EPZ 004777

Catalog # Availability Size / Price Qty
5567/10
Cat.No. 5567 - EPZ 004777 | C28H41N7O4 | CAS No. 1338466-77-5
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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%

Product Details
Reviews

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.

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
Solubility:
Soluble to 100 mM in DMSO and to 100 mM in ethanol
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
1338466-77-5

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.

Additional Information

Licensing Caveats:
Sold under license from Epizyme, Inc.

Background References

  1. Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors.
    Yu et al.
    Nat.Commun., 2012;3:1288

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