EPZ 004777

Name: EPZ 004777
Brand: Tocris Bioscience
SKU: 5567

Tocris Bioscience, part of Bio-Techne | Catalog # 5567

Citations (6)

COA / SDS

Highly potent DOT1L inhibitor

Key Product Details

Description:	Highly potent DOT1L inhibitor
Chemical Name:	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
Purity:	≥98% (HPLC)
Molecular Weight:	539.67

View Full Technical Details for EPZ 004777

Technical Data
Citations

Biological Activity for EPZ 004777

EPZ 004777 is a highly potent DOT1L inhibitor (IC₅₀ = 0.4 nM). Exhibits >1000-fold selectivity for DOT1L over a panel of other methyltransferases. Selectively inhibits proliferation and induces apoptosis of MLL-rearranged cells in vitro. Prolongs survival in a MLL xenograft mouse model. Enhances efficiency of Yamanaka-factor factor reprogramming of fibroblasts by 3-4-fold.

For more information about how EPZ 004777 may be used, see our protocol:

Highly Efficient Generation of CiPSCs from MEFs

Licensing Information

Sold under license from Epizyme, Inc.

Compound Libraries for EPZ 004777

EPZ 004777 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Epigenetics Library and Tocriscreen Stem Cell Library. Find out more about compound libraries available from Tocris.

External Portal Information

Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of EPZ004777 is reviewed on the chemical probes website.

Technical Data for EPZ 004777

M. Wt	539.67
Formula	C₂₈H₄₁N₇O₄
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	1338466-77-5
PubChem ID	56962336
InChi Key	WXRGFPHDRFQODR-ICLZECGLSA-N
Smiles	NC1=C2C(N([C@H]3[C@H](O)[C@H](O)[C@@H](CN(CCCNC(NC4=CC=C(C(C)(C)C)C=C4)=O)C(C)C)O3)C=C2)=NC=N1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for EPZ 004777

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	53.97	100
	ethanol	53.97	100

Preparing Stock Solutions for EPZ 004777

The following data is based on the product molecular weight 539.67.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.85 mL	9.26 mL	18.53 mL
5 mM	0.37 mL	1.85 mL	3.71 mL
10 mM	0.19 mL	0.93 mL	1.85 mL
50 mM	0.04 mL	0.19 mL	0.37 mL

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References for EPZ 004777

References are publications that support the biological activity of the product.

Onder Chromatin-modifying enzymes as modulators of reprogramming. Nature 2012 PMID: 22388813
Yu Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors. Nat.Commun. 2012 PMID: 23250418