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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).
AZD5582 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. 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. For the detailed information of AZD 5582, the solubility of AZD 5582 in water, the solubility of AZD 5582 in DMSO, the solubility of AZD 5582 in PBS buffer, the animal experiment (test) of AZD 5582, the cell expriment (test) of AZD 5582, the in vivo, in vitro and clinical trial test of AZD 5582, the EC50, IC50,and affinity,of AZD 5582, For the detailed information of AZD 5582, the solubility of AZD 5582 in water, the solubility of AZD 5582 in DMSO, the solubility of AZD 5582 in PBS buffer, the animal experiment (test) of AZD 5582, the cell expriment (test) of AZD 5582, the in vivo, in vitro and clinical trial test of AZD 5582, the EC50, IC50,and affinity,of AZD 5582, Please contact DC Chemicals. |