tcsc0091 AZ 628

AZ628 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: AZ628 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. AZ628 also inhibits activation of number of tyrosine protein kinases including VEGFR2, DDR2, Lyn, Flt1, FMS and others. AZ628 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].