-1 Cat. No.: HY-101774

CSF1R-IN-2 Cat. No.: HY-111787

Edicotinib (JNJ-40346527) Cat. No.: HY-109086

GENZ-882706 (RA03546849) Cat. No.: HY-101526

GENZ-882706(Raceme) (GENZ-882706 racemate) Cat. No.: HY-101526R

GW2580 Cat. No.: HY-10917

JTE-952 Cat. No.: HY-122906

Ki20227 Cat. No.: HY-10408

OSI-930 Cat. No.: HY-10204

Pazopanib Hydrochloride (GW786034 (Hydrochloride)) Cat. No.: HY-12009
https://www.MedChemExpress.com/CSF1R-IN-1.htmlhttps://www.MedChemExpress.com/TPX-022.htmlhttps://www.MedChemExpress.com/Edicotinib.htmlhttps://www.MedChemExpress.com/GENZ-882706.htmlhttps://www.MedChemExpress.com/GENZ-882706_Raceme_.htmlhttps://www.MedChemExpress.com/GW2580.htmlhttps://www.MedChemExpress.com/JTE-952.htmlhttps://www.MedChemExpress.com/Ki20227.htmlhttps://www.MedChemExpress.com/OSI-930.htmlhttps://www.MedChemExpress.com/Pazopanib-Hydrochloride.html


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Bioactivity: Pexidartinib (PLX-3397) is a potent, selective andATP-competitive and inhibitor, withCSF1R (cFMS) c-Kit

s of 20 and 10 nM, respectively. Pexidartinib exhibits 10-IC50to 100-fold selectivity for c-Kit and CSF1R over other rela

Bioactivity: Pexidartinib hydrochloride (PLX-3397 hydrochloride) is apotent, selective and ATP-competitive andCSF1R (cFMS)

inhibitor, with s of 20 and 10 nM, respectively.c-Kit IC50Pexidartinib exhibits 10- to 100-fold selectivity for c-Kitand CSF1R over other related kinases. Anti-cancer activity

Bioactivity: PLX647 is a highly specific dual FMS/KIT kinase inhibitor withIC50 of 28/16 nM respectively. IC50 value: 28/16 nM(FMS/KIT)[1] Target: FMS/KIT dual inhibitor in vitro: PLX647 was testedagainst a panel of 400 kinases at a concentration of 1 M,35-fold above its FMS enzymatic IC50 and 60-fold above its KIT


Pexidartinib (PLX-3397) Cat. No.: HY-16749

Pexidartinib hydrochloride (PLX-3397 hydrochloride) Cat. No.: HY-16749A

PLX647 Cat. No.: HY-13838
https://www.MedChemExpress.com/Pexidartinib.htmlhttps://www.MedChemExpress.com/pexidartinib-hydrochloride.htmlhttps://www.MedChemExpress.com/PLX647.html


c-KitSCFR;CD117

c-Kit (Mast/stem cell growth factor receptor, SCFR or CD117) is aproteinthat in humans is encoded by the KIT gene. c-Kit (CD117) is animportant cell surface marker used to identify certain types ofhematopoietic(blood) progenitors in the bone marrow. c-Kit is acytokine receptor expressed on the surface of hematopoietic stemcells as well as other cell types. Altered forms of this receptor may beassociated with some types of cancer. c-Kit is a receptor tyrosinekinase type III, which binds to stem cell factor. When c-Kit binds tostem cell factor (SCF) it forms adimer that activates its intrinsictyrosine kinase activity, that in turn phosphorylates and activatessignal transduction molecules that propagate the signal in the cell.

Signalling through c-Kit plays a role in cell survival, proliferation, and differentiation.
https://www.MedChemExpress.com/Targets/c-Kit.html



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c-Kit Inhibitors & Modulators

Bioactivity: AC710 is a potent inhibitor with s of 0.6, 1.57, 1,PDGFR Kd1.3, 1.0 nM for FLT3, CSF1R, KIT, PDGFR and PDGFR,respectively.

