EPZ 004777

Cat. No. 5567

EPZ 004777 C28H41N7O4 [1338466-77-5]

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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

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
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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

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.

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Keywords: EPZ 004777, supplier, EPZ004777, highly, potent, DOT1L, methyltransferases, histones, inhibitors, inhibits, HMTs, MLL, leukemia, mll-rearranged, H3K79me, Tocris Bioscience, Lysine Methyltransferase Inhibitor products

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