AZ20

Mechanism of action: ATR serine/threonine kinase inhibitor

Preclinical pharmacology

AZ20 is a potent inhibitor of ATR immunoprecipitated from HeLa nuclear extracts with an IC₅₀ of 4.5nM and ATR mediated phosphorylation of Chk1 in HT29 colorectal adenocarcinoma tumour cells with an IC₅₀ of 50 nMATR. AZ20 is orally bioavailable mouse, rat and dog with unbound mouse plasma C_max = 0.86 µM ±0.12 @ 50mg/kg PO, 2h. The CNS exposure is unknown.

LoVo single agent activity: 78% TGI p <0.0005 d 21 (50mg/kg QD or 25mg/kg BD PO, 2-weeks), ≤10% body weight loss.

Additional Information

Publications for this compound

Find out more about this compound by reading related Publications:

PlublMed.gov

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.

Gene information from the NCBi

This compound works on the following genes:

Gene 545 - learn more