PHA-665752

PHA-665752 is a potent, selective, ATP-competitive c-Met inhibitor with Ki/IC50 of 4/9 nM, inhibits c-Met RTK autophosphorylation in A549 cells with IC50 of 45 nM; exhibits >50-fold selectivity for c-Met against a panel of kinases with exceptions of Ron and VEGFR2 (IC50=68 and 200 nM) ; inhibited HGF-stimulated or constitutive phosphorylation of mediators of downstream signal transduction of c-Met, including Gab-1, ERK, Akt, STAT3, PLCγ, and FAK in multiple tumor cell lines; inhibits c-Met phosphorylation and tumor growth in vivo.