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AZ20 {[allProObj[0].p_purity_real_show]}

货号:A838709

AZ20是一种强效且选择性的 ATR 抑制剂,IC50 为 5 nM,对 mTOR(IC50 = 38 nM)具有 8 倍选择性。

AZ20 化学结构 CAS号:1233339-22-4
AZ20 化学结构
CAS号:1233339-22-4
AZ20 3D分子结构
CAS号:1233339-22-4
AZ20 化学结构 CAS号:1233339-22-4
AZ20 3D分子结构 CAS号:1233339-22-4
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AZ20 纯度/质量文件 产品仅供科研

货号:A838709 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 ATM ATR 其他靶点 纯度
Wortmannin ++

ATM, IC50: 150 nM

MLCK,DNA-PK,PI3K 99%+
CP-466722 +

ATM, IC50: 410 nM

99%+
Torin 2 ++

ATM, EC50: 28 nM

++

ATR, EC50: 35 nM

DNA-PK,mTOR 99%+
KU-55933 +++

ATM, IC50: 12.9 nM

96%
ETP-46464 +

ATM, IC50: 545 nM

+++

ATR, IC50: 14 nM

DNA-PK,mTOR 98%
CGK733 ++

ATM, IC50: 200 nM

++

ATR, IC50: 200 nM

99%+
AZD0156 99%+
Dactolisib +++

ATR, IC50: 21 nM

98+%
Ceralasertib ++++

ATR, IC50: 1 nM

99%+
Berzosertib +++

ATR, IC50: 19 nM

99%+
VE-821 +++

ATR, Ki: 13 nM

99%+
AZ20 ++++

ATR, IC50: 5 nM

mTOR 99%+
Schizandrin B +

ATR, IC50: 7.25 μM

P-gp 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

AZ20 生物活性

靶点
  • ATR

    ATR, IC50:5 nM

描述 AZ20 is a potent inhibitor of the ATR kinase, effectively inhibiting ATR extracted from HeLa nuclear extracts and ATR-mediated phosphorylation of Chk1 in HT29 colorectal adenocarcinoma cells with IC50 values of 5 nM and 50 nM, respectively[1].
体内研究

Administered orally at doses of 25 and 50 mg/kg, AZ20 exhibits high permeability and good stability in rat hepatocytes, achieving significant tumor growth inhibition in LoVo tumor-bearing female nude mice despite challenges in enhancing solubility, which suggests its potential as an anticancer agent[1].

体外研究

AZ20 is a potent inhibitor of the ATR kinase, effectively inhibiting ATR extracted from HeLa nuclear extracts and ATR-mediated phosphorylation of Chk1 in HT29 colorectal adenocarcinoma cells with IC50 values of 5 nM and 50 nM, respectively[1].

AZ20 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
HT29 cells Function assay 1 h  Inhibition of ATR-mediated CHK1 phosphorylation at serine 345 in human HT29 cells after 1 hr in presence of 4-nitroquinoline 1-oxide, IC50=0.05 μM 23394205
human MDA-MB-468 cells Function assay Inhibition of mTOR-mediated AKT phosphorylation at serine 473 in human MDA-MB-468 cells, IC50=2.4 μM 23394205
LoVo cells Growth inhibition assay 72 h Growth inhibition of human LoVo cells after 72 hrs by MTS assay, GI50=0.2 μM 23394205

AZ20 动物研究

Dose Mice: 25 mg/kg, 50 mg/kg[1] (p.o.)
Administration p.o.

AZ20 参考文献

[1]Foote KM, et al. Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity. J Med Chem. 2013 Mar 14

AZ20 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.42mL

0.48mL

0.24mL

12.12mL

2.42mL

1.21mL

24.24mL

4.85mL

2.42mL

AZ20 技术信息

CAS号1233339-22-4
分子式C21H24N4O3S
分子量 412.505
别名
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry,2-8°C

溶解度

DMSO: 105 mg/mL(254.54 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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