Birinapant
产品介绍
Birinapant (TL32711, TL-32711),又称比瑞那帕,是线粒体促凋亡蛋白SMAC的肽模拟物,是XIAP/cIAP1的拮抗剂,Kd值为45 nM和<1 nM,能促进结合TRAF2的cIAP1和cIAP2的蛋白酶体降解,具有潜在抗癌活性。凋亡抑制蛋白因子(IAP)在各种恶性肿瘤中经常过表达,被认为是癌症治疗的适当靶标。
产品性质
产品特色
参考文献
- Infante JR, et al. Phase I dose-escalation study of LCL161, an oral inhibitor of apoptosis proteins inhibitor, in patients with advanced solid tumors. J Clin Oncol. 2014 Oct 1;32(28):3103-10.
- Chen KF, et al. Inhibition of Bcl-2 improves effect of LCL161, a SMAC mimetic, in hepatocellular carcinoma cells. Biochem Pharmacol. 2012 Aug 1;84(3):268-77.
- Dhuria S, et al. Time-dependent inhibition and induction of human cytochrome P4503A4/5 by an oral IAP antagonist, LCL161, in vitro and in vivo in healthy subjects. J Clin Pharmacol. 2013 Jun;53(6):642-53.
存储条件
冰袋运输。粉末直接保存于-20℃,有效期3年。建议分装后-20℃干燥保存,避免反复冻融。
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