B-Raf inhibitor,potent and selective
CAS：1191385-19-9
分子式：C26H21Cl3N8
分子量：551.86
纯度：98%
存储：Store at -20°C

Background:

B-Raf inhibitor 1 is an inhibitor of B-Raf kinase with IC50 values of 0.31μM and 0.72μM for cell proliferation, respectively in A375 and HCT116 [1].

B-Raf is important in signal transduction and some mutant B-Raf occurs in cancer cells. The most common mutation of these is V600E, which makes B-Raf kinase constitutively active. B-Raf inhibitor 1 belongs to the type IIA inhibitors and binds to the DFG-out ATP-binding site of B-Raf. The selectivity of B-Raf inhibitor 1 is less than of other type inhibitors. Besides mutant B-Raf, it can also inhibit wild type B-Raf and other tyrosine kinase. In cells with wild type B-Raf, B-Raf inhibitor 1 can activate the RAF-MEK-ERK signaling pathway via Raf dimerization. The preclinical toxicity test shows B-Raf inhibitor 1 can induce hyperplasia in a mouse model [1, 2].

参考文献:
[1] Wang X,?Kim J. Conformation-specific effects of Raf kinase inhibitors. J Med Chem.?2012 Sep 13;55(17):7332-41.
[2] Smith AL,?DeMorin FF,?Paras NA,?Huang Q,?Petkus JK,?Doherty EM,?Nixey T,?Kim JL,?Whittington DA,?Epstein LF,?Lee MR,?Rose MJ,?Babij C,?Fernando M,?Hess K,?Le Q,?Beltran P,?Carnahan J. Selective?inhibitors?of the?mutant?B-Raf?pathway:?discovery?of a potent?and?orally?bioavailable?aminoisoquinoline. J Med Chem.?2009 Oct 22;52(20):6189-92.