EPZ 004777

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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
Reviews
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.

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

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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


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View Related Products by Product Action

View all Other Lysine Methyltransferase Inhibitors

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Citations for EPZ 004777

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Literature in this Area

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