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EPZ020411 2HCl (1700663-41-7(free base))

Name: EPZ020411 2HCl (1700663-41-7(free base))
Brand: TargetMol
SKU: T4334
Rating: 4.5 (1 reviews)

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Catalog No. T4334

EPZ020411 is an effective and specific small molecule PRMT6 inhibitor (IC50=10 nM).

EPZ020411 2HCl (1700663-41-7(free base))

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Catalog No. T4334

EPZ020411 is an effective and specific small molecule PRMT6 inhibitor (IC50=10 nM).

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$245	Inquiry	Inquiry
5 mg	$428	Inquiry	Inquiry
10 mg	Inquiry	Inquiry	Inquiry
25 mg	Inquiry	Inquiry	Inquiry
1 mL x 10 mM (in DMSO)	Inquiry	Inquiry	Inquiry

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Product Introduction

Bioactivity

Description	EPZ020411 is an effective and specific small molecule PRMT6 inhibitor (IC50=10 nM).
Targets&IC50	PRMT8:223 nM, PRMT1:119 nM, PRMT6:10 nM
In vitro	In A375 human melanoma cells exogenously overexpressing PRMT6,treatment with EPZ020411IC50=0.637±0.241 μM) results in a dose-dependent decrease in H3R2 methylation.
In vivo	Male Sprague-Dawley rats administered a single dose of EPZ020411 (1 mg/kg by i.v.) ,show a moderate clearance (CL) of 19.7±1.0 mL/min/kg, with a volume of distribution at steady state (Vss) of 11.1±1.6 L/kg, translating to a mean terminal half-life (t1/2) of 8.54±1.43 h. At dose of EPZ020411(5 mg/kg s.c.) a good bioavailability of 65.6 ± 4.3% is observed, resulting on EPZ020411 unbound blood concentration remaining above the PRMT6 biochemical IC50 value for more than 12 h.
Cell Research	A375 (CRL-1619) cells are incubated in the presence of increasing concentrations of EPZ020411 up to 20 μM for 48 hours.
Animal Research	Sprague-Dawley rats are treated with EPZ020411(1 mg/kg i.v.) prepared in saline, pH 6.5.

Chemical Properties

Molecular Weight	515.51
Formula	C₂₅H₄₀Cl₂N₄O₃
Smiles	Cl.Cl.CNCCN(C)Cc1c[nH]nc1-c1ccc(O[C@H]2C[C@@H](C2)OCCC2CCOCC2)cc1
Relative Density.	no data available

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

Ethanol: 93 mg/mL (180.4 mM), Sonication is recommended.

DMSO: 93 mg/mL (180.4 mM), Sonication is recommended.

Solution Preparation Table

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	1.9398 mL	9.6991 mL	19.3983 mL	96.9913 mL
5 mM	0.3880 mL	1.9398 mL	3.8797 mL	19.3983 mL
10 mM	0.1940 mL	0.9699 mL	1.9398 mL	9.6991 mL
20 mM	0.0970 mL	0.4850 mL	0.9699 mL	4.8496 mL
50 mM	0.0388 mL	0.1940 mL	0.3880 mL	1.9398 mL
100 mM	0.0194 mL	0.0970 mL	0.1940 mL	0.9699 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

PRMT8PRMT6PRMT1HistoneMethyltransferaseHistone MethyltransferaseEPZ020411 2HCl (1700663-41-7(free base))EPZ-020411 2HCl (1700663-41-7(free base))EPZ020411 2HCl (1700663417(free base))EPZ020411 2HCl (1700663 41 7(free base))

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EPZ020411 2HCl (1700663-41-7(free base))

EPZ020411 2HCl (1700663-41-7(free base))

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Keywords