AZD5582 是一种IAP拮抗剂，可诱导凋亡，可与 cIAP1、cIAP2 和 XIAP 的 BIR3 结构域结合，IC50值分别为 15、21和15 nM。

AZD5582 is an inhibitor of IAPs, which binds to the BIR3 domains cIAP1, cIAP2, and XIAP with IC50s of 15, 21, and 15 nM, respectively. It induces apoptosis.

AZD5582 (20 nM; 48 hours) inhibited cell viability by cooperation with IFNγ or viral double-stranded RNA (dsRNA) in H1975 NSCLC cells[2]. AZD5582 (20 nM; 48 hours) involves in apoptosis due to induction of cell death and active caspase-3/ -8 activities by AZD5582 and IFNγ co-treatment in HCC827 NSCLC cells[2]. AZD5582 (20 nM; 17 or 25 hours) down-regulates cIAP-1, activates RIPK1( upstream regulator of caspase-8), and triggers the activation of extrinsic (caspase-8) and intrinsic (caspase-9) apoptosis pathways, causing the cleavage of caspase-3 and caspase-7[2].

AZD5582 (intravenous injection; 0.1-3.0 mg/kg; once a week; 2 weeks) causes degradation of cIAP1 and caspase 3 cleavage in tumor cells, and after a two-week treatment, the tumors largely resolved. When the mice are given a medium dose (0.5 mg/kg) of AZD5582, cIAP1 degrades after administration, but it takes a while time to reach apoptosis-inducing effect[1].

1258392-53-8

C58H78N8O8

1015.29

DMSO:66.25 mg/mL (65.25 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years