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主要文書

原産地証明書（COO）/試験成績書（COA）

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安全性情報

適用法令

SML2900

AZD5582

Name: AZD5582
Brand: SIGMA

≥98% (HPLC)

別名:

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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About This Item

実験式（ヒル表記法）:

C₅₈H₇₈N₈O₈

CAS番号:

1258392-53-8

分子量:

1015.29

MDL番号:

MFCD28411397

UNSPSCコード:

12352200

NACRES:

NA.77

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Sigma-Aldrich

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（+/-）-JQ1

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SML1985

GSK6853

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13752

ペニシリンG ナトリウム塩

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Sigma-Aldrich

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Sigma-Aldrich

P0022

PS48

Sigma-Aldrich

T6674

腫瘍壊死因子-α ヒト

Y0001239

Dobutamine impurity mixture

Sigma-Aldrich

H0879

臭化ヘキサメトニウム

品質水準

100

アッセイ

≥98% (HPLC)

フォーム

powder

色

white to beige

保管温度

−20°C

SMILES記法

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

生物化学的／生理学的作用

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.

保管分類コード

11 - Combustible Solids

WGK

WGK 3

適用法令

試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。

Jan Code

SML2900-25MG:
SML2900-5MG:
SML2900-BULK:
SML2900-VAR:

最新バージョンのいずれかを選択してください：

試験成績書（COA）

Lot/Batch Number

0000342582

適切なバージョンが見つかりませんか。

特定のバージョンが必要な場合は、ロット番号またはバッチ番号で特定の証明書を検索できます。

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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

Necroptosis directly induces the release of full-length biologically active IL-33 in vitro and in an inflammatory disease model.

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

Successful Anti-PD-1 Cancer Immunotherapy Requires T Cell-Dendritic Cell Crosstalk Involving the Cytokines IFN-γ and IL-12.

Christopher S Garris et al.

Immunity, 49(6), 1148-1161 (2018-12-16)

Anti-PD-1 immune checkpoint blockers can induce sustained clinical responses in cancer but how they function in vivo remains incompletely understood. Here, we combined intravital real-time imaging with single-cell RNA sequencing analysis and mouse models to uncover anti-PD-1 pharmacodynamics directly within tumors.

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

主要文書

安全性情報

AZD5582

≥98% (HPLC)

About This Item

おすすめの製品

特性

品質水準

アッセイ

フォーム

色

保管温度

SMILES記法

InChI

InChI Key

詳細

生物化学的／生理学的作用

安全性情報

保管分類コード

WGK

適用法令

Jan Code

資料

試験成績書（COA）

以前この製品を購入いただいたことがある場合

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