EPZ015666 (GSK3235025)

Catalog No.S7748

For research use only.

EPZ015666 (GSK3235025) is a potent, selective and orally bioavailable PRMT5 inhibitor with Ki of 5 nM, >20,000-fold selectivity over other PMTs.

EPZ015666 (GSK3235025) Chemical Structure

CAS No. 1616391-65-1

Selleck's EPZ015666 (GSK3235025) has been cited by 17 publications

Purity & Quality Control

Choose Selective Histone Methyltransferase Inhibitors

Biological Activity

Description EPZ015666 (GSK3235025) is a potent, selective and orally bioavailable PRMT5 inhibitor with Ki of 5 nM, >20,000-fold selectivity over other PMTs.
Targets
PRMT5 [1]
(Cell-free assay)
5 nM(Ki)
In vitro

EPZ015666 shows potent cellular activity that blocks symmetric dimethylation of SmD3 and inhibit proliferation of MCL cell lines (Z-138, Granta-519, Maver-1, Mino, and Jeko-1) with IC50 of 96-904 nM. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MDA-MB-468 NGHXd3lHfW6ldHnvckBie3OjeR?= NIG4Z5M1QCCq NGrnb5FqdmirYnn0d{BRWk2WNTDhZ5Rqfmm2eR?= NEXrTZU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEm1O|k5QCd-M{C5OVc6QDh:L3G+
HCC1954 NXm0d2tPS2WubDD2bYFjcWyrdImgZZN{[Xl? NGjEb|VKSzVyPUCuPEDPxE1? NEH5NpM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEm1O|k5QCd-M{C5OVc6QDh:L3G+
MDA-MB-453 MlPiR4VtdCC4aXHibYxqfHliYYPzZZk> NEPYXYdKSzVyPUGg{txO MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODl3N{m4PEc,OzB7NUe5PFg9N2F-
HCC38 NVXqfXh{S2WubDD2bYFjcWyrdImgZZN{[Xl? NITkR2RKSzVyPUKuNkDPxE1? MljrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB7NUe5PFgoRjNyOUW3PVg5RC:jPh?=
MDA-MB-468 MnPSR4VtdCC4aXHibYxqfHliYYPