[CAS NO. 1338466-77-5] EPZ004777

Ships within

Stock

Price

Qty

Total

$0.00

Please click "REQUEST A QUOTE" button if you need other sizes or custom synthesis

request a quote

If there is no stock, or you need other sizes or custom synthesis, please:

PRODUCTS SPECIFICATIONS [1338466-77-5]

Catalog

SLK-S7353

Brand

Selleck

CAS

1338466-77-5

DESCRIPTION [1338466-77-5]

Overview

MDL	MFCD25563264
Molecular Weight	539.67
Molecular Formula	C28H41N7O4
SMILES	O[C@H]1[C@](N2C=3C(C=C2)=C(N)N=CN3)(O[C@H](CN(CCCNC(NC4=CC=C(C(C)(C)C)C=C4)=O)C(C)C)[C@H]1O)[H]

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	1.8530 mL	9.2649 mL	18.5298 mL
5 mM	0.3706 mL	1.8530 mL	3.7060 mL
10 mM	0.1853 mL	0.9265 mL	1.8530 mL
50 mM	0.0371 mL	0.1853 mL	0.3706 mL

Description

EPZ004777 is a potent, selective 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. EPZ004777 induces .

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. 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.

In vivo

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

References

[1] Daigle SR, et al. Cancer Cell. 2011, 20(1), 53-65.
[2] Chen L, et al. Leukemia. 2013, 27(4), 813-822.
[3] Deshpande AJ, et al. Blood. 2013, 121(13), 2533-2541.

Synonyms

7H-Pyrrolo[2,3-d]pyrimidin-4-amine, 7-[5-deoxy-5-[[3-[[[[4-(1,1-dimethylethyl)phenyl]amino]carbonyl]amino]propyl](1-methylethyl)amino]-β-D-ribofuranosyl]-

7-[5-Deoxy-5-[[3-[[[[4-(1,1-dimethylethyl)phenyl]amino]carbonyl]amino]propyl](1-methylethyl)amino]-β-D-ribofuranosyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine

EPZ 004777