AZD-5582
AZD-5582 Basic information
- Product Name:
- AZD-5582
- Synonyms:
-
- AZD-5582
- 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]
- AZD5582;AZD-5582;AZD 5582
- CS-2673
- (S,S,2S,2'S)-N,N'-((1S,1'S,2R,2'R)-(hexa-2,4-diyne-1,6-diylbis(oxy))bis(2,3-dihydro-1H-indene-2,1-diyl))bis(1-((S)-2-cyclohexyl-2-((S)-2-(methylamino)propanamido)acetyl)pyrrolidine-2-carboxamide)
- L-Prolinamide, 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-
- ZD5582
- (2S,2'S)-1,1'-((S,2S,2'S)-2,2'-(((1S,1'S,2R,2'R)-(Hexa-2,4-diyne-1,6-diylbis(oxy))bis(2,3-dihydro-1H-indene-2,1-diyl))bis(cyclohexane-3,1-diyl))bis(2-((S)-2-(methylamino)propanamido)acetyl))bis(pyrrolidine-2-carboxamide)
- CAS:
- 1258392-53-8
- MF:
- C58H78N8O8
- MW:
- 1015.29
- Mol File:
- 1258392-53-8.mol
AZD-5582 Chemical Properties
- Boiling point:
- 1207.3±65.0 °C(Predicted)
- Density
- 1.26±0.1 g/cm3(Predicted)
- storage temp.
- 4°C, protect from light, stored under nitrogen
- solubility
- DMF: 30 mg/ml; DMSO: 15 mg/ml; Ethanol: 30 mg/ml
- form
- A crystalline solid
- pka
- 12.99±0.40(Predicted)
- color
- White to yellow
AZD-5582 Usage And Synthesis
Uses
It is a novel class of dimeric Smac mimetics as potent IAP antagonists resulting in a clinical candidate for the treatment of cancer.
Biological Activity
AZD5582 is a divalent AVPI motif-based Smac (DIABLO) mimetic (SMC) th at acts a potent apoptosis protein repe at (BIR) domain-targeting antagonist against inhibitor of apoptosis proteins (IAPs) cIAP1/2 (BIR3 IC50 = 15/21 nM against 2.5 nM AbuRPFK-5FAM) and XIAP (BIR2/3 IC50 = 21/15 nM). AZD5582 abolishes cellular XIAP-caspase-9 interaction (1 μM, 4 hrs), induces cIAP1/2 degradation (EC50 = 0.1 nM, 1 hr) and apoptosis (GI50 <60 pM, 48 hrs) in MDA-MB-231 breast cancer cultures. AZD5582 causes substantial tumor regression by inducing cIAP1 degradation and apoptosis in tumor cells in MDA-MB-231 xenograft-bearing mice in vivo (3.0 mg/kg/wk i.v.).
AZD-5582Supplier
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