AZD5582

A Smac mimetic and IAP inhibitor

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库存: 现货

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数量
2mg

￥550.00

440.00

- +
5mg

￥812.00

650.00

- +
10mg

￥1350.00

1080.00

- +
50mg

￥4050.00

3240.00

- +

已选 0 种 0 瓶

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货号: ajci22342
CAS: 1258392-53-8
别名:
分子式: C58H78N8O8
分子量: 1015.29
纯度: >98%
溶解度: DMSO : ≥ 66.25 mg/mL (65.25 mM)
储存: 4°C, protect from light, stored under nitrogen
库存: 现货

Background

AZD5582 is a novel class of dimeric Smac mimetics as potent IAP antagonist; binds potently to the BIR3 domains of cIAP1, cIAP2, and XIAP (IC50 = 15, 21, and 15 nM, respectively). IC50 value: 15/21/15 nM (cIAP1/cIAP2/XIAP) [1]Target: IAPs inhibitorAZD5582 causes cIAP1 degradation and induces apoptosis in the MDA-MB-231 breast cancer cell line at subnanomolar concentrations in vitro. When administered intravenously to MDA-MB-231 xenograft-bearing mice, AZD5582 results in cIAP1 degradation and caspase-3 cleavage within tumor cells and causes substantial tumor regressions following two weekly doses of 3.0 mg/kg. Antiproliferative effects are observed with AZD5582 in only a small subset of the over 200 cancer cell lines examined, consistent with other published IAP inhibitors [1]. AZD5582 significantly enhanced apoptosis induced by the death receptor (DR) agonist tumour necrosis factor-related apoptosis-inducing ligand (TRAIL). Importantly, killing by TRAIL plus AZD5582 was independent of adverse prognostic features including TP53 deletion which is strongly associated with chemoresistance in CLL [2].

参考文献:
[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.
[2]. Zhuang J, et al. Selective IAP inhibition results in sensitization of unstimulated but not CD40-stimulated chronic lymphocytic leukaemia cells to TRAIL-induced apoptosis. Pharmacol Res Perspect. 2014 Dec;2(6):e00081.