文献

Background Information:

AZD5582 is a cell permeable, novel class of dimeric SMAC mimetic designed to mimick the AVPI motif of SMAC. It is a potent and selective inhibitor of X-linked (XIAP) and cellular (cIAP) inhibitor of apoptosis protein with IC50 values of 15, 15 and 21 nM for XIAP, cIAP1 and cIAP2, respectively. At nanomolar concentrations AZD5582 causes extensive degradation of cIAP-1 and cIAP-2, and induces apoptosis in MDA-MB-231 breast cancer cells. It causes substantial tumor regressions following two weekly doses of 3.0 mg/kg in MDA-MB-231 xenograft-bearing mice.

Reference:

1.E.J. Hennessy, 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, 56 (24), pp 9897–9919.

APIM050294: AZD5582

CAS No.: 1258392-53-8.
Molecular Formula: C58H78N8O8 ? 2HCl ? 2.5H2O.
Molecular Weight: 1133.3.
Purity: ≥99% purity (HPLC).
QC: HPLC-MS, 1HNMR, and Quantitative Elemental Analysis.
Solubility: Soluble in DMSO, Water.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.