Chemical Name : PHA-665752
CAS : 477575-56-7
Synonyms: (2R)-1-[[5-[(Z)-[5-[[(2,6-Dichlorophenyl)methyl]sulfonyl]-1,2-dihydro-2-oxo-3H-indol-3-ylidene]methyl]-2,4-dimethyl-1H-pyrrol-3-yl]carbonyl]-2-(1-pyrrolidinylmethyl)pyrrolidine;(3Z)-5-[[(2,6-DICHLOROPHENYL)METHYL]SULFONYL]-3-[[3,5-DIMETHYL-4-[[(2R)-2-(1-PYRROLIDINYLMETHYL)-1-PYRROLIDINYL]CARBONYL]-1H-PYRROL-2-YL]METHYLENE]-1,3-DIHYDRO-2H-INDOL-2-ONE HYDRATE
Solubility:Soluble to 100 mM in DMSO
Storage:Store at +4
Biologieal
Potent, selective and ATP-competitive inhibitor of MET kinase (IC50 values are 9, 68, 200, 1400, 3000, 3800 and 6000 nM for MET, Ron, Flk-1, c-abl, FGFR1, EGFR and c-src respectively and > 10000 nM for IGF-IR, PDGFR, AURORA2, PKA, PKB��, p38��, MK2 and MK3). Antitumor agent; inhibits tumorigenicity and angiogenesis in mouse lung cancer xenografts.
Reference
Christensen et al (2003) A selective small molecule inhibitor of c-Met kinase inhibits c-Met-dependent phenotypes in vitro and exhibits cytoreductive antitumour activity in vivo. Cancer Res. 63 7345. Smolen et al (2006) Amplification of MET may identify a subset of cancers with extreme sensitivity to the selective tyrosine kinase inhibitor PHA-665752. Proc.Natl.Acad.Sci.USA 103 2316. Puri et al (2007) A selective small molecule inhibitor of c-Met, PHA665752, inhibits tumorigenicity and angiogenesis in mouse lung cancer xenografts. Cancer Res. 67 3529.