tcsc0693 ZM 336372

ZM 336372 is a potent inhibitor of the protein kinase c-Raf. The IC₅₀ value is 0.07 μM in the standard assay, which contains 0.1 mM ATP.

In Vitro: ZM 336372 is a potent inhibitor of human c-Raf. The IC₅₀ value is 0.07 μM in the standard assay, which contains 0.1 mM ATP. The IC₅₀, decreases to 0.01μM at 0.025 mM ATP and increases to 0.9 μM at 2.5 mM ATP indicating that ZM 336372 is a competitive inhibitor with respect to ATP. ZM 336372 inhibits c-Raf tenfold more potently than B-Raf^[1]. Cell proliferation analysis of ZM336372. 3,4-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide growth assay of H727 and BON treated as control, DMSO, and 100 μM ZM336372 to days 16 and 10, respectively. Both H727 and BON cell proliferation is inhibited in the presence of drug compared with controls. H727 cells treated with ZM336372 are growth suppressed, whereas control treatments have significantly more growth by day 6, continuing up to 16 days. A similar response is also seen in BON cells as growth suppression occurred as early as day 4 and was maintained out to day 10^[2].