ATR Kinase inhibitor / AZ20 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
Biochemicals & reagents
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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
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TARGET: Kinase -- PATHWAY: DNA damage -- RESEARCH AREA: Cell death -- DISEASE AREA: Cancer