Bioactivity: Amuvatinib (MP470) is a multi-targeted receptor tyrosinekinases inhibitor, which inhibits , c-Kit (D816V) c-Kit

, , , , and(D816H) c-Kit (V560G) c-Kit (V654A) PDGFR (D842V) with s of 950 nM, 10 nM, 34 nM, 127 PDGFR (V561D) IC50

Bioactivity: Amuvatinib hydrochloride (MP470 hydrochloride) is amulti-targeted receptor tyrosine kinases inhibitor, whichinhibits , , , c-Kit (D816V) c-Kit (D816H) c-Kit (V560G) c-Kit

, , and with s of(V654A) PDGFR (D842V) PDGFR (V561D) IC50950 nM, 10 nM, 34 nM, 127 nM, 81 nM, and 40 nM, respectively

Bioactivity: AST 487 is a kinase inhibitor with of 880 nM,RET IC50inhibits RET autophosphorylation and activation of downstreameffectors, also inhibits with of 520 nM.Flt-3 IC50

Bioactivity: Avapritinib is a potent and selective exon 17 mutant KIT kinaseinhibitor with of 0.27 nM for .IC50 KIT D816V

Bioactivity: AZD2932 is a potent and multi-targeted kinase inhibitor, , and with s of 8, 4, 7 and 9 nMVEGFR2 PDGF Flt-3 c-Kit IC50

in cell assay, respectively.

Bioactivity: AZD3229 is a potent pan- mutant inhibitor for the treatmentKITof gastrointestinal stromal tumors.

Bioactivity: AZD3229 Tosylate is a potent pan-KIT mutant inhibitor for thetreatment of gastrointestinal stromal tumors.

Bioactivity: c-Kit-IN-1 is a potent inhibitor of and withc-Kit c-Mets of



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Purity: 95.0%Clinical Data: Phase 3Size: 10mM x 1mL in Water,

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Bioactivity: Cabozantinib is a potent multiple receptor tyrosine kinasesinhibitor that inhibits , , , and withVEGFR2 c-Met Kit Axl Flt3

s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.IC50

Bioactivity: CHMFL-KIT-033 is a potent and selective inhibitor of c-KIT for gastrointestinal stromal tumors (GISTs),T670I mutant

with an of 0.045 M .IC50[1]

Bioactivity: Dovitinib is a multi-targeted tyrosine kinase inhibitor withs of 1, 2, 8/9, 10/13/8, 27/210 nM for , ,IC50 FLT3 c-Kit

, and , respectively.FGFR1/3 VEGFR1/2/3 PDGFR/

Bioactivity: Flumatinib (HHGV678) is a multi-kinase inhibitor with IC50Values of 1.2 nM, 307.6 nM and 2662 nM for c-Abl, PDGFR andc-Kit respectively.

Bioactivity: Flumatinib mesylate (HH-GV-678 mesylate), a derivative ofimatinib, is a multi-kinase inhibitor with IC50 Values of 1.2nM, 307.6 nM and 2662 nM for c-Abl, PDGFR and c-Kitrespectively. IC50 Value: 1.2 nM (c-Abl); 307.6 nM(PDGFR);2662 nM (c-Kit) [1] Target: c-Abl; c-Kit; PDGRF in vitro:

Bioactivity: Imatinib (STI571) is a tyrosine kinases inhibitor thatinhibits , , and ( =100 nM) tyrosinec-Kit Bcr-Abl PDGFR IC50kinases.

Bioactivity: Imatinib Mesylate (STI571 Mesylate) is a tyrosine kinasesinhibitor that inhibits , , and ( =100c-Kit Bcr-Abl PDGFR IC50nM) tyrosine kinases.

Bioactivity: ISCK03 is a specific inhibitor.SCF/c-Kit

Bioactivity: Masitinib is an orally available inhibitor with an ofKit IC50200 nM. It also inhibits with an of 540 nM/800PDGFR/ IC50nM nM.

Bioactivity: Masitinib mesylate is a novel inhibitor for and Kit PDGFR/with of 200 nM and 540 nM/800 nM, and has weak inhibitionIC50to ABL and c-Fms.

