EPZ5676

EPZ5676

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Histone Methyltransferase Inhibitors with Unique Features

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

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Cited by 1 publications：

1 customer reviews : in vivo invitation

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Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

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Catalog No.S7062

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

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EPZ5676 Chemical Structure
Molecular Weight: 562.71

Cell Rep,2014, 9(3):1163-70

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Most Potent DOT1L Inhibitor

SGC 0946 DOT1L, IC50=0.3 nM.
FDA-approved HMT Inhibitor

Entacapone Approved by FDA for Parkinson's disease.
Newest HMT Inhibitor

EPZ004777 Potent, selective DOT1L inhibitor with IC50 of 0.4 nM.
Classic HMT Inhibitor

UNC1999 Potent, orally bioavailable and selective inhibitor of EZH2 and EZH1 with IC50 of 2 nM and 45 nM, respectively, showing >1000-fold selectivity over a broad range of epigenetic and non-epigenetic targets.

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Cat.No.	Product Name	Solubility (25°C)
Cat.No.	Product Name	Water	DMSO	Ethanol
S7062	EPZ5676	<1 mg/mL	100 mg/mL	92 mg/mL
S7004	EPZ005687	<1 mg/mL	2 mg/mL	<1 mg/mL
S7164	GSK343	<1 mg/mL	<1 mg/mL	4 mg/mL
S8006	BIX 01294	98 mg/mL	98 mg/mL	8 mg/mL
S7128	Tazemetostat (EPZ-6438)	<1 mg/mL	4 mg/mL	<1 mg/mL
S7120	3-deazaneplanocin A (DZNeP) HCl	52 mg/mL	52 mg/mL	<1 mg/mL
S7165	UNC1999	<1 mg/mL	100 mg/mL	100 mg/mL
S7265	MM-102	100 mg/mL	100 mg/mL	100 mg/mL
S7079	SGC 0946	<1 mg/mL	100 mg/mL	100 mg/mL
S3147	Entacapone	<1 mg/mL	61 mg/mL	2 mg/mL
S7616	CPI-169	<1 mg/mL	100 mg/mL	100 mg/mL
S7353	EPZ004777	<1 mg/mL	100 mg/mL	100 mg/mL
S7294	PFI-2	4 mg/mL	99 mg/mL	66 mg/mL
S7619	MI-3 (Menin-MLL Inhibitor)	<1 mg/mL	19 mg/mL	19 mg/mL
S7618	MI-2 (Menin-MLL Inhibitor)	<1 mg/mL	75 mg/mL	75 mg/mL
S7610	UNC0631	<1 mg/mL	100 mg/mL	5 mg/mL
S7611	EI1	<1 mg/mL	42 mg/mL	<1 mg/mL
S7591	BRD4770	<1 mg/mL	27 mg/mL	<1 mg/mL
S7570	UNC0379	<1 mg/mL	82 mg/mL
S7061	GSK126	<1 mg/mL	3 mg/mL	<1 mg/mL
S7748	EPZ015666	<1 mg/mL	60 mg/mL	48 mg/mL
S7884	AMI-1	10 mg/mL	100 mg/mL	<1 mg/mL
S7804	GSK503	<1 mg/mL	100 mg/mL	26 mg/mL
S7656	CPI-360	<1 mg/mL	20 mg/mL	18 mg/mL
S7832	SGC707	<1 mg/mL	59 mg/mL	59 mg/mL

Research Area
Research Area

Biological Activity Clinical Trial Information Chemical Information FAQ Tech Support

Species	Mouse	Rat	Rabbit	Guinea pig	Hamster	Dog
Weight (kg)	0.02	0.15	1.8	0.4	0.08	10
Body Surface Area (m²)	0.007	0.025	0.15	0.05	0.02	0.5
K_m factor	3	6	12	8	5	20

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B K_m
	Animal A K_m

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the K_m factor for a mouse and then divide by the K_m factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×	mouse K_m(3)	= 11.2 mg/kg
	rat K_m(6)

[1] Robert A. Protein methyltransferases in cancer. AACR Annual Meeting, 2013.

[2] Pollock RM, 54th ASH Annual Meeting and Exposition, 2012, Abst 2379

NCT Number	Recruitment	Conditions	Sponsor /Collaborators	Start Date	Phases
NCT02141828	Active, not recruiting	Leukemia\|Acute Myeloid Leukemia\|Acute Lymphocytic Leukemia\|Acute Leukemias	Epizyme, Inc.\|Celgene Corporation	May 2014	Phase 1
NCT01684150	Active, not recruiting	Acute Myeloid Leukemia\|Acute Lymphoblastic Leukemia\|Myelodysplastic Syndrome\|Myeloproliferative Disorders	Epizyme, Inc.\|Celgene Corporation	September 2012	Phase 1

Download EPZ5676 SDF

Molecular Weight (MW)	562.71
Formula	C₃₀H₄₂N₈O₃
CAS No.	1380288-87-8

Storage	3 years -20℃powder
Storage	6 months-80℃in solvent
Synonyms	N/A

Solubility (25°C) *	In vitro	DMSO	100 mg/mL warming (177.71 mM)
		Ethanol	92 mg/mL warming (163.49 mM)
		Water	<1 mg/mL (<1 mM)
	In vivo	2% DMSO+30% PEG 300+5% Tween 80+ddH2O	5mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

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]-

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Question 1
Is the vehicle 30% PEG400/0.5% Tween80/5% propylene glycol recommended for in vivo use?

Answer: S7062 EPZ-5676 in 30% PEG400/0.5% Tween80/5% propylene glycol at 30 mg/ml is a suspension. For injection, 2% DMSO/30% PEG 300/5% Tween 80/ddH2O at 5 mg/ml is suitable.

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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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Description

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

DOT1L ^[1]
(Cell-free assay)

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.

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.