defactinib-pf-04554878

Description: Defactinib (formerly known as VS-6063, PF-04554878) is a selective, ATP-competitive and orally bioactive small molecule inhibitor of the FAK (focal adhesion kinase) with potential antitumor activity. It inhibits the phosphorylation of FAK at the Tyr397 site in a time- and dose-dependent manner. FAK is a nonreceptor tyrosine kinase that plays a vital role in many oncogenic pathways. Increased FAK expression has been reported in a number of tumor types, including breast, colon, and ovarian cancers. Therefore, as an inhibitor of FAK, defactinib has potential antineoplastic activities.

References: J Natl Cancer Inst. 2013 Oct 2; 105(19):1485-95; Oncotarget. 2014 Sep 15; 5(17):7945-59.

Related CAS: 1073154-85-4 (free base); 1345713-71-4 (free base); 1073160-26-5 (HCl)

Chemical Name: N-methyl-4-((4-(((3-(N-methylmethylsulfonamido)pyrazin-2-yl)methyl)amino)-5-(trifluoromethyl)pyrimidin-2-yl)amino)benzamide

SMILES Code: O=C(NC)C1=CC=C(NC2=NC=C(C(F)(F)F)C(NCC3=NC=CN=C3N(C)S(=O)(C)=O)=N2)C=C1