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