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SML2900

AZD5582

Name: AZD5582
Brand: SIGMA

≥98% (HPLC), Smac mimetic and IAP inhibitor, powder

别名:

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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关于此项目

经验公式（希尔记法）:

C₅₈H₇₈N₈O₈

化学文摘社编号:

1258392-53-8

分子量:

1015.29

UNSPSC Code:

12352200

NACRES:

NA.77

MDL number:

MFCD28411397

Assay:

≥98% (HPLC)

Form:

powder

Quality level:

100

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属性

产品名称

AZD5582, ≥98% (HPLC)

Quality Level

100

assay

≥98% (HPLC)

form

powder

color

white to beige

storage temp.

−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

说明

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 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.

存储类别

11 - Combustible Solids

wgk

WGK 3

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Discovery of a novel class of dimeric Smac mimetics as potent IAP antagonists resulting in a clinical candidate for the treatment of cancer (AZD5582).

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

A novel small-molecule IAP antagonist, AZD5582, draws Mcl-1 down-regulation for induction of apoptosis through targeting of cIAP1 and XIAP in human pancreatic cancer.

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

AZD5582, an IAP antagonist that leads to apoptosis in head and neck squamous cell carcinoma cell lines and is eligible for combination with irradiation.

Lorenz Kadletz et al.

Acta oto-laryngologica, 137(3), 320-325 (2016-10-16)

On the one hand, AZD5582, an inhibitor of inhibitor of apoptosis family proteins (IAP), leads to cellular growth arrest and induction of apoptosis in head and neck squamous cell carcinoma (HNSCC) cell lines. On the other hand, it is a

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全球贸易项目编号

货号	GTIN
SML2900-25MG	04061842611041
SML2900-5MG	04061842611058