PF-562271

Soluble in DMSO or ethanol. PF-562,271 is a potent, ATP-competitive, reversible inhibitor of FAK and Pyk2 catalytic activity with a IC(50) of 1.5 and 14nM, respectively. In addition, PF-562,271 displayed robust inhibition in an inducible cell-based assay measuring phospho-FAK with an IC(50) of 5nM. PF-562,271 was evaluated against multiple kinases and displays >100x selectivity against a long list of nontarget kinases. In tests, PF-562,271 inhibits FAK phosphorylation in vivo in a dose-dependent fashion with a calculated EC50 of 93ng/mL using injections. Substrate: Tyrosine