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| 产品名称 | ATM ↓ ↑ | ATR ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Wortmannin |
++
ATM, IC50: 150 nM |
DNA-PK,PI3K,MLCK | 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% | ||||||||||||||||
| m-PEG25-NHS ester |
++++
ATR, IC50: 7 nM |
95% | |||||||||||||||||
| 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。 | |||||||||||||||||||
| 靶点 |
|
| 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]. |
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活性说明 | 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 |
| Dose | Mice: 25 mg/kg, 50 mg/kg[1] (p.o.) |
| Administration | p.o. |
| 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 |
|
| CAS号 | 1233339-22-4 |
| 分子式 | C21H24N4O3S |
| 分子量 | 412.51 |
| SMILES Code | O=S(C1(C2=CC(N3[C@H](C)COCC3)=NC(C4=CC=CC5=C4C=CN5)=N2)CC1)(C)=O |
| MDL No. | MFCD25976730 |
| 别名 | |
| 运输 | 蓝冰 |
| InChI Key | SCGCBAAYLFTIJU-CQSZACIVSA-N |
| Pubchem ID | 46244454 |
| 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 |
| 溶解方案 |
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 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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