Cabozantinib (XL184; BMS-907351) Cat. No.: HY-13016

CHMFL-KIT-033 Cat. No.: HY-128589

Dovitinib (CHIR-258; TKI258) Cat. No.: HY-50905

Flumatinib (HHGV678) Cat. No.: HY-13904

Flumatinib mesylate (HHGV678 mesylate) Cat. No.: HY-13905

Imatinib (STI571; CGP-57148B) Cat. No.: HY-15463

Imatinib Mesylate (STI571 (Mesylate); CGP-57148B (Mesylate)) Cat. No.: HY-50946

ISCK03 Cat. No.: HY-101443

Masitinib (AB1010) Cat. No.: HY-10209

Masitinib mesylate (AB-1010 mesylate) Cat. No.: HY-10209A
https://www.MedChemExpress.com/Cabozantinib.htmlhttps://www.MedChemExpress.com/chmfl-kit-033.htmlhttps://www.MedChemExpress.com/Dovitinib.htmlhttps://www.MedChemExpress.com/Flumatinib.htmlhttps://www.MedChemExpress.com/flumatinib-mesylate.htmlhttps://www.MedChemExpress.com/Imatinib.htmlhttps://www.MedChemExpress.com/Imatinib-Mesylate.htmlhttps://www.MedChemExpress.com/ISCK03.htmlhttps://www.MedChemExpress.com/Masitinib.htmlhttps://www.MedChemExpress.com/masitinib-mesylate.html


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Bioactivity: Motesanib is a potent ATP-competitive inhibitor ofwith sof 2 nM/3 nM/6 nM,VEGFR1/2/3 IC50

respectively, and has similar activity against Kit, and isappr 10-fold more selective for VEGFR than PDGFR andRet.

Bioactivity: Motesanib Diphosphate is a potent ATP-competitive inhibitor of with s of 2 nM/3 nM/6 nM, respectively, andVEGFR1/2/3 IC50

has similar activity against Kit, and is approximately 10-foldmore selective for VEGFR than PDGFR and Ret.

Bioactivity: OSI-930 is a potent inhibitor of Kit, KDR and CSF-1R with IC50of 80 nM, 9 nM and 15 nM, respectively; also potent to Flt-1,c-Raf and Lck and low activity against PDGFR/, Flt-3 andAbl. IC50 value: 9 nM(VEGFR2); 15 nM(CSF1R); 80 nM (Kitactivated) [1] Target: VEGFR2/Kit/CSF1R in vitro: OSI-930

Bioactivity: Pazopanib (GW786034) is a novel multi-target inhibitor of, , , , , , and VEGFR1 VEGFR2 VEGFR3 PDGFR c-Kit FGFR1 c-Fms

with s of 10, 30, 47, 84, 74, 140 and 146 nM,IC50respectively.

Bioactivity: Pazopanib Hydrochloride (GW786034 Hydrochloride) is a novelmulti-target inhibitor of , , , ,VEGFR1 VEGFR2 VEGFR3 PDGFR

, , and with an of 10, 30, 47, 84, 74,c-Kit FGFR1 c-Fms IC50140 and 146 nM, respectively.

Bioactivity: Pexidartinib (PLX-3397) is a potent, selective andATP-competitive and inhibitor, withCSF1R (cFMS) c-Kit

s of 20 and 10 nM, respectively. Pexidartinib exhibits 10-IC50to 100-fold selectivity for c-Kit and CSF1R over other rela

Bioactivity: Pexidartinib hydrochloride (PLX-3397 hydrochloride) is apotent, selective and ATP-competitive andCSF1R (cFMS)

inhibitor, with s of 20 and 10 nM, respectively.c-Kit IC50Pexidartinib exhibits 10- to 100-fold selectivity for c-Kitand CSF1R over other related kinases. Anti-cancer activity

Bioactivity: PLX647 is a highly specific dual FMS/KIT kinase inhibitor withIC50 of 28/16 nM respectively. IC50 value: 28/16 nM(FMS/KIT)[1] Target: FMS/KIT dual inhibitor in vitro: PLX647 was testedagainst a panel of 400 kinases at a concentration of 1 M,35-fold above its FMS enzymatic IC50 and 60-fold above its KIT

Bioactivity: Ripretinib (DCC-2618) is a pan- and inhibitor, andKIT PDGFRAhas antitumor activity.

