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EPZ5676

Catalog No.S7062

EPZ-5676 is an S-adenosyl methionine (SAM) competitive inhibitor of protein methyltransferase DOT1L with K_i of 80 pM, demonstrating >37,000-fold selectivity against all other PMTs tested, inhibits H3K79 methylation in tumor. Phase 1.

: Selleck USA Tel: +1-832-582-8158[email protected]

EPZ5676 Chemical Structure
Molecular Weight: 562.71

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From Jan. to Oct. 2013, 610 scientific articles have cited using Selleck products,including many in journals with an impact factor greater than 20.
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Product Information

Compare Histone Methyltransferase Inhibitors

Compare Histone Methyltransferase Inhibitors

Inhibitory Selectivity
Solubility

Cat.No.	Product Name	Solubility (25°C)
Cat.No.	Product Name	Water	DMSO	Ethanol
S8006	BIX 01294	98 mg/mL	98 mg/mL	8 mg/mL
S7004	EPZ005687	<1 mg/mL	2 mg/mL	<1 mg/mL
S7062	EPZ5676	<1 mg/mL	100 mg/mL	100 mg/mL
S3147	Entacapone	<1 mg/mL	61 mg/mL	2 mg/mL
S7164	GSK343	<1 mg/mL	1 mg/mL	4 mg/mL

Research Area
Research Area
Dr. Antonino Maria Sparta demonstrates a breakthrough in leukemia research by utilizing two inhibitors produced by Selleck Chemicals.

Product Description

Biological Activity Protocol Clinical Trial Information Chemical Information Tech Support & FAQs

Biological Activity

Description	EPZ-5676 is an S-adenosyl methionine (SAM) competitive inhibitor of protein methyltransferase DOT1L with K_i of 80 pM, demonstrating >37,000-fold selectivity against all other PMTs tested, inhibits H3K79 methylation in tumor. Phase 1.
Targets	DOT11L
IC50	80 pM K_i
In vitro	EPZ-5676 reduces H3K79 dimethylation with a cellular IC50 of 2.6 nM in MV4-11 cells. EPZ-5676 treatment results in concentration- and time-dependent reduction of H3K79 methylation without effect on the methylation status of other histone sites, which leads to inhibition of key MLL target genes and selective, apoptotic cell killing in MLL-rearranged leukemia cells. EPZ-5676 inhibits proliferation of MLL-AF4 rearranged cell line MV4-11 with an IC50 of 9 nM.
If your cell culture is contaminated by mycoplasma, please use our new product MycoClean™ Mycoplasma Removal Kit (Catalog No. K9000). This is a novel, efficient and safe kit to remove mycoplasma.
In vivo	EPZ-5676 continuously intravenous infusion for 21 days to xenograft model of MLL-rearranged leukemia, leads to dose-dependent anti-tumor activity. At the highest dose of 70.5 mg/kg/day, complete tumor regressions are achieved with no regrowth for up to 32 days after the cessation of treatment. No significant weight loss or obvious toxicity is observed in rats treated with EPZ-5676 during efficacy study.
Features

Protocol(Only for Reference)

References

Clinical Trial Information( data from http://clinicaltrials.gov)

NCT Number	Recruitment	Conditions	Sponsor /Collaborators	Start Date	Phases
NCT01684150	Recruiting	Acute Myeloid Leukemia\|Acute Lymphoblastic Leukemia\|Myelodysplastic Syndrome\|Myeloproliferative Disorders\|Chronic Myeloid Leukemia	Epizyme, Inc.\|Celgene Corporation	2012-09	Phase 1

Chemical Information

Molecular Weight (MW)	562.71
Formula	C₃₀H₄₂N₈O₃
CAS No.	1380288-87-8
Synonyms	N/A

Solubility (25°C) * <1 mg/ml means slightly soluble or insoluble DMSO 100 mg/mL Water <1 mg/mL Ethanol 100 mg/mL
Storage	2 years -20°CPowder
Storage	6 months-80°Cin DMSO

Chemical Name	9H-Purin-6-amine, 9-[5-deoxy-5-[[cis-3-[2-[6-(1,1-dimethylethyl)-1H-benzimidazol-2-yl]ethyl]cyclobutyl](1-methylethyl)amino]-β-D-ribofuranosyl]-

Preparing Stock Solutions

Stock Solution (1ml DMSO)	1mM	10mM	20mM	30mM
Mass(mg)	0.56271	5.6271	11.2542	16.8813

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Research Area

Tech Support & FAQs

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Related Histone Methyltransferase Inhibitors

EPZ005687
EPZ005687 is a potent and selective inhibitor of EZH2 with K_i of 24 nM, 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases.
BIX 01294
BIX01294 is an inhibitor of G9a histone methyltransferase with IC50 of 2.7 μM, reduces H3K9me2 of bulk histones, also weakly inhibits GLP (primarily H3K9me3), no significant activity observed at other histone methyltransferases.
GSK343
GSK343 is a potent, selective EZH2 inhibitor with IC50 of 4 nM, showing 60 fold selectivity against EZH1, and >1000 fold selectivity against other histone methyltransferases.

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EPZ5676