PF-562271

Description: PF-562271 is a novel, potent, ATP-competitive, orally bioavailable, reversible inhibitor of FAK (focal adhesion kinase) and Pyk2 catalytic activity with a IC50 of 1.5 and 14 nmol/L, respectively. it has > 100-fold selectivity against other protein kinases. Additionally, PF-562, 271 displayed robust inhibition in an inducible cell-based assay measuring phospho-FAK with an IC(50) of 5 nmol/L. PF-562, 271 was evaluated against multiple kinases and displays > 100x selectivity against a long list of nontarget kinases. PF-562, 271 inhibits FAK phosphorylation in vivo in a dose-dependent fashion (calculated EC(50) of 93 ng/mL, total) after p.o. administration to tumor-bearing mice. In vivo inhibition of FAK phosphorylation (> 50%) was sustained for > 4 hours with a single p.o. dose of 33 mg/kg. Antitumor efficacy and regressions were observed in multiple human s.c. xenograft models. PF-562271 is a potential therapeutic agent either alone or in combination with other agents for the treatment of cancer.

References: Cancer Res. 2008 Mar 15; 68(6):1935-44; Cancer Biol Ther. 2010 Jul 1; 10(1):38-43.

Related CAS #: 939791-39-6 (mesylate); 939791-41-0 (HCl); 939791-40-9 (tosylate); 939791-38-5 (besylate); 717907-75-0 (free base);

Chemical Name: N-methyl-N-(3-(((2-((2-oxoindolin-5-yl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)methyl)pyridin-2-yl)methanesulfonamide

SMILES Code: CS(=O)(N(C)C1=NC=CC=C1CNC2=NC(NC3=CC4=C(NC(C4)=O)C=C3)=NC=C2C(F)(F)F)=O