Bioactivity: Sitravatinib (MGCD516; MG516) is an orally bioavailable, inhibitor with s of 1.5receptor tyrosine kinase (RTK) IC50

nM, 2 nM, 2 nM, 5 nM, 6nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5nM, and9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT , FLT3, DD


Motesanib (AMG 706; ) Cat. No.: HY-10228

Motesanib Diphosphate (AMG 706 (Diphosphate)) Cat. No.: HY-10229

OSI-930 Cat. No.: HY-10204

Pazopanib (GW786034) Cat. No.: HY-10208

Pazopanib Hydrochloride (GW786034 (Hydrochloride)) Cat. No.: HY-12009

Pexidartinib (PLX-3397) Cat. No.: HY-16749

Pexidartinib hydrochloride (PLX-3397 hydrochloride) Cat. No.: HY-16749A

PLX647 Cat. No.: HY-13838

Ripretinib (DCC-2618) Cat. No.: HY-112306

Sitravatinib (MGCD516; MG516) Cat. No.: HY-16961
https://www.MedChemExpress.com/Motesanib.htmlhttps://www.MedChemExpress.com/Motesanib-Diphosphate.htmlhttps://www.MedChemExpress.com/OSI-930.htmlhttps://www.MedChemExpress.com/Pazopanib.htmlhttps://www.MedChemExpress.com/Pazopanib-Hydrochloride.htmlhttps://www.MedChemExpress.com/Pexidartinib.htmlhttps://www.MedChemExpress.com/pexidartinib-hydrochloride.htmlhttps://www.MedChemExpress.com/PLX647.htmlhttps://www.MedChemExpress.com/DCC-2618.htmlhttps://www.MedChemExpress.com/Sitravatinib.html



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Bioactivity: SU14813 is a multi-targeted receptor tyrosine kinasesinhibitor with s of 50, 2, 4, 15 nM for , ,IC50 VEGFR2 VEGFR1

and .PDGFR KIT

Bioactivity: SU14813 maleate is a multi-targeted receptor tyrosine kinasesinhibitor with s of 50, 2, 4, 15 nM for , ,IC50 VEGFR2 VEGFR1

and .PDGFR KIT

Bioactivity: Telatinib (Bay 57-9352) is an orally active, small moleculeinhibitor of , , , and with sVEGFR2 VEGFR3 PDGF c-Kit IC50of 6, 4, 15 and 1 nM, respectively.

SU14813 Cat. No.: HY-10501

SU14813 maleate Cat. No.: HY-10501A

Telatinib (Bay 57-9352) Cat. No.: HY-10527
https://www.MedChemExpress.com/SU14813.htmlhttps://www.MedChemExpress.com/SU14813-maleate.htmlhttps://www.MedChemExpress.com/Telatinib.html

c-Met/HGFR

c-Met (hepatocyte growth factor receptor, HGFR) is a proteinpossesses tyrosine kinase activity. The primary single chain precursorprotein is post-translationally cleaved to produce the alpha and betasubunits, which are disulfide linked to form the mature receptor.c-Met is a membrane receptor that is essential for embryonicdevelopment and wound healing. Hepatocyte growth factor (HGF) isthe only known ligand of the c-Met receptor. c-Met is normallyexpressed by cells of epithelial origin, while expression of HGF isrestricted to cells of mesenchymalorigin. Upon HGF stimulation,c-Met induces several biological responses that collectively give riseto a program known as invasive growth.

https://www.MedChemExpress.com/Targets/c-Met_HGFR.html



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Purity: 99.36%Clinical Data: No Development ReportedSize: 10mM x 1mL in Water,

1 g

c-Met/HGFR Inhibitors & Modulators

Bioactivity: 2-Phospho-L-ascorbic acid trisodium salt acts as anantioxidant and a stimulator of hepatocyte growth factor

production.(HGF)

Bioactivity: Altiratinib (DCC-2701) is a multi-targeted kinase inhibitorwith s of 2.7, 8, 9.2, 9.3, 0.85, 4.6, 0.83 nM for ,IC50 MET

, , , , , and respectively.TIE2 VEGFR2 FLT3 Trk1 Trk2 Trk3

Bioactivity: AMG-208 is a potent small molecular c-Met inhibitor with anIC50 of 9.3 nM. IC50 value: 9.3 nM Target: c-Met in vitro:AMG-208 shows the potent inhibition of kinase c-Met activitywith IC50 of 9 nM in a cell-free assay. Besides, AMG-208treatment also leads to the inhibition of HGF-mediated c-Met

Bioactivity: AMG-337 is a potent and highly selective small moleculeATP-competitive MET kinase inhibitor. AMG 337 inhibits METkinase activity with an IC50 of < 5nM in enzymatic assays.

