ホームページ PI3K/Akt/mTOR ATM/ATR inhibitor AZ20 For research use only.

AZ20

AZ20 is a novel potent and selective inhibitor of ATR kinase with IC50 of 5 nM in a cell-free assay, 8-fold selectivity over mTOR.

AZ20化学構造

CAS No. 1233339-22-4

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 40500 国内在庫あり
JPY 29500 国内在庫あり
JPY 85500 国内在庫あり
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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文献中Selleckの製品使用例（48）

製品安全説明書

現在のバッチを見る： 純度： 99.92%
99.92

AZ20関連製品

シグナル伝達経路

ATM/ATR Signaling Pathways

ATM/ATRシグナル伝達経路

ATM/ATR阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
LoVo Antitumor assay 50 mg/kg 13 days Antitumor activity against human LoVo cells xenografted in Swiss nu/nu mouse assessed as tumor growth inhibition at 50 mg/kg, po qd for 13 days relative to control 23394205
LoVo Antitumor assay 25 mg/kg 13 days Antitumor activity against human LoVo cells xenografted in Swiss nu/nu mouse assessed as tumor growth inhibition at 25 mg/kg, po bid for 13 days relative to control 23394205
LoVo Function assay 25 mg/kg 8 hrs Plasma concentration in Swiss nu/nu mouse xenografted with human LoVo cells at 25 mg/kg, po bid after 8 hrs, Cp=1.8μM 30346772
LoVo Function assay 50 mg/kg 8 hrs Plasma concentration in Swiss nu/nu mouse xenografted with human LoVo cells at 50 mg/kg, po qd after 8 hrs, Cp=3.5μM 30346772
LoVo Growth inhibition assay 72 hrs Growth inhibition of human LoVo cells after 72 hrs by MTS assay, GI50=0.2μM 23394205
HT29 Function assay 1 hr Inhibition of ATR-mediated CHK1 phosphorylation at serine 345 in human HT29 cells after 1 hr in presence of 4-nitroquinoline 1-oxide, IC50=0.05μM 23394205
HT29 Function assay 60 mins Inhibition of ATR in human HT29 cells after 60 mins by Hoechst 33258 staining-based assay, IC50=0.061μM 30346772
LoVo Cytotoxicity assay 72 hrs Cytotoxicity against human LoVo cells after 72 hrs by MTS assay, GI50=0.2μM 30346772
HT-29 Cytotoxicity assay 72 hrs Cytotoxicity against human HT-29 cells after 72 hrs by MTS assay, GI50=0.97μM 30346772
MDA-MB-468 Function assay Inhibition of mTOR-mediated AKT phosphorylation at serine 473 in human MDA-MB-468 cells, IC50=2.4μM 23394205
MDA-MB-468 Function assay Inhibition of mTOR in human MDA-MB-468 cells assessed as decrease in 70S6K S235/236 phosphorylation, IC50=0.72μM 30346772
MDA-MB-468 Function assay Inhibition of mTOR in human MDA-MB-468 cells assessed as decrease in AKT phosphorylation at S473 residue, IC50=2.4μM 30346772
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生物活性

製品説明 AZ20 is a novel potent and selective inhibitor of ATR kinase with IC50 of 5 nM in a cell-free assay, 8-fold selectivity over mTOR.
特性 ATR-selective inhibitor with high permeability and good stability.
Targets
ATR [2]
(Cell-free assay)		 mTOR [2]
(Cell-free assay)
5 nM 38 nM
In Vitro
In vitro AZ20 shows good selectivity against all of the PI3K isoforms together with ATM and DNA-PK. [2] In vitro, AZ20 decreases pChk1 Ser345, pChk1 Ser317 and pChk1 Ser296 levels in a concentration-dependent manner. Prolonged exposure with AZ20 increases γH2AX pan-nuclear staining, indicative of replication stress. This is associated with S-phase arrest and increase in phospho-histone H3. AZ20 induces growth inhibition and cell death in vitro and its profile of activity is distinct from other cytotoxic agents. The cytotoxic effect of AZ20 can be increased in combination with the selective ATM inhibitor KU-60019. [1]
実験結果図 Methods Biomarkers 結果図 PMID
Growth inhibition assay IC50 28176818
Western blot p-CDK1 / CDK1 / p-CDK2 / CDK2 γH2AX / RRM1 / RRM2 28176818
In Vivo
In Vivo Female nude mice bearing LoVo tumors are treated with AZ20 orally at a dose of 25 mg/kg twice daily or 50 mg/kg once daily for 13 days, led to significant tumor growth inhibition. [2] This is associated with a persistent elevation of γH2AX pan-nuclear staining in xenograft tissue, but a transient increase in mouse bone marrow at therapeutic doses, suggesting a favourable therapeutic index. [1] AZ20 is assessed for drug−drug interaction (DDI) potential specifically from inhibition of cytochrome P450 enzymes. AZ20 is found to inhibit the cytochrome 3A4-mediated metabolism of midazolam by 50% at 10 μM. AZ20 has respectable bioavailability in a low dose rat PK study. [2]
動物実験 動物モデル LoVo colorectal adenocarcinoma xenografts
投与量 25 mg/kg twice daily and 50 mg/kg once daily
投与経路 orally

化学情報

分子量 412.51 化学式

C21H24N4O3S
CAS No. 1233339-22-4 SDF Download AZ20 SDFをダウンロードする
Smiles CC1COCCN1C2=NC(=NC(=C2)C3(CC3)S(=O)(=O)C)C4=C5C=CNC5=CC=C4
保管

In vitro
Batch:

DMSO : 83 mg/mL ( (201.2 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 3 mg/mL

Water : Insoluble

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。

技術サポート

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Handling Instructions

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よくある質問（FAQ）

質問1:
If I want to completely block the kinase activity from the in vitro cell lines, how much concentration I should use?

回答
IC50 5nM was quoted from a previous publication in which the author tested IC50 of AZ20 in cell free assay. In cell culture, many factors, such as membrane permeability and target protein concentration, may affect the efficiency. Each cell line responses to the same compound differently and it is very difficult to predict the optimized concentration simply based on cell free data. In cell culture experiment, the required concentration is usually higher. We recommend that you perform a pilot experiment and test different concentrations (50nM to 500uM) to get the optimized condition.

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