PF-00562271

PF-00562271 is an orally bioavailable, potent, ATP‐competitive and reversible small molecule inhibitor of focal adhesion kinase (FAK; also known as protein tyrosine kinase 2). It exhibits high selectivity for FAK with an IC50 of 1.5 nM in cell-free assays and is approximately tenfold less potent against proline-rich tyrosine kinase 2 (Pyk2), with over a hundredfold selectivity versus other kinases except some cyclin-dependent kinases. The drug was developed primarily for its antineoplastic and antiangiogenic activities by targeting FAK signaling pathways involved in tumor cell invasion, proliferation, survival, and angiogenesis. Clinical studies have shown that it displays nonlinear pharmacokinetics and acts as a potent CYP3A inhibitor. The maximum tolerated dose identified in phase I trials was 125 mg twice daily with food[1][2][6][8].

Other names

N-methyl-N-[3-[[[2-[(2-oxo-1,3-dihydroindol-5-yl)amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]methyl]-2-pyridinyl]methanesulfonamidePF562271 besylatePF-562271 besylatePF 562271 besylate