Bioactivity: BMS 777607 is a inhibitor for , ,Met-related c-Met Axl and with s of 3.9 nM, 1.1 nM, 1.8 nM and 4.3Ron Tyro3 IC50

nM, respectively, and 40-fold more selective for Met-relatedtargets than Lck, VEGFR-2, and TrkA/B, with more than 500-foldgreater selectivity versus all other receptor and non receptor

Bioactivity: BMS-794833 is a and inhibitor extracted fromVEGFR2 Metpatent WO2009094417, compound example 1; has s of 15 andIC501.7 nM, respectively.

Bioactivity: c-Kit-IN-1 is a potent inhibitor of and withc-Kit c-Mets of


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Bioactivity: Capmatinib (INCB28060) is a potent and selective c-METkinase inhibitor. Capmatinib (INCB28060) inhibits c-MET kinaseactivity with an average of 0.13 nM.IC50

Bioactivity: CEP-40783 is a potent, selective and orally availableinhibitor of and with values of 7 nM and 12AXL c-Met IC50nM, respectively.

Bioactivity: Crizotinib is a potent inhibitor of and with anc-Met ALK of 11 nM and 24 nM in cell-based assays, respectively.IC50

Bioactivity: Crizotinib hydrochloride is a potent inhibitor of andc-Met with s of 11 nM and 24 nM in cell-based assays,ALK IC50

respectively.

Bioactivity: CSF1R-IN-2 (compound 5) is an oral-active inhibitor of ,SRC and , with values of 0.12 nM, 0.14 nM andMET c-FMS IC50

0.76 nM for SRC, MET and c-FMS respectively .[1]

Bioactivity: Dihexa is an orally active, blood-brain barrier-permeableangiotensin IV analog; exhibits high affinity bindinghepatocyte growth factor ( ) with a of 65 pM.HGF Kd

Bioactivity: Ensartinib (X-396) is a potent and dual / inhibitorALK METwith s of


Purity: >98%Clinical Data: Phase 1Size: 5 mg, 10 mg, 50 mg


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Bioactivity: Glumetinib (SCC244) is a potent and highly selective c-Met inhibitor with an of 0.42 nM. Glumetinib showskinase IC50

antitumor activity and a superior safety margin .[1]

Bioactivity: Golvatinib (E-7050) is a potent dual inhibitor of both and kinases with s of 14 and 16 nM,c-Met VEGFR2 IC50

respectively.

Bioactivity: JNJ-38877605 is an ATP-competitive inhibitor of c-Met withIC50 of 4 nM, 600-fold selective for c-Met than 200 othertyrosine and serine-threonine kinases. IC50 value: 4 nM [1]Target: c-Met in vitro: JNJ-38877605 shows more than 600-foldselectivity for c-Met compared with more than 200 other

Bioactivity: JNJ-38877618 is a potent, highly selective, orallybioavailable kinase inhibitor with s of 2 and 3 nMMet IC50for wild type and mutant Met, respectively.

Bioactivity: Merestinib (LY2801653) is a type-II ATP competitive, slow-offinhibitor of tyrosine kinase with a dissociationMETconstant ( ) of 2 nM.Ki

Bioactivity: Merestinib dihydrochloride (LY2801653 dihydrochloride) is atype-II ATP competitive, slow-off inhibitor of tyrosineMETkinase with a dissociation constant ( ) of 2 nM.Ki

Bioactivity: MGCD-265-analog (structurally related to MGCD-265) is anorally bioavailable multitargeted tyrosine kinase inhibitorwith potential antineoplastic activity with IC50 of 29 nM and10 nM for c-Met and VEGFR2, respectively. IC50 value:10 nM(VEGFR2), 29 nM(c-Met) [1] Target:VEGFR, c-Met in vivo:

Bioactivity: MK-2461 is a novel ATP-competitive multitargeted inhibitor ofactivated c-Met with a mean IC50 of 2.5 nM.

