Synonyms: 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]; AZD 5582; AZD-5582
Molecular Formula: C58H78N8O8
Molecular Weight: 1015.29
Linear Structural Formula: C58H78N8O8
MDL Number: MFCD28411397
Purity: >=98% (HPLC)
Storage: -20C
Biochem Physiol Actions: AZD5582 is a divalent AVPI motif-based Smac (DIABLO) mimetic (SMC) that acts a potent apoptosis protein repeat (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 muM, 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 g k i.v.).<>