AZ 628

AZ 628 is a pan-Raf kinase inhibitor with IC₅₀s of 105, 34 and 29 nM for B-Raf, B-RafV600E, and c-Raf-1, respectively. IC50 & Target: IC50: 105 nM (B-Raf), 34 nM (B-RafV600E), 29 nM (c-Raf-1)^[1] In Vitro: AZ 628 reduces activities of preactivated B-Raf, B-RafV600E, and c-Raf-1 in in vitro kinase assays, with IC₅₀ values of 105, 34 and 29 nM, respectively. AZ 628 also inhibits activation of number of tyrosine protein kinases including VEGFR2, DDR2, Lyn, Flt1, FMS and others. AZ 628 inhibits anchorage-dependent and -independent growth, causes cell cycle arrest, and induces apoptosis in colon and melanoma cell lines harboring B-RafV600E mutation^[1]. AZ 628 suppresses growth in cells expressing K-RAS^G13D. Inhibition of RAF with AZ 628 suppresses MEK and ERK phosphorylation. AZ 628 selectively affects viability in K-RAS mutant cells^[2].