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EPZ004777

(CAS No:1338466-77-5)

EPZ004777 is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM in a cell-free assay and demonstrates >1,200-fold selectivity for DOT1L over all other tested PMTs.

CAS No:1338466-77-5

Molecular Weight(MW):539.67

Purity:99.00%

Specification:500MG;1G;5G;10G;50G;100G

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QC Documents

COA	MSDS	HPLC	NMR

ChemicalInfomation

CAS No:	1338466-77-5
Molecular formula(MF)	C₂₈H₄₁N₇O₄
Molecular Weight(MW):	539.67
Alias

Solubility

In vitro	DMSO	100 mg/mL (185.29 mM)
	Ethanol	100 mg/mL (185.29 mM)
	Water	<1 mg/mL
In vivo

Biological Activity

Description

EPZ004777 is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM in a cell-free assay and demonstrates >1,200-fold selectivity for DOT1L over all other tested PMTs.

Targets

DOT1L ^[1]
(Cell-free assay)

0.4 nM

In vitro

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. ^[1] EPZ004777 selectively inhibits proliferation of MLL–AF10 and CALM–AF10-transformed murine bone marrow cells. ^[2] 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. ^[3]

Cell Data

Cell Lines	Assay Type	Activity Description	PMID
human MOLM13 cells	Proliferation assay	Antiproliferative activity against human MOLM13 cells containing MLL-AF9, EC50=4 nM	23879463
human MV4-11 cells	Proliferation assay	Antiproliferative activity against human MV4-11 cells containing MLL-AF4, EC50=4 nM	23879463
human THP1 cells	Proliferation assay	Antiproliferative activity against human THP1 cells containing MLL-AF9, IC50=4 nM	23879463
human MCF10A cells	Function assay	Inhibition of DOT1L in human MCF10A cells assessed as reduction of H3K79 levelï¼ IC50=84 nM	25406853
human MLL cells	Function assay	Inhibition of Hoxa9 and Meis1 gene expression in human MLL cells	23879463
Sf9 cells	Function assay	Inhibition of human full length PRMT7 expressed in Sf9 cells, IC50=7.5 Î¼M	25893041

... Click to View More Cell Line Experimental Data

In vivo

EPZ004777 produces potent antitumor efficacy, and significantly increases median survival in a mouse xenograft model of MLL leukemia. ^[1]