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GSK3368715 dihydrochloride

Name: GSK3368715 dihydrochloride
Brand: TargetMol
SKU: T11500L
Price: 98 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T11500LCas No. 1628925-77-8

Alias GSK3368715 2HCl, EPZ019997 dihydrochloride, EPZ019997 2HCl

GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) is an orally active and potent inhibitor of type I protein arginine methyltransferases (PRMTs), including PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8. It exhibits anticancer and antitumor activity and can be used to study advanced solid tumors.

GSK3368715 dihydrochloride

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Purity: 99.66%

Catalog No. T11500LAlias GSK3368715 2HCl, EPZ019997 dihydrochloride, EPZ019997 2HClCas No. 1628925-77-8

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
1 mg	$98	In Stock	In Stock
5 mg	Preferential	In Stock	In Stock

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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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Purity:99.66%

Appearance:Solid

Color:White

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COA LCMS

Product Introduction

Bioactivity

Description	GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) is an orally active and potent inhibitor of type I protein arginine methyltransferases (PRMTs), including PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8. It exhibits anticancer and antitumor activity and can be used to study advanced solid tumors.
Targets&IC50	PRMT3:48 nM, PRMT1:3.1 nM, PRMT6:5.7 nM, PRMT4:1148 nM, PRMT8:1.7 nM
In vitro	In the majority of 249 cancer cell lines representing 12 tumor types, GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) exhibits 50% or more growth inhibition relative to DMSO-treated cells[1].
In vivo	GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) markedly inhibits the growth of BxPC3 xenografts at all tested doses, achieving tumor growth reductions of 78% and 97% at 150 mg/kg and 300 mg/kg, respectively[1].
Synonyms	GSK3368715 2HCl, EPZ019997 dihydrochloride, EPZ019997 2HCl

Chemical Properties

Molecular Weight	439.46
Formula	C₂₀H₄₀Cl₂N₄O₂
Cas No.	1628925-77-8
Smiles	Cl.Cl.CCOCC1(COCC)CCC(CC1)c1n[nH]cc1CN(C)CCNC
Relative Density.	no data available

Storage & Solubility Information

Storage

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

Solubility Information

H2O: 100 mg/mL (227.55 mM), Sonication is recommended.

DMSO: 100 mg/mL (227.55 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (9.1 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

H2O/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.2755 mL	11.3776 mL	22.7552 mL	113.7760 mL
5 mM	0.4551 mL	2.2755 mL	4.5510 mL	22.7552 mL
10 mM	0.2276 mL	1.1378 mL	2.2755 mL	11.3776 mL
20 mM	0.1138 mL	0.5689 mL	1.1378 mL	5.6888 mL
50 mM	0.0455 mL	0.2276 mL	0.4551 mL	2.2755 mL
100 mM	0.0228 mL	0.1138 mL	0.2276 mL	1.1378 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