PND-1186
  • 化学数据
CAS号 1061353-68-1 货号 BCP10711
中文名 PND-1186
英文名 PND-1186
中文别名
英文别名 PND1186;PND 1186; SR 2516; SR2516; SR2516; VS4718; VS4718; VS 4718;
分子式 C25H26F3N5O3 分子量 501.5
  • 用途
生物活性 PND-1186, also known as SR-2156 and VS-4718, is a potent FAK inhibitor with a 50% inhibitory concentration (IC50) of 1.5 nM in vitro. PND-1186 has an IC50 of ~100 nM in breast carcinoma cells. Notably, 1.0 µM PND-1186 (>5-fold above IC50) had limited effects on cell proliferation. However, under non-adherent conditions as spheroids and as colonies in soft agar, 0.1 µM PND-1186 blocked FAK and p130Cas tyrosine phosphorylation, promoted caspase-3 activation, and triggered cell apoptosis. PND-1186 inhibited 4T1 breast carcinoma subcutaneous tumor growth correlated with elevated tumor cell apoptosis and caspase 3 activation.
信号通路 Angiogenesis/Protein Tyrosine Kinase 
靶 点 FAK 

结构式

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