AZD 5582 dihydrochloride

Cat. No. 5141

AZD 5582 dihydrochloride C58H78N8O8.2HCl

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Chemical Name: 3,3'-[2,4-Hexadiyne-1,6-diylbis[oxy[(1S,2R)-2,3-dihydro-1H-indene-2,1-diyl]]]bis[N-methyl-L-alanyl-(2S)-2-cyclohexylglycyl-L-prolinamide

Biological Activity

Dimeric Smac mimetic; potent inhibitor of X-linked (XIAP) and cellular (cIAP) inhibitor of apoptosis protein (IC50 values are 15, 15 and 21 nM for XIAP, cIAP1 and cIAP2 respectively). Binds to the BIR3 domain of XIAP to prevent interaction with caspase-9. Causes degradation of cIAP1 and cIAP2 and induces apoptosis in MDA-MB-231 breast cancer cells. Causes tumor regression in MDA-MB-231 xenograft-bearing mice.

Licensing Information

Sold with the permission of AstraZeneca UK Ltd

Technical Data

Soluble to 100 mM in water and to 100 mM in DMSO
>97 %
Store at -20°C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch
Safety Data Sheet: View Safety Data Sheet

Hennessy et al (2013) 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. 56 9897. PMID: 24320998.

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Keywords: AZD 5582 dihydrochloride, supplier, AZD5582, dihydrochloride, dimeric, smac, inhibitors, potent, x-linked, cellular, cIAP1, cIAP2, XIAP, IAP, inhibits, apoptosis, protein, anticancer, BIR3, domain, 1258392-53-8, Tocris Bioscience, Inhibitor of Apoptosis Inhibitor products

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