b-raf in 11

B-Raf IN 11 是一种新型选择性抑制剂。 B-Raf 激酶V600E 突变体的DFG-in 构象优于结肠直肠癌中的DFG-out 构象。

SB590885 是一种 B-Raf 抑制剂，Ki 值为 0.16 nM，对其选择性是对 c-Raf 的 11 倍多。

Sorafenib N-oxide is an active metabolite of sorafenib , an inhibitor of Raf-1, B-RAF, and receptor tyrosine kinases. Sorafenib N-oxide inhibits FLT3 that contains the internal tandem duplication mutation (FLT3-ITD; Kd = 70 nM) and inhibits proliferation of MV4-11 acute myeloid leukemia (AML) cells expressing FLT3-ITD (IC50 = 25.8 nM). It is selective for AML cell lines containing FLT3-ITD over lines containing wild-type FLT3 (IC50s = 3.9-13.3 μM). Sorafenib N-oxide is also a linear-mixed inhibitor of the cytochrome P450 (CYP) isoform CYP3A4 (Ki = 15 μM in human liver microsomes).