Bioactivity: MK-8033 is a novel and specific dual ATP competitive c-Met/Roninhibitor (IC50=1 nM Wt c-Met) under investigation as atreatment for cancer. IC50 Value: 1 nM (Wt c-Met); 2.0 nM(c-Met N1100Y) [1] Target: c-Met/Ron in vitro: MK-8033 binds3-fold more tightly to phosphorylated c-Met kinase domain (Kd=

Bioactivity: MK8033 Hcl is a novel and specific dual ATP competitivec-Met/Ron inhibitor (IC50=1 nM Wt c-Met) under investigationas a treatment for cancer.

Glumetinib (SCC244) Cat. No.: HY-116000

Golvatinib (E-7050) Cat. No.: HY-13068

JNJ-38877605 Cat. No.: HY-50683

JNJ-38877618 Cat. No.: HY-111050

Merestinib (LY2801653) Cat. No.: HY-15514

Merestinib dihydrochloride (LY2801653 (dihydrochloride)) Cat. No.: HY-15514A

MGCD-265 analog Cat. No.: HY-10991

MK-2461 Cat. No.: HY-50703

MK-8033 Cat. No.: HY-13299

MK-8033 hydrochloride Cat. No.: HY-13299A
https://www.MedChemExpress.com/glumetinib.htmlhttps://www.MedChemExpress.com/e-7050.htmlhttps://www.MedChemExpress.com/JNJ-38877605.htmlhttps://www.MedChemExpress.com/JNJ-38877618.htmlhttps://www.MedChemExpress.com/LY2801653.htmlhttps://www.MedChemExpress.com/LY2801653-dihydrochloride.htmlhttps://www.MedChemExpress.com/MGCD-265-analog.htmlhttps://www.MedChemExpress.com/MK-2461.htmlhttps://www.MedChemExpress.com/MK-8033.htmlhttps://www.MedChemExpress.com/MK-8033-hydrochloride.html


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Bioactivity: Ningetinib is a potent, orally bioavailable small moleculetyrosine kinase inhibitor ( ) with s of 6.7, 1.9 andTKI IC50



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Bioactivity: SCR-1481B1 (c-Met inhibitor 2) is a potent compound that hasactivity against cancers dependent upon Met activation andalso has activity against cancers as a VEGFR inhibitor.

Bioactivity: SGX-523 is a selective Met inhibitor with IC50 of 4 nM, noactivity to BRAFV599E, c-Raf, Abl and p38. IC50 value: 4 nM[1] Target: Met in vitro: SGX-523 belongs to the class ofc-Met/hepatocyte growth factor receptor (HGFR) tyrosine kinaseinhibitors. SGX-523 stabilizes MET in a unique inactive

Bioactivity: SRI 31215 (TFA), a triplex inhibitor of , matriptase hepsinand with s ofhepatocyte growth factor activator (HGFA) IC500.69 M, 0.65 M, 0.3 M, blocks pro-HGF activation and thusmimics the activity of HAI-1/2 .[1]

Bioactivity: SU11274 is a selective inhibitor with of 10 nM,Met IC50but has no effects on PGDFR, EGFR or Tie2.

Bioactivity: TAS-115 is a potent and hepatocyte growth factorVEGFRreceptor ( )-targeted kinase inhibitor with sc-Met/HGFR IC50of 30 and 32 nM for rVEGFR2 and rMET, respectively.

Bioactivity: TAS-115 mesylate is a potent and hepatocyte growthVEGFRfactor receptor ( )-targeted kinase inhibitor,c-Met/HGFRwith s of 30 and 32 nM for rVEGFR2 and rMET, respectively.IC50

Bioactivity: Tepotinib (EMD-1214063) is a potent and selective c-Metinhibitor with IC50 of 4 nM, >200-fold selective for c-Metthan IRAK4, TrkA, Axl, IRAK1, and Mer.

