AZD5582 |
Katalog-Nr.GC19050 |
AZD5582 ist ein Antagonist des Inhibitor of Apoptosis Proteins (IAPs), der an die BIR3-DomÄnen cIAP1, cIAP2 und XIAP mit IC50-Werten von 15, 21 bzw. 15 nM bindet. AZD5582 induziert Apoptose.
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Cas No.: 1258392-53-8
Sample solution is provided at 25 µL, 10mM.
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].
References:
[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.
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