A potent inhibitor of focal adhesion kinase (FAK) and Pyk2.
生化機理
PF-562271 displays selective inhibitory effects on FAK (IC50 of 1.5 nM) and Pyk2(IC50 of 14 nM) tyrosine kinase activity. In cell-based assays, PF-562271 is shown to be more selective for FAK compared to other kinase targets (IC50 of 5 nM). PF-562271 results in a dose-dependent cell proliferation inhibition in FAK WT (IC50 of 3.3 μM), FAK?/? (IC50 of 2.08 μM) and FAK kinase-deficient (KD) cells (IC50 of 2.01 μM), in 2 dimensional (2D) cultures.