1883545-51-4

AZD5582 dihydrochloride is an antagonist of the inhibitor of apoptosis proteins (IAPs), which binds to the BIR3 domains cIAP1, cIAP2, and XIAP with IC50s of 15, 21, and 15 nM, respectively. AZD5582 induces apoptosis[1].

cIAP1: 15 nM (IC₅₀); cIAP2: 21 nM (IC₅₀); XIAP: 15 nM (IC₅₀)

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[1] Hennessy EJ, et al. 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. 2013 Dec 27;56(24):9897-919. DOI:10.1021/jm401075x
[2] Qin Hao, et al. IF-γ and Smac mimetics synergize to induce apoptosis of lung cancer cells in a TNFα-independent manner,Cancer Cell Int. 2018; 18: 84. DOI:10.1186/s12935-018-0579-y