EPZ 004777

Pricing Availability Delivery Time Qty
Cat.No. 5567 - EPZ 004777 | C28H41N7O4 | CAS No. 1338466-77-5
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)
Datasheet
Citations
Literature

Biological Activity

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.

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.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 539.67. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will 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

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Yu et al (2012) Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors. Nat.Commun. 3 1288 PMID: 23250418


If you know of a relevant reference for EPZ 004777, please let us know.

View Related Products by Target

View Related Products by Product Action

View all Lysine Methyltransferase Inhibitors

Keywords: EPZ004777 highly potent DOT1L methyltransferases histones inhibitors inhibits HMTs MLL leukemia mll-rearranged H3K79me Lysine Methyltransferases

Citations for EPZ 004777

Citations are publications that use Tocris products.

Currently there are no citations for EPZ 004777. Do you know of a great paper that uses EPZ 004777 from Tocris? If so please let us know.

Commented out for usability testing

Reviews

TODO: Add Reviews

Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Epigenetics

Epigenetics Scientific Review

Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.

Pathways for EPZ 004777

Protocols

TODO: Add Protocols