pf-573228

Description: PF-573228 (PF573228) is a selective and ATP-competitive FAK (focal adhesion kinase) inhibitor with potential antitumor activity. It inhibits FAK with an IC50 of 4 nM in a cell-free assay, and is ca.50- to 250-fold more selective for FAK over other kinases including Pyk2, CDK1/7 and GSK-3beta. PF-573228 shows high in vivo antitumor efficacy in PC3M-luc-C6 xenograft models. FAK is a non-receptor protein-tyrosine kinase that regulates integrin and growth factor signaling pathways involved in cell migration, proliferation, and survival. FAK is over expressed in many cancers, including breast and prostate cancer.

References: J Biol Chem. 2007 May 18; 282(20):14845-52.

PF573, 228; PF 573, 228; PF-573, 228; PF573228; PF 573228; PF-573228;

Chemical Name: 3, 4-Dihydro-6-[[4-[[[3-(methylsulfonyl)phenyl]methyl]amino]-5-(trifluoromethyl)-2-pyrimidinyl]amino]-2(1H)-quinolinone