Bioactivity: Tivantinib is a novel and highly selective tyrosinec-Metkinase inhibitor with of 355 nM.Ki

Bioactivity: A Tyrosine kinase inhibitor. Bioactivity: X-376 is a potent and dual / inhibitor with sALK MET IC50of 0.61 nM and 0.69 nM, respectively.

SCR-1481B1 (c-Met inhibitor 2) Cat. No.: HY-18711A

SGX-523 Cat. No.: HY-12019

SRI 31215 TFA Cat. No.: HY-114363A

SU11274 (PKI-SU11274) Cat. No.: HY-12014

TAS-115 Cat. No.: HY-12423

TAS-115 mesylate (TAS-115 methanesulfonate) Cat. No.: HY-12423A

Tepotinib (EMD-1214063) Cat. No.: HY-14721

Tivantinib (ARQ 197) Cat. No.: HY-50686

Tyrosine kinase inhibitor Cat. No.: HY-10421

X-376 Cat. No.: HY-16590
https://www.MedChemExpress.com/c-Met-inhibitor-2.htmlhttps://www.MedChemExpress.com/SGX-523.htmlhttps://www.MedChemExpress.com/sri-31215-tfa.htmlhttps://www.MedChemExpress.com/SU11274.htmlhttps://www.MedChemExpress.com/TAS-115.htmlhttps://www.MedChemExpress.com/TAS-115_mesylate.htmlhttps://www.MedChemExpress.com/EMD-1214063.htmlhttps://www.MedChemExpress.com/Tivantinib.htmlhttps://www.MedChemExpress.com/Tyrosine-kinase-inhibitor.htmlhttps://www.MedChemExpress.com/Ensartinib.html

Discoidin Domain Receptor

Discoidin domain receptors (DDRs) are receptor tyrosine kinases withthe unique ability among receptor tyrosine kinases to respond tocollagen. Several signaling molecules have been implicated in DDRsignaling, including Shp-2, Src, and MAPK pathways. DDRs have beenreported to induce the expression of various genes including matrixmetalloproteinases and bone morphogenetic proteins, but theregulatory mechanisms underlying DDR-induced gene expressionremain to be determined. DDRs regulate cell-collagen interactions innormal and pathological conditions and thus are emerging as majorsensors of collagen matrices and potential novel therapeutic targets.

https://www.MedChemExpress.com/Targets/Discoidin Domain Receptor.html



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Purity: >98%Clinical Data: No Development ReportedSize:


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Discoidin Domain Receptor Inhibitors & Modulators

Bioactivity: DDR Inhibitor is a potent discoidin domain receptor (DDR)inhibitor, with an of 3.3 nM for DDR2, and shows 53%IC50inhibition on DDR1 at 1.5 nM.

Bioactivity: DDR1-IN-1 is a potent and selective DDR1 receptor tyrosine inhibitor with an of 105 nM; 4-fold less potent forkinase IC50

DDR2 (IC = 413 nM) .50[1]

Bioactivity: DDR1-IN-1 dihydrochloride is a potent and selective DDR1 inhibitor with an of 105 nM;receptor tyrosine kinase IC50

4-fold less potent for DDR2 (IC = 413 nM) .50[1]

Bioactivity: DDR1-IN-2 is a potent inhibitor of discoidin domain receptor 1( ), with an of 13.1 nM, and also less potentlyDDR1 IC50inhibits DDR2, with an of 203 nM.IC50

Bioactivity: DDR1-IN-3 is a selective Discoidin Domain Receptor 1 (DDR1)inhibitor, with an value of 9.4 nM.IC50

Bioactivity: Sitravatinib (MGCD516; MG516) is an orally bioavailable, inhibitor with s of 1.5receptor tyrosine kinase (RTK) IC50

nM, 2 nM, 2 nM, 5 nM, 6nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5nM, and9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT , FLT3, DD

