B-Raf is a MAP kinase kinase kinase, which functions downstream of Ras family GTPases to activate MEK1/2 and ERK1/2 signaling. Mutations of B-Raf, particularly at Val600, are common in melanomas and melanocytic nevi. SB-590885 is a potent inhibitor of B-Raf (Kd = 0.3 nM). It less effectively inhibits c-Raf (Ki =...

Potent B-Raf inhibitor, selective for B-Raf against 46 other kinases. Decreases anchorage-independent growth of melanoma cell lines. Inhibits ERK phosphorylation and proliferation in tumor cells expressing B-Raf.

Soluble in DMSO or ethanol. SB-590885 is a novel, potent and selective small molecule inhibitor of B-Raf kinase, with a Ki of 0.16nM. It shows an 11-fold greater selectivity for B-Raf over c-Raf. It was used to address the dependence of MAPK signalling and tumor cell growth on B-Raf kinase activity. Target: ARaf -...

Description: SB590885 is an effective B-Raf inhibitor (Ki: 0.16 nM, in a cell-free assay). The selectivity of SB590885 for B-Raf is 11-fold greater over c-Raf, no acts to other human kinases. Target: Raf. Smiles: CN(C)CCOc1ccc(cc1)-c1nc(c([nH]1)-c1ccncc1)-c1ccc2\C(CCc2c1)=N\O. References: King AJ, et al. Cancer Res,...