Chemical Information

Biological Activity of AZ20

AZ20 is a potent and selective inhibitor of ATR with an IC50 of 5 nM; 8-fold selectivity over mTOR(IC50=38 nM).
IC50 Value: 5 nM [1]
Target: ATR
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].

References on AZ20

[1]. Foote KM, Blades K, Cronin A, 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;56(5):2125-38.

[2]. Xavier Jacq, Lisa Smith, Elaine Brown, Abstract 1823: AZ20, a novel potent and selective inhibitor of ATR kinase with in vivo antitumour activity. Cancer Research: April 15, 2012; Volume 72, Issue 8, Supplement 1