化合物 AZ20|T1958|TargetMol

AZ20
1233339-22-4

￥313 2mg 起订

￥488 5mg 起订

￥747 10mg 起订

上海更新日期：2024-09-29

TargetMol中国（陶术生物）

VIP3年

联系人：邵小姐

手机：4008200310 拨打

邮箱：marketing@tsbiochem.com

产品详情:

中文名称：: 化合物 AZ20

英文名称：: AZ20

CAS号：: 1233339-22-4

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 98.02%

产品类别：: 抑制剂

货号：: T1958

Product Introduction

Bioactivity

Name	AZ20
Description	AZ20 is an effective and specific inhibitor of ATR kinase (IC50: 5 nM, in a cell-free assay), 8-fold selectivity over mTOR.
Cell Research	AZ20 is dissolved in 100% DMSO. Compound dose ranges are created by diluting in 100% DMSO and then further into assay medium (EMEM, 10% FCS, 1% glutamine) using a Labcyte Echo acoustic dispensing instrument. Cells are plated in 384-well Costar plates at 9×104?cells per mL in 40 μL of EMEM, 10% FCS, 1% glutamine and grown for 24 h. Following addition of compound the cells are incubated for 60 min. A final concentration of 3 μM?4NQO?(prepared in 100% DMSO) is then added using the Labcyte Echo, and the cells are incubated for a further 60 min. The cells are fixed by adding 40 μL of 3.7% v/v formaldehyde solution for 20 min. After removal of fix, cells are washed with PBS and permeabilized in 40 μL of PBS containing 0.1% Triton X-100. The cells are then washed, and 15 μL primary antibody solution (pChk1 Ser345) is added. The plates are incubated at 4°C overnight. The primary antibody is then washed off, and 20 μL of secondary antibody solution and 1 μM Hoechst 33258 added for 90 min at room temperature. The plates are washed and left in 40 μL of PBS. Plates are then read on an ArrayScan VTI instrument to determine staining intensities, and dose responses are obtained and used to determine the IC50?values for the compounds.
Kinase Assay	ATR for use in the in vitro enzyme assay is obtained from HeLa nuclear extract by immunoprecipitation with rabbit polyclonal antiserum raised to amino acids 400-480 of ATR contained in the following buffer: 25 mM HEPES (pH 7.4), 2 mM MgCl2, 250 mM NaCl, 0.5 mM EDTA, 0.1 mM Na3VO4, 10% v/v glycerol, and 0.01% v/v Tween 20. ATR-antibody complexes are isolated from nuclear extract by incubating with protein A-Sepharose beads for 1 h and then through centrifugation to recover the beads. In the well of a 96-well plate, 10 μL ATR-containing Sepharose beads are incubated with 1 μg of substrate glutathione?S-transferase-p53N66 (NH2-terminal 66 amino acids of p53 fused to glutathione?S-transferase are expressed in?E. coli) in ATR assay buffer (50 mM HEPES (pH 7.4), 150 mM NaCl, 6 mM MgCl2, 4 mM MnCl2, 0.1 mM Na3VO4, 0.1 mM DTT, and 10% (v/v) glycerol) at 37°C in the presence or absence of inhibitor. After 10 min with gentle shaking, ATP is added to a final concentration of 3 μM and the reaction continued at 37°C for an additional 1 h. The reaction is stopped by addition of 100 μL of PBS, and the reaction is transferred to a white opaque glutathione coated 96-well plate and incubated overnight at 4°C. This plate is then washed with PBS/0.05% (v/v) Tween 20, blotted dry, and analyzed by a standard ELISA technique with a phosphoserine 15 p53 antibody. The detection of phosphorylated glutathione?S-transferase-p53N66 substrate is performed in combination with a goat anti-mouse horseradish peroxidase-conjugated secondary antibody. Enhanced chemiluminescence solution is used to produce a signal, and chemiluminescent detection is carried out via a TopCount plate reader. The resulting calculated % enzyme activity is then used to determine the IC50?values for the compounds (IC50?taken as the concentration at which 50% of the enzyme activity is inhibited).
In vitro	AZ20（10 μM）可使CYP3A4介导的咪达唑仑代谢的50％被抑制.LoVo肿瘤的雌性裸鼠中,服用13天AZ20（25 mg/kg,2次/天,p.o.;50 mg/kg/day,p.o. ）可使肿瘤生长受到显著抑制,这与异种移植组织中γH2AX核染色的持续广泛升高有关.
In vivo	在体外,AZ20浓度依赖性地降低pChk1 Ser345/317/296水平。延长AZ20的处理时间可增加γH2AX核染色,这是因为存在复制压力,且与S期阻滞和组蛋白H3的磷酸化水平增加有关。AZ20对体外生长抑制和细胞死亡的诱导作用是完全不同于其它细胞毒性药物的。AZ2与ATM 抑制剂KU-60019联用会增加细胞毒性。
Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
Solubility Information	Ethanol : 3 mg/mL (7.27 mM) H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 50 mg/mL (121.21 mM), Sonication is recommended.
Keywords	AZ20 \| Ataxia telangiectasia mutated \| inhibit \| AZ-20 \| ATM and RAD3 related \| Inhibitor \| ATM/ATR \| AZ 20
Inhibitors Related	Schisandrin B \| α-Hydroxyglutaric Acid Lithium \| P-2281 \| Capivasertib \| Rapamycin \| Elimusertib \| Bimiralisib \| L-Leucine \| GDC0084 \| Tacrolimus \| Dihydromyricetin \| Sapanisertib
Related Compound Libraries	Inhibitor Library \| Bioactive Compound Library \| Bioactive Compounds Library Max \| Anti-Cancer Metabolism Compound Library \| Kinase Inhibitor Library \| Anti-Aging Compound Library \| NO PAINS Compound Library \| Anti-Lung Cancer Compound Library \| DNA Damage & Repair Compound Library \| Glycolysis Compound Library

AZ20|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

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