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AZ20ATR inhibitor,potent and selective


Catalog No. A3210
Size Price Stock Qty
5mg $128.00 In stock
10mg $214.00 In stock
50mg $727.00 In stock

Tel: +1-832-696-8203


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Sample solution is provided at 25 µL, 10mM.

Product Citations

1. Shah, Govind A., and Clodagh C. O’Shea. "Viral and cellular genomes activate distinct DNA damage responses." Cell 162.5 (2015): 987-1002. PMID:26317467

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Chemical structure


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Related Biological Data


Biological Activity

Description AZ20 is a potent and selective inhibitor of ATR kinase with IC50 value of 5 nM.
Targets ATR kinase          
IC50 5 nM          

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Chemical Properties

Cas No. 1233339-22-4 SDF Download SDF
Synonyms AZ-20;AZ 20
Chemical Name (3R)-4-[2-(3H-indol-4-yl)-6-(1-methylsulfonylcyclopropyl)pyrimidin-4-yl]-3-methylmorpholine
Canonical SMILES CC1COCCN1C2=NC(=NC(=C2)C3(CC3)S(=O)(=O)C)C4=C5CC=NC5=CC=C4
Formula C21H24N4O3S M.Wt 412.51
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request


AZ20 is a potent and selective inhibitor of ATR. AZ20 inhibits ATR immunoprecipitated from HeLa nuclear extracts with an IC50 value of 5 nM and ATR mediated phosphorylation of Chk1 in HT29 colorectal adenocarcinoma tumor cells with an IC50 value of 50 nM.
ATR is an attractive new anticancer drug target whose inhibitors have potential as chemo- or radiation sensitizers or as monotherapy in tumors addicted to particular DNA-repair pathways.
AZ20 is the first reported inhibitor of ATR protein kinase demonstrating tumor growth inhibition in vivo and is therefore a useful probe molecule to aid further investigation of ATR tumor biology. AZ20 potently inhibited the growth of LoVo colorectal adenocarcinoma tumor cells in vitro. In the mTOR (pAKT) cell assay, AZ20 weak inhibited recombinant mTOR enzyme activity. AZ20 shows good selectivity against all of the PI3K isoforms together with ATM and DNA-PK, and when tested in a large panel of kinases, AZ20 shows very high general kinase selectivity.
Female nude mice bearing LoVo tumors were treated with AZ20 orally at a dose of 25 mg/kg twice daily or 50 mg/kg once daily for 13 days. AZ20 showed monotherapy in vivo antitumor efficacy in LoVo colorectal xenografts in nude mice.
[1]. Foote KM, Blades K, Cronin A et al. 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.