A Bcr-Abl inhibitor; inhibits wild-type and mutant forms of Bcr-Abl

PD 180970 – 5 mg

Brand:
Cayman
CAS:
287204-45-9
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

PD 180970 is an inhibitor of Bcr-Abl.{54237} It inhibits wild-type and mutant forms of Bcr-Abl, as well as the p210 isoform, a marker of chronic myelogenous leukemia (CML), with IC50 values ranging from 5 to 48 nM.{54237,54238} PD 180970 is selective for Bcr-Abl over basic FGFR (bFGFR) and PDGFR (IC50s = 934 and 1,430 nM, respectively) but also inhibits Src, LCK, KIT, and EGFR (IC50s = 0.8, 1 phase and apoptosis in K562 CML cells when used at a concentration of 50 nM.{54241} PD 180970 (500 nM) inhibits constitutive STAT3 DNA-binding activity in, and proliferation of, MDA-MB-468 breast cancer cells.{54242} It also inhibits proliferation of Ba/F3 cells expressing mutant p210 Bcr-AblY253F that are resistant to imatinib (Item No. 13139) with an IC50 value of 48 nM.{54238}  

 

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SKU: 30619 - 5 mg Category:

Description

A Bcr-Abl inhibitor; inhibits wild-type and mutant forms of Bcr-Abl, as well as the p210 isoform (IC50s = 5-48 nM); selective for Bcr-Abl over bFGFR and PDGFR (IC50s = 934 and 1,430 nM, respectively) but also inhibits Src, LCK, KIT, and EGFR (IC50s = 0.8, 1 phase and apoptosis in K562 cells at 50 nM; inhibits constitutive STAT3 DNA-binding activity in and proliferation of MDA-MB-468 breast cancer cells; inhibits proliferation of imatinib-resistant mutant p210 Bcr-AblY253F Ba/F3 cells

Formal name: 6-(2,6-dichlorophenyl)-2-[(4-fluoro-3-methylphenyl)amino]-8-methyl-pyrido[2,3-d]pyrimidin-7(8H)-one

Synonyms: 

Molecular weight: 429.3

CAS: 287204-45-9

Purity: ≥98%

Formulation: A solid

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