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AZ20

产品编号 T1958 CAS 1233339-22-4

AZ20 是一种有效且特异性的 ATR 激酶抑制剂，IC50值为 5 nM。它还抑制mTOR 活性，IC50值为 38 nM。

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AZ20, CAS 1233339-22-4

规格	价格/CNY	货期
2 mg	￥ 313	现货
5 mg	￥ 488	现货
10 mg	￥ 747	现货
25 mg	￥ 1,380	现货
50 mg	￥ 2,390	现货
100 mg	￥ 3,730	现货
1 mL * 10 mM (in DMSO)	￥ 547	现货

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	AZ20 is an effective and specific inhibitor of ATR kinase (IC50: 5 nM, in a cell-free assay), 8-fold selectivity over mTOR.
靶点活性	mTOR:38 nM, ATR:5 nM
体外活性	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.
体内活性	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。
激酶实验	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).
细胞实验	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.

分子量	412.51
分子式	C21H24N4O3S
CAS No.	1233339-22-4

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: 3 mg/mL (7.27 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 77 mg/mL (186.7 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
Ethanol / DMSO	1 mM	2.4242 mL	12.1209 mL	24.2418 mL	60.6046 mL
Ethanol / DMSO	5 mM	0.4848 mL	2.4242 mL	4.8484 mL	12.1209 mL
DMSO	10 mM	0.2424 mL	1.2121 mL	2.4242 mL	6.0605 mL
	20 mM	0.1212 mL	0.606 mL	1.2121 mL	3.0302 mL
	50 mM	0.0485 mL	0.2424 mL	0.4848 mL	1.2121 mL
	100 mM	0.0242 mL	0.1212 mL	0.2424 mL	0.606 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Xavier Jacq, et al. Cancer Res 2012;72(8 Suppl):Abstract nr 1823. 2. Foote KM, et al. J Med Chem, 2013, 56(5), 2125-2138.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

AZ20 1233339-22-4 DNA Damage/DNA Repair PI3K/Akt/mTOR signaling ATM/ATR mTOR Ataxia telangiectasia mutated inhibit AZ-20 ATM and RAD3 related Inhibitor AZ 20 inhibitor

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AZ20

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords