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。

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.

在负荷突变体B-Raf表达的A375P黑色素瘤移植的小鼠体内,SB590885可使肿瘤发生率明显降低,且对肿瘤生长有一定抑制作用.

在表达致癌B-RafV600E的Colo205,HT29,A375P,SKMEL28,和MALME-3M细胞中,SB590885可有效抑制ERK磷酸化（EC50：28/58/290/58/190 nM）,并抑制增殖（EC50：0.1/0.87/0.37/0.12/0.15 μM）。相比于c-Raf（Ki：1.72 nM）,SB590885对B-Raf的选择性明显更高（Ki：0.16 nM）。与多激酶抑制剂BAY43-9006不同,SB590885稳定致癌B-Raf激酶域的活性结构。且对B-Raf亲和力很高（Kd：0.3 nM）。大多数具有BRAF V600E突变体而无CDK4突变体(451Lu,WM983和WM35)的黑色素瘤细胞系对SB590885十分敏感（IC50<1 μM）。

Cells are treated with increasing concentrations of SB590885 and incubated for 72 hours. Viable cells are quantified using CellTiter-Glo reagent and luminescence detection on a Victor 2V plate reader. Cells are prepared for cell cycle analysis on a Becton Dickinson FACScan. Data is acquired and analyzed using CellQuest v3.3 software.(Only for Reference)

405554-55-4

C27H27N5O2

453.546

DMSO:25 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years