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EPZ004777 EPZ004777 is a potent, selective inhibitor of DOT1L. Treatment of mixed lineage leukemia (MLL) cells with EPZ004777 selectively inhibits H3K79 methylation and blocks expression of leukemogenic genes. Exposure of leukemic cells to EPZ004777 results in selective killing of those cells bearing the MLL gene translocation, with little effect on non-MLL-translocated cells. Finally, in vivo administration of EPZ004777 leads to extension of survival in a mouse MLL xenograft model. These results provide compelling support for DOT1L inhibition as a basis for targeted therapeutics against MLL. Uses: Reprogramming. Synonyms: EPZ004777; EPZ 004777; EPZ-004777. Grades: 0.98. CAS No. 1338466-77-5. Molecular formula: C28H41N7O4. Mole weight: 539.681. BOC Sciences 11
EPZ004777 hydrochloride EPZ004777 selectively inhibits cellular H3K79 methylation and inhibits expression of key MLL fusion target genes. Following DOT1L inhibition, EPZ004777 selectively inhibits proliferation of MLL-Rearranged cell lines and MLL-AF9-transformed murine hematopoietic cells. In addition, EPZ004777 also induces differentiation and apoptosis in MLL-rearranged cells. EPZ004777 selectively inhibits proliferation of MLL-AF10 and CALM-AF10-transformed murine bone marrow cells. DOT1L inhibition by EPZ004777 results in significantly decreased proliferation, decreased expression of MLL-AF6 target genes, and cell cycle arrest of MLL-AF6-transformed cells. Synonyms: EPZ 004777 hydrochloride; EPZ-004777 hydrochloride; EPZ004777 hydrochloride. Grades: >98%. CAS No. 1380316-03-9. Molecular formula: C28H42ClN7O4. Mole weight: 576.13. BOC Sciences 10

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