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PD153035 hydrochlorideCat. No.: A8199

CAS No.: 153436-54-5

Formula: C16H14BrN3O2·HCl

M.Wt: 396.67

Synonyms: ZM252868,PD153035 HCL

Target: JAK/STAT Signaling

Pathway: EGFR

Storage: Store at RT

In Vitro

3.97mg/mL in DMSO with gentle warming,insoluble in EtOH,insoluble in H2O

Preparing

Stock Solutions

Mass

1mg 5mg 10mgSolvent

Concentration

1 mM 2.5210 mL 12.6049 mL 25.2099 mL

5 mM 0.5042 mL 2.5210 mL 5.0420 mL

10 mM 0.2521 mL 1.2605 mL 2.5210 mL

Please refer to the solubility information to select the appropriate solvent.

Shortsummary Potent EGFR inhibitor

IC₅₀ & Target 5.2 pM (Ki) (EGFR), 29 pM (EGFR)

In Vitro

Cell Viability Assay

Cell Line: A panel of cancer cell lines overexpressing various levels of EGF receptor and

HER2/neu.

Preparation method The solubility of this compound in DMSO is limited. General tips for obtaining a

higher concentration: Please warm the tube at 37°C for 10 minutes and/or

shake it in the ultrasonic bath for a while. Stock solution can be stored below

-20°C for several months.

Reacting conditions: 0.5-2800 nM; 2 h

Product Name: PD153035 hydrochlorideRevision Date: 01/10/2020

Product Data Sheet

Solvent & Solubility

Biological Activity

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PD153035 hydroooooooooooocccccccccccchhhhhhhhhhhlorideCat. No.: A81999999999999999999999

CAS No.: 151555155551515151511515515153434343433434343434343636363633636363636366366------5455555555555 -5

Formula: CCC1C1C1C1CCC1C1C1C1CCC16H14BrN3O2·HCl

M.Wt: 396.67

Synonyms: ZM252868,PD153035 HCL

Target: JAK/STAT Signaling

Pathway: EGFR

Storage: Store at RT

In Vitro

3.97mg/mL in DMSO with gentle warming,insoluble in EtOH,insooolulululululululululuulululuull blblblblblblblbblbblblbbb e e e e eeeee eeeeee iininnniniinnnnininnii HHHHHHHH2O

Preparing

Stock Solutions

Mass

1mg 5mg 10mgSolvent

Concentration

1 mM 2.5210 mL 12.6049 mL 25.2099 mL

5 mM 0.5042 mL 2.5210 mL 5.0420 mL

10 mM 0.2521 mL 1.26666666666050505050505055050505050 mmmmmmmmmmmLLLLLLLLLL 2.5210 mL

Pleaaaaaaaaasesesseseseseseseeeseeeeese rrrrrrrrrrefefefefefefefeffeeeeefeefe erererererererererer ttttttttttto oooooooooo ttthttt e solubility information to select the appropriate solventntnttntnttntntt.

Shortsummary Potent EGFR inhibitor

IC₅₀ & Target 5.2 pM (Ki) (EGFR), 29 pM (EGFR)

In Vitro

Cell Viability Assay

Cell Line:e:e:e:e:e:e:eee A panel of cancer cell lines overexpressinggggggggg vavavavavavavavavavavavv riririririririririiououououuuuuououuouuuoououuuusssss s ssss s ss ssss ss leleleleleleleleleleleleeeevev ls of EGF receptor and

HER2/neu.

PrPrPrPrPrPrPrPrPrPrepepepepepepepepepepepepepaaaaaraaaaaa ation method The solubility of this compound in DDDDDDDDDDDDDDMSMSMSMSMSMSMSMSMSMSMSMSMSMSSM OOOOO OOOOOOOO is limited. General tips for obtaining a

higher concentration: Please warm the tube at 37°C for 10 minutes and/or

shake it in the ultrasonic bath for a while. Stock solution can be stored below

-20°C for several months.

Reacting conditions: 0.5-2800 nM; 2 h

Product Name: PD153035 hydrochlorideyRevision Date: 01/10/ 02020

etProduct Data Shee

Solvent & Soluuuuuubbbbbbiiiiiillllllllliiiittttttttyyyyyyyyyy

Biologicaaaallllll AAAAAAActivity

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Applications: In EGF receptor-overexpressing cell lines, PD153035 caused a

dose-dependent decrease in ligand-inducedEGF receptor phosphorylation.

PD153035 only inhibited HER2/neu phosphorylation at the highest

concentrations tested (1400-2800 nM). PD153035 also inhibited cell

proliferation in EGF receptor-positive cell lines.

In Vivo

Animal experiment

Animal models: Immunodeficient nude mice xenografted with A431 human epidermoid tumors

Dosage form: i.p. dose of 80 mg/kg

Applications: In immunodeficient nude mice xenografted with A431 human epidermoid

tumors, PD153035 rapidly suppressed the tyrosine phosphorylation of the EGF

receptor by 80-90% in the tumors. Following a single i.p. dose of 80 mg/kg, the

drug levels in the plasma and tumor rose to 50 and 22 μM within 15 minutes.

Other notes: Please test the solubility of all compounds indoor, and the actual solubility may

slightly differ with the theoretical value. This is caused by an experimental

system error and it is normal.

1. Duggan BM, Foley KP, et al."Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and

dysglycemia." Sci Rep. 2017 May 8;7(1):1578.PMID:28484277

See more customer validations on www.apexbt.com.

[1] Bos M, Mendelsohn J, Kim YM, Albanell J, Fry DW, Baselga J. PD153035, a tyrosine kinase inhibitor, prevents epidermal growth

factor receptor activation and inhibits growth of cancer cells in a receptor number-dependent manner. Clin Cancer Res. 1997

Nov;3(11):2099-106.

[2]. Kunkel MW1, Hook KE, Howard CT, et al. Inhibition of the epidermal growth factor receptor tyrosine kinase by PD153035 in

human A431 tumors in athymic nude mice. Invest New Drugs. 1996;13(4):295-302.

FOR RESEARCH PURPOSES ONLY.NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.Specific storage and handling information for each product is indicated on the product datasheet. Most APExBIO products are stable

under the recommended conditions. Products are sometimes shipped at a temperature that differs from the recommended storage

temperature. Shortterm storage of many products are stable in the short-term at temperatures that differ from that required for

long-term storage. We ensure that the product is shipped under conditions that will maintain the quality of the reagents. Upon receipt

of the product, follow the storage recommendations on the product data sheet.

Product Citations

References

Caution

2 | www.apeexbt.ccccccoomomomomommoooooooooomoommoo

Applications: In EGF receptor-overexpressing cell lines, PD153035 caused a

dose-dependent decrease in ligand-inducedEGF receptor phosphorylation.

PD153035 only inhibited HER2/neu phosphorylation at the highest

concentrations tested (1400-2800 nM). PD153035 also inhibited cell

proliferation in EGF receptor-positive cell lines.

In Vivo

Animal exxxxxxxxpepepepepepepepepepeperiririririririririririmememememememememememem ntntntntntntntntntntntntntttn

Animmmmmmmmmmmalalalalalalalalalall mmmmmmmmmmodododododdododddodododododododdodoododdelelelelelelelelelelelee sss:sssss Immunodeficient nude mice xenografted wiwiwiwiwiwiwiwiwiwiwithththththththththththth AAAAAAAAAAA43434343433333433434343333331111111111111111111 huhuhuhhuhuhhhuhuhhuhh man epidermoid tumors

DoDoDooDooDoooDDDDDDDDDDDD sasasasasasasasasasaagegegegegegeggegegegg form: i.p. dose of 80 mg/kg

AAAAAAApAAAAA plications: In immunodeficient nude mice xennnnnnnnnnnnnogogogogogogogogogoggrafted with A431 human epidermoid

tumors, PD153035 rapidly suppressed the tyrosine phosphorylation of the EGF

receptor by 80-90% in the tumors. Following a single i.p. dose of 80 mg/kg, the

drug levels in the plasma and tumor rose to 50 and 22 μM within 15 minutes.

Other notes: Please test the solubility of all compounds indoor, and the actual solubility may

slightly differ with the theoretical value. This is caused by an experimental

system error and it is normal.

1. Duggan BM, Foley KP, et al."Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and

dysglycemia." Sci Rep. 2017 May 8;7(1):1578.PMID:28484277

See more customer validations on www.apexbt.com.

