1233339-22-4

AZ20 (1233339-22-4) is a potent and highly selective inhibitor of Ataxia telangiectasia mutated and RAD3-related (ATR) kinase (IC50?= 5 nM in vitro; IC50?= 50 nM in HT29 colorectal adenocarcinoma cells).1?Combination therapy with AZ20 and gemcitabine resulted in synergistic inhibition of tumor cell growth and cell death initiation in pancreatic cancer cell lines.2

AZ20 is a potent and selective inhibitor of ATR (ATM-Rad3-related) kinase with in vivo antitumor activity.

ChEBI: (3R)-4-[2-(1H-indol-4-yl)-6-(1-methylsulfonylcyclopropyl)-4-pyrimidinyl]-3-methylmorpholine is a member of indoles.

This novel potent inhibitor (FW = 412.51 g/mol; CAS 1233339-22-4; Solubility: 83 mg/mL DMSO; <1 mg/mL H2O), also named AZ 20 and 4- [4-[ (3R) -3-methyl-4-morpholinyl]-6-[1- (methylsulfonyl) cyclopropyl]-2- pyrimidinyl]-1H-indole, selectively targets ATR kinase, a serine/threonine- protein kinase also known as ataxia telangiectasia and Rad3-related protein (or ATR) kinase with IC50 of 5 nM, 8-fold selectivity over mTOR.

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1) Foote?et al.?(2013)?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.?56?2125 2) Liu?et al.?(2017)?Inhibition of ATR potentiates the cytotoxic effect of gemcitabine on pancreatic cancer cell lines through enhancement of DNA damage and abrogation of ribonucleotide reductase induction by gemcitabine; Oncol. Rep.?37?3377