BFH772

Description: BFH772 (also known as BFH-772) is a novel and potent orally bioavailable VEGFR2 inhibitor that targets VEGFR2 kinase with IC50 of 3 nM. BFH772 was highly effective at targeting VEGFR2 kinase, however, lost 500-fold potency on FLK-1, FLT-1, and FLT-4. BFH772 also targeted B-RAF, RET, and TIE-2, albeit with at least 40-fold lower potency. BFH772 inhibited the ligand induced autophosphorylation of RET, PDGFR, and KIT kinases. BFH772 was selective against the kinases of EGFR, ERBB2, INS-R, and IGF-1R and against the cytoplasmic BCR-ABL kinase.

References: J Med Chem. 2016 Jan 14; 59(1):132-46.