| 生化机理 |
Description:
IC50 Value: 5nM [1]
AZ20 is a potent and selective inhibitor of ATR with an IC50 value of 5 nM. AZ20 was discovered from a lead discovery and early optimization campaign from an mTOR inhibitor screening hit.
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 [2].
in vivo: AZ20 induces significant tumour growth inhibition in vivo at well tolerated doses [2].
Clinical trial: N/A
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