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
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