AZ20

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Description

AZ20 is a novel potent and selective inhibitor of ATR kinase with IC50 of 5 nM, 8-fold selectivity over mTOR. In vitro, AZ20 decreases pChk1 Ser345, pChk1 Ser317 and pChk1 Ser296 levels in a concentration-dependent manner. Prolonged exposure with AZ20 increases H2AX pan-nuclear staining, indicative of replication stress. AZ20 induces growth inhibition and cell death and its profile of activity is distinctly when compares with other cytotoxic agents. in vivo,AZ20 induces significant tumour growth inhibition at well tolerated doses.

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