DDR Inhibitor Cat. No.: HY-W018931

DDR1-IN-1 Cat. No.: HY-13979

DDR1-IN-1 dihydrochloride Cat. No.: HY-13979A

DDR1-IN-2 Cat. No.: HY-U00444

DDR1-IN-3 Cat. No.: HY-100695

Sitravatinib (MGCD516; MG516) Cat. No.: HY-16961
https://www.MedChemExpress.com/Targets/Discoidin Domain Receptor.htmlhttps://www.MedChemExpress.com/DDR_Inhibitor.htmlhttps://www.MedChemExpress.com/DDR1-IN-1.htmlhttps://www.MedChemExpress.com/ddr1-in-1-dihydrochloride.htmlhttps://www.MedChemExpress.com/DDR1-IN-2.htmlhttps://www.MedChemExpress.com/DDR1-IN-3.htmlhttps://www.MedChemExpress.com/Sitravatinib.html

DYRKDual specificity tyrosine phosphorylation regulated kinase;Dual specificity tyrosine regulated kinase

Mammalian DYRKs are a subfamily of mitogen-activated proteinkinase-related protein kinases and are originally discovered on thebasis of homology to the Yak1 and Saccharomyces cerevisiae

mini-brain kinases. DYRKs possess Ser/ThrDrosophilaphosphorylation activity as well as autophosphorylation activity onTyr residue(s).Two isoforms of DYRK, DYRK1A and DYRK1B, co-immunoprecipitatewith HAN11 when coexpressed in COS cells indicating that theproteins interact in mammalian cells. Co-expression of DYRK1A,DYRK1B, or DYRK2 with a series of glycogen synthase mutants withSer/Ala substitutions at the phosphorylation sites in COS cells

revealed that protein kinases cause phosphorylation of site 3a in glycogen synthase. Control of glycogen synthase byDYRK represents a novel mechanism, and a potentially novel pathway, for the regulation of glycogen synthesis.

https://www.MedChemExpress.com/Targets/DYRK.html



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DYRK Inhibitors & Modulators

Bioactivity: AZ191 is a potent inhibitor that selectively inhibits DYRK1Bwith of 17 nM .IC50

[1]Bioactivity: EHT 5372 is a strong inhibitor of family kinases, withDYRKs

of 0.22, 0.28 nM for DYRK1A and DYRK1B, respectively.IC s50

Bioactivity: Harmine is a natural dual-specificity tyrosinephosphorylation-regulated kinase ( ) inhibitor with(DYRK)anticancer and anti-inflammatory activities.

Bioactivity: ID-8 is a DYRK inhibitor, and sustains embryonic stem cellself-renewal in long-term culture.

Bioactivity: Mirk-IN-1 is a potent inhibitor of Dyrk1B(Mirk kianse) andDyrk1A with IC50 of 6848 nM and 228 nM respectively. IC50value: 6848/228 nM (Dyrk1B/Dyrk1A) [1] Target: Dyrkinhibitor Mirk-IN-1 had an EC50 of 1.9 0.2 mmol/L on SW620cells. At a much higher concentration of 10 mmol/L in a kinase

Bioactivity: Protein kinase inhibitors 1 is a novel inhibitor of withHIPK2an of 74 nM and of 9.5 nM.IC50 Kd

Bioactivity: Protein kinase inhibitors 1 hydrochloride is a potent HIPK2inhibitor, with s of 136 and 74 nM for HIPK1 and HIPK2,IC50and a of 9.5 nM for HIPK2.Kd

AZ191 Cat. No.: HY-12277

EHT 5372 Cat. No.: HY-111380

Harmine (Telepathine) Cat. No.: HY-N0737A

ID-8 Cat. No.: HY-15838

Mirk-IN-1 (Dyrk1B/A-IN-1) Cat. No.: HY-12838

Protein kinase inhibitors 1 Cat. No.: HY-U00439

Protein kinase inhibitors 1 hydrochlorideCat. No.: HY-U00439A
https://www.MedChemExpress.com/Targets/DYRK.htmlhttps://www.MedChemExpress.com/AZ191.htmlhttps://www.MedChemExpress.com/EHT_5372.htmlhttps://www.MedChemExpress.com/Harmine.htmlhttps://www.MedChemExpress.com/ID-8.htmlhttps://ww

protein tyrosine kinase/rtk 1 inhibitors, agonists, screening libraries protein tyrosine kinase/rtk...

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