[1] Bos M, Mendelsohn J, Kim YM,M,MM,M,M,M,M,MM,MM, AAAAAAAAAAAAlblblblblblblblblbananananananananananneleeeeeee l J, Fry DW, Baselga J. PD153035, a tyrosine kinase inhiiiibibbbbbbbbb tooooooooooooooooooor,rrrr,rrr,r pppppppppprerererererererererer veveveveveveveveveevevents epidermal growth

factor receptor activation aaaaaaaaandndndndndndndndndddndddddndd iiiiinhnhnhnhnhnhnhhnhnhnnnnnnnnn ibibibibibibibibibbbbititititititititititittsssssssss growth of cancer cells in a receptor number-dependddenenenenenenenenenene t ttttttttt mamamamamamamamamamamannnnnnnnnnnnnnnnnnnnnnnnnnnnnereeeeeeeeeee . Clin Cancer Res. 1997

Nov;3(11):2099-106.

[2]. Kunkel MW1,1,1,,1,1,,1,1,,11 HHHHHHHHHHHHHHHHooooooooooooooooooooooooooooooooo k kk k k k k k kk KEKKEKEKEKEKEKEKEKEKEKKK , Howard CT, et al. Inhibition of the epidermal growth factooooooooorrrrrrrrrrrrr rerererererererererererererer cecececececcecececccccc ptor tyrosine kinase by PD153035 in

human A431 tumororrrrrrrrrrsssssssssss ss iiiiniiiiiii athymic nude mice. Invest New Drugs. 1996;13(4):295-302.

FOR RESEARCH PURPOSES ONLY.NOT FOR HUMAN, VETERINARRRRRRRRRRY Y Y YY YYYYYYY DIDIDIDIDIDIDIDDIDIDIAGAGAGAGAGAGAGAGAGAGAGAGAGNOSTIC OR THERAPEUTTIC USE.Specific storage and handlininnininnininng g gg g g gg g gggg ininininininnininininnnni fofofofofofofofofofofofoffffff rmrmrmrmrmrmrmrmrmrmmatatatatatatatatatatatata ioioiiiiiii n for each product is indicatted on the product datasheeeeeeeeeeeteteteteteteteteteet. MoMoMoMoMoMoMoMoMoMMMoMoststststststststststsstsss AAAAAAAAAAAPExBEE IO ble products are stab

under the recommendedededededededeededdeded d d d dd d dd dd cococococococococooc ndndndndndndndnddnddnditittitititititititittitittioiioioioioioioioioi ns. Products are sometimes shipped at a temperature from the recommended storageed at a temperature ththththththththththththhhatatatatatatatatattatatatatatattt ddddddddddddddddddifififiififiififififfiffiffefefefefefefefefefefefeeefefeerrsrrsrsrrsrrrrrrr from the recommended storag

temperature. Shoooooooooooortrtrtrtrtrtrtrtrtrtrtrrtrrtrrttetetetetetetetteteteteeeeermrrmrmrmrmmmrmmrmrmmmrmrmrmrmmr sssssssssstototototototototototoottt rage of many products are stable in the sshort-term at temperattttturururururuururururuu eeeees that differ from that required for

long-term storagee. WeWeWeWeWeWeWeWeWeWeWeWeWeWWWeWe ensure that the product is shipped under conditions that will maintain the quality of the reagents. Upon receipt e

of the product, follow the storage recommendations on the product ddata sheet.

Product CCCCCCiiiiiittttttttaaaaattttttiiiiiioooooons

References

Caution

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APExBIO Technologywww.apexbt.com

7505 Fannin street, Suite 410, Houston, TX 77054. Tel: +1-832-696-8203 | Fax: +1-832-641-3177 | Email: info@apexbt.com

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APExBIO Technologywww.apexbt.com

7505 Fannin street, Suite 410, Houston, TX 77054.TeTeTeTeTeTeTeTeTeTeeTeTeTeTeT l:ll:l:l:l::l:l::l:l:l:: +1-832-696-8203 | Fax: +1-832-641-3177 | Email: info@a@a@a@a@a@aa@aaa@a@a@a@a@@ pepepepepepepepepepepepexbxbxbxbxbxbxbxbxbxbbt.t.t.t.t.t.t.t.t.t.t..cocococococococococococococommmmmmmmmm