AZD5582
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CAS No. | 1258392-53-8 | Cat. No. | BCP20145 |
Name | AZD5582 | ||
Synonyms | AZD-5582;AZD 5582; | ||
SMILES | CN[C@@H](C)C(N[C@](C(N1[C@](C(N[C@]2C3=CC=CC=C3C[C@]2OCC#CC#CCO[C@]4[C@@H](NC([C@@H]5CCCN5C([C@@H](NC([C@](C)NC)=O)C6CCCCC6)=O)=O)C(C=CC=C7)=C7C4)=O)CCC1)=O)C8CCCCC8)=O | ||
Chemical Name | |||
Formula | C58H78N8O8 | M. Wt | 1015.29 |
Purity | 98% | Storage | Store at 4-8°C |
Description | AZD5582 is a potent IAP inhibitor, which is a dimeric compound based on the AVPI motif of Smac. AZD5582 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 14 in only a small subset of the over 200 cancer cell lines examined, consistent with other published IAP inhibitors. As a result of its in vitro and in vivo profile, AZD5582 was nominated as a candidate for clinical development. |
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