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AZD5582

AZD5582, a novel small-molecule IAP inhibitor, binds potently to the BIR3 domains of cIAP1, cIAP2, and XIAP with IC50 values of 15, 21, and 15 nM. AZD5582 induces apoptosis.

AZD5582化学構造

CAS No. 1258392-53-8

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JPY 22000 国内在庫あり
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JPY 598500 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール：[email protected]
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AZD5582関連製品

シグナル伝達経路

IAP Signaling Pathways

IAPシグナル伝達経路

IAP阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
MDA-MB-231 Apoptosis assay 0.5 to 1.5 nM 1 to 3 hrs Induction of apoptosis in human MDA-MB-231 cells assessed as caspase-3 cleavage at 0.5 to 1.5 nM preincubated for 1 to 3 hrs followed by compound-washout measured after 24 hrs by luciferase reporter gene assay 24320998
MDA-MB-231 Antitumor assay 0.1 to 3 mg/kg 2 weeks Antitumor activity against human MDA-MB-231 cells xenografted in CB17 SCID mouse assessed as tumor growth inhibition at 0.1 to 3 mg/kg, iv administered once a week for 2 weeks measured twice a week for 78 days 24320998
MDA-MB-231 Function assay 0.05 to 3 mg/kg 4 to 18 hrs Induction of caspase-3 cleavage in tumor of CB17 SCID mouse xenografted with human MDA-MB-231 cells at 0.05 to 3 mg/kg, iv after 4 to 18 hrs by ELISA 24320998
MDA-MB-231 Function assay 0.05 to 3 mg/kg up to 18 hrs Induction of cIAP1 degradation in tumor of CB17 SCID mouse xenografted with human MDA-MB-231 cells at 0.05 to 3 mg/kg, iv up to 18 hrs by ELISA 24320998
MDA-MB-231 Apoptosis assay 0.5 to 1.5 nM 1 to 3 hrs Induction of apoptosis in human MDA-MB-231 cells assessed as cell death at 0.5 to 1.5 nM preincubated for 1 to 3 hrs followed by compound-washout measured after 72 hrs by MTS assay 24320998
MDA-MB-231 Function assay 1 uM 4 hrs Inhibition of XIAP-caspase-9 interaction in human MDA-MB-231 cells at 1 uM after 4 hrs by immunoprecipitation assay 24320998
MDA-MB-231 Function assay 0.03 to 1 nM 1 hr Binding affinity to cIAP2 in human MDA-MB-231 cells assessed as induction of protein degradation at 0.03 to 1 nM after 1 hr by Western blotting analysis 24320998
MDA-MB-231 Antiproliferative assay 48 hrs Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition after 48 hrs by Alamar Blue assay, GI50 = 0.00006 μM. 24320998
MDA-MB-231 Function assay 1 hr Binding affinity to cIAP1 in human MDA-MB-231 cells assessed as induction of protein degradation after 1 hr by ELISA, EC50 = 0.0001 μM. 24320998
BT549 Growth inhibition assay Growth inhibition of human BT549 cells 24320998
647V Growth inhibition assay Growth inhibition of human 647V cells 24320998
35612 Growth inhibition assay Growth inhibition of human 97-7 cells 24320998
MIAPaCa2 Growth inhibition assay Growth inhibition of human MIAPaCa2 cells 24320998
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生物活性

製品説明 AZD5582, a novel small-molecule IAP inhibitor, binds potently to the BIR3 domains of cIAP1, cIAP2, and XIAP with IC50 values of 15, 21, and 15 nM. AZD5582 induces apoptosis.
Targets
cIAP1 [1]
(Cell-free assay)		 XIAP [1]
(Cell-free assay)		 cIAP2 [1]
(Cell-free assay)
15 nM 15 nM 21 nM
In Vitro
In vitro Human pancreatic cancer cells display different sensitivities to the synthetic IAP antagonist, AZD5582. Treating human pancreatic cancer cells with AZD5582 differentially induces apoptosis, dependent on the expression of p-Akt and p-XIAP. It targets cIAP1 to induce TNF-α-induced apoptosis. AZD5582 induces a decrease of Mcl-1 protein, a member of the Bcl-2 family, but not that of Bcl-2 and Bcl-xL[1]. HNSCC (head and neck squamous cell carcinoma) cell lines SCC25, Cal27, and FaDu show a dose-dependent cytotoxic effect after treatment with AZD5582[2].
細胞実験 細胞株 The human pancreatic cancer cell lines including BxPC-3, Miapaca-2, Panc-1, Panc0813, PL45, Capan-1, Capan-2 and AsPC-1
濃度 0, 0.01, 0.1, 0.5 μM
反応時間 72 h
実験の流れ

DNA or siRNA-transfected or AZD5582-treated cells are collected and cell death is determined by trypan blue exclusion using at least 200∼500 cells. For the MTS assay, pancreatic cancer cells are seeded at 1∼3 × 104 cells/well in a 96-well microtiter plate. The following day, cells are treated with AZD5582, an IAP antagonist, with various doses for 72 h. The MTS assay is performed according to the MTS assay protocol 
実験結果図 Methods Biomarkers 結果図 PMID
Western blot XIAP 26314849
In Vivo
In Vivo After AZD5582 treatment, tumor growth and weight decrease, whereas cleaved caspase 3 expression increases in Panc-1-derived xenograft model[1]. When administered intravenously to MDA-MB-231 xenograft-bearing mice, AZD5582 results in cIAP1 degradation and caspase-3 cleavage within tumor cells and causes substantial tumor regressions following two weekly doses of 3.0 mg/kg. Following a modest 0.5 mg/kg intravenous bolus dose of AZD5582 in mice, unbound plasma levels remain above the concentrations at which apoptosis induction and cell death are observed in MDA-MB-231 cells over the course of several hours. Although cIAP1 degradation happens very quickly upon exposure to AZD5582 in vivo, apoptosis induction (as measured by the amount of cleaved caspase-3) takes longer to reach a maximal effect. A single agent AZD5582 does not exhibit broad-based cytotoxicity but instead should be employed in selected tumor settings expected to be sensitive to IAP inhibitors or in rational combinations with other targeted therapies. The dihydrochloride salt of AZD5582 has sufficient aqueous solubility (>7 mg/mL at pH 4−6) to enable formulation for intravenous administration at the projected efficacious doses. With respect to chemical stability, AZD5582 is found to be photostable and hydrolytically stable between pH 4−6, although some amide hydrolysis is observed under strongly acidic (pH < 1) and basic (pH > 8) conditions. In addition, the compound is stable in the plasma of multiple species, with no compound degradation observed after several hours under physiological conditions[3].
動物実験 動物モデル Xenograft tumor (in Balb/c nude mice)
投与量 3 mg/kg
投与経路 i.v.

化学情報

分子量 1015.29 化学式

C58H78N8O8
CAS No. 1258392-53-8 SDF Download AZD5582 SDFをダウンロードする
Smiles CC(C(=O)NC(C1CCCCC1)C(=O)N2CCCC2C(=O)NC3C(CC4=CC=CC=C34)OCC#CC#CCOC5CC6=CC=CC=C6C5NC(=O)C7CCCN7C(=O)C(C8CCCCC8)NC(=O)C(C)NC)NC
保管

In vitro
Batch:

Water : 100 mg/mL

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

mg/kg g μL 匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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