BAY 87-2243 是一种选择性的低氧诱导因子-1 抑制剂。

BAY 87-2243 is a potent and selective inhibitor of hypoxia-inducible factor-1 (HIF-1).

BAY87-2243（4 mg/kg口服）减少H460异种移植小鼠模型中肿瘤重量,HIF-1α蛋白和HIF-1靶基因表达水平.

在缺氧肺癌H460细胞中,BAY 87-2243抑制HIF靶基因表达,并抑制HIF-1α蛋白质积累。BAY 87-2243在葡萄糖消耗下,通过干扰线粒体功能抑制细胞增殖。BAY87-2243抑制HIF-1的报告基因活性和CA9蛋白表达,IC50分别为0.7 nM 和2 nM。

To evaluate the cytotoxicity of BAY 87-2243, 2.000 cells of the respective cell lines are seeded in 96-well plates and cultured in the appropriate growth medium containing 10% FCS. BAY 87-2243 at various concentrations is added at 24 h after seeding for additional 48 h and cell viability is determined using Cell Titer Glow Assay.(Only for Reference)

1227158-85-1

C26H26F3N7O2

525.536

DMSO:62.8 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years