EPZ 004777
Tocris Bioscience, part of Bio-Techne | Catalog # 5567
Highly potent DOT1L inhibitor
Key Product Details
Description
Highly potent DOT1L inhibitor
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
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.
| 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
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
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
Product Specific Notices for EPZ 004777
For research use only
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