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CAS No. : 1883545-51-4
MCE 国际站:AZD5582 dihydrochloride
产品活性:AZD5582 dihydrochloride 是 IAP 拮抗剂,可以有效与 cIAP1,cIAP2 和 XIAP 的 BIR3 结构域结合, IC50 值分别为 15,21,15 nM。AZD5582 诱导凋亡 (apoptosis)。
研究领域:Apoptosis
作用靶点:IAP | Apoptosis
In Vitro: AZD5582 (20 nM; 48 hours) inhibits cell viability by cooperation with IFNγ or viral double-stranded RNA (dsRNA) in H1975 NSCLC cells.AZD5582 (20 nM; 17 or 25 hours) downregulates 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.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.
In Vivo: 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.
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