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Merck
모든 사진(1)

주요 문서

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SML2900

Sigma-Aldrich

AZD5582

≥98% (HPLC)

동의어(들):

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

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모든 사진(1)

About This Item

실험식(Hill 표기법):
C58H78N8O8
CAS Number:
1258392-53-8
Molecular Weight:
1015.29
MDL number:
MFCD28411397
UNSPSC 코드:
12352200
NACRES:
NA.77

Quality Level

100

분석

≥98% (HPLC)

양식

powder

색상

white to beige

저장 온도

−20°C

SMILES string

CN[C@@H](C)C(N[C@@H](C1CCCCC1)C(N2[C@H](C(N[C@H]3C4=C(C=CC=C4)C[C@H]3OCC#CC#CCO[C@@H]5CC6=C(C=CC=C6)[C@@H]5NC([C@@H]7CCCN7C([C@H](C8CCCCC8)NC([C@H](C)NC)=O)=O)=O)=O)CCC2)=O)=O

InChI

1S/C58H78N8O8/c1-37(59-3)53(67)61-49(39-21-9-7-10-22-39)57(71)65-31-19-29-45(65)55(69)63-51-43-27-15-13-25-41(43)35-47(51)73-33-17-5-6-18-34-74-48-36-42-26-14-16-28-44(42)52(48)64-56(70)46-30-20-32-66(46)58(72)50(40-23-11-8-12-24-40)62-54(68)38(2)60-4/h13

InChI key

WLMCRYCCYXHPQF-ZVMUOSSASA-N

생화학적/생리학적 작용

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 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.).
Divalent Smac mimetic compound (SMC) as a potent BIR domain-targeting antagonist against inhibitor of apoptosis proteins (IAPs) cIAP1/2 & XIAP in vitro and in vivo.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

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시험 성적서(COA)

Lot/Batch Number

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문서 라이브러리 방문

Jai-Hee Moon et al.
Oncotarget, 6(29), 26895-26908 (2015-09-01)
Inhibitor of apoptosis proteins (IAPs) plays an important role in controlling cancer cell survival. IAPs have therefore attracted considerable attention as potential targets in anticancer therapy. In this study, we investigated the anti-tumor effect of AZD5582, a novel small-molecule IAP
Inbar Shlomovitz et al.
The FEBS journal, 286(3), 507-522 (2018-12-24)
Interleukin-33 (IL-33) is a pro-inflammatory cytokine that plays a significant role in inflammatory diseases by activating immune cells to induce type 2 immune responses upon its release. Although IL-33 is known to be released during tissue damage, its exact release
Edward J Hennessy et al.
Journal of medicinal chemistry, 56(24), 9897-9919 (2013-12-11)
A series of dimeric compounds based on the AVPI motif of Smac were designed and prepared as antagonists of the inhibitor of apoptosis proteins (IAPs). Optimization of cellular potency, physical properties, and pharmacokinetic parameters led to the identification of compound
Sefi Zargarian et al.
PLoS biology, 15(6), e2002711-e2002711 (2017-06-27)
Necroptosis is a regulated, nonapoptotic form of cell death initiated by receptor-interacting protein kinase-3 (RIPK3) and mixed lineage kinase domain-like (MLKL) proteins. It is considered to be a form of regulated necrosis, and, by lacking the "find me" and "eat
Qin Hao et al.
Cancer cell international, 18, 84-84 (2018-06-28)
The prognosis of lung cancer is very poor and hence new therapeutic strategies are urgently desired. In this study, we searched for efficacious Smac mimetic-based combination therapies with biomarkers to predict responses for non-small cell lung cancer (NSCLC). NSCLC cell
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