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Description: AZD7762 is a novel, potent, selective and ATP-competitive small molecule inhibitor of Chk1 (checkpoint kinases) with IC50 of 5 nM in a cell-free assay. It is equally potent against Chk2 and less potent against CAM, Yes, Fyn, Lyn, Hck and Lck. AZD7762 prevents cell cycle arrest and DNA repair in DNA damaged tumor cells, causing tumor cell apoptosis. Hence, it potentiates the antitumor activity of DNA damaging agents and can be used as a chemosensitizing agent. Chk1 (checkpoint kinases) are protein kinases that regulate either G1/S or G2/M transitions in the cell cycle. In the presence of DNA damage or incomplete DNA replication, Chks become activated and initiate cell cycle arrest to allow DNA repair or the completion of DNA replication.
References: Mol Cancer Ther. 2008 Sep; 7(9):2955-66.
Related CAS?1246094-78-9 (AZD7762 HCl); 860352-01-8 (free base)
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