Description
A tyrosine kinase inhibitor; inhibits c-Src, Yes, and LCK (IC50s = 25, 22, and 5 nM, respectively), as well as Bcr-Abl and c-Kit (IC50s = 1-2 and 25 nM, respectively), and is selective for these kinases over InsR, α-FGFR, bFGFR, PDGFR, and PKC; induces cell cycle arrest at the G2/M phase in DU145 prostate, SKOV3 ovarian, HT-29 colon, A549 lung, and A431 skin cancer cell at 5,000 nM; inhibits proliferation of MDA-MB-468 and MCF-7 breast cancer cells (IC50s = 500 and 1,000 nM, respectively), as well as patient-derived peripheral blood CML progenitor cells (IC50= ~7.5 nM)
Formal name: 6-(2,6-dichlorophenyl)-8-methyl-2-[[3-(methylthio)phenyl]amino]-pyrido[2,3-d]pyrimidin-7(8H)-one
Synonyms:
Molecular weight: 443.4
CAS: 260415-63-2
Purity: ≥98%
Formulation: A crystalline solid