SB590885

Description: SB590885 (SB 590885; SB-590885) is a novel and potent B-Raf inhibitor with potential antineoplastic activity. It inhibits B-Raf with a Ki of 0.16 nM in a cell-free assay, and exhibits a 11-fold higher selectivity for B-Raf over c-Raf. It does not inhibit other closely related kinases. It is found that SB590885 binds to B-Raf within the ATP-binding pocket and stabilizes the active conformation of B-Raf. SB590885 decreases the phosphorylation of ERK and shows anti-proliferation only in tumor cells expressing oncogenic B-Raf V600E. Malignant cells expressing oncogenic B-Raf show selective inhibition of mitogen-activated protein kinase activation, proliferation, transformation, and tumorigenicity when exposed to SB-590885 , whereas other cancer cell lines and normal cells display variable sensitivities or resistance to similar treatment.

References: Cancer Res. 2006 Dec 1; 66(23):11100-5; Bioorg Med Chem Lett. 2006 Jan 15; 16(2):378-81.