EPZ 004777

Tocris Bioscience | Catalog # 5567

Highly potent DOT1L inhibitor
Tocris Bioscience

Key Product Details

Description

Highly potent DOT1L inhibitor
View all Lysine Methyltransferase Inhibitors »

Product Description

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. Enables generation of Chemically Induced Pluripotent Stem Cells (CiPSCs) from mouse embryonic fibroblasts (MEFs) (see protocol below).

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.

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.

Product Specifications for EPZ 004777

Molecular Weight

539.67

Formula

C28H41N7O4

Storage

Store at -20°C

Purity

≥98% (HPLC)

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

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.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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

Calculators

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Background References

References are publications that support the biological activity of the product. See our Citations tab to view 8 publications citing the usage of this product.

Product Documents for EPZ 004777

Certificate of Analysis

To download a Certificate of Analysis, please enter a lot or batch number in the search box below.

Product Specific Notices for EPZ 004777

For research use only

Related Research Areas

Epigenetics

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