AZD 5582 dihydrochloride 是凋亡蛋白抑制剂 (IAPs) 的拮抗剂，可与 BIR3 结构域 cIAP1、cIAP2 和 XIAP 结合，IC50 分别为 15、21 和 15 nM。 AZD5582 诱导细胞凋亡。
货号:ajcx26940
CAS:1883545-51-4
分子式:C58H78N8O8.2HCl
分子量：1088.21
溶解度:Soluble in DMSO
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Dimeric Smac mimetic; potent inhibitor of X-linked (XIAP) and cellular (cIAP) inhibitor of apoptosis protein (IC50 values are 15, 15 and 21 nM for XIAP, cIAP1 and cIAP2 respectively). Binds to the BIR3 domain of XIAP to prevent interaction with caspase-9. Causes degradation of cIAP1 and cIAP2 and induces apoptosis in MDA-MB-231 breast cancer cells. Causes tumor regression in MDA-MB-231 xenograft-bearing mice.

Hennessy et al (2013) Discovery of a novel class of dimeric Smac mimetics as potent IAP antagonists resulting in a clinical candidate for the treatment of cancer (AZD5582). J.Med.Chem. 56 9897 PMID:24320998