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Description: EPZ004777 (EPZ-004777) is a potent and selective inhibitor of DOT1 Like Histone Lysine Methyltransferase (DOT1L) inhibitor with antineoplastic activity. It inhibits DOT1L with an IC50 of 0.4 nM in a cell-free assay. It shows potent in vitro antiproliferative activity and high in vivo antitumor efficacy. Exposure of leukemic cells to EPZ 004777 laed to selective killing of cells bearing MLL gene translocation, with little effect on non-MLL-translocated cells. In addition, EPZ004777 extended the survival of mice bearing a MLL xenograft model.
References: Leukemia. 2013 Apr; 27(4):813-22; Cancer Cell. 2011 Jul 12; 20(1):53-65.
Related CAS: 1380316-03-9 (HCl)
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