Potent ATP-competitive reversible inhibitor of FAK and Pyk2. 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 non target 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.
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