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Background: EPZ004777 selectively inhibits cellular H3K79 methylation and inhibits expression of key MLL fusion target genes. EPZ004777 produces potent antitumor efficacy, and significantly increases median survival in a mouse xenograft model of MLL leukemia. 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. 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. EPZ004777 has also been found to selectively inhibit the proliferation of MLL-AF10 and CALM-AF10 transformed cells in a dose dependent manner (IC50: 0.1 µM to 1 µM), in which the mRNA expression levels of two hallmark leukemogenic genes (Hoxa9 and Meis1) are suppressed by EPZ004777 in a concentration dependent manner.
Biological Activity: EPZ004777 is a potent, selective DOT1L inhibitor with IC50 of 400 pM. EPZ004777 also exhibits anti-proliferative activity against both MLL-rearranged and non-rearranged human leukemia cell lines, including RS4;11 (IC50: 6.47 µM), SEM (IC50: 1.72 µM), MV4-11 (IC50: 0.17 µM), THP-1 (IC50: 3.36 µM), MOLM-13 (IC50: 0.72 µM), KOPN-8 (IC50: 0.62 µM), REH (IC50: 13.9 µM), Kasumi-1 (IC50: 32.99 µM) and 697 (IC50: 36.57 µM)
CAS Number: 1338466-77-5
Description: EPZ004777 is a potent, selective DOT1L inhibitor with IC50 of 400 pM. EPZ004777 selectively kills a variety of MLL-rearranged leukemia cells, including an MLL-AF4 leukemia cell line MV4-11 and an MLL-AF9 leukemia cell line MOLM13.
Solubility: Soluble in DMSO
Storage Stability: Store at or below -20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.
Target: Dot1L
Biosafety Level: Not applicable (BSL-1)
References: 1. Yu W, Cet al. Nat Commun. 2012;3:1288.
2. Chen L,et al. 2013 Apr;27(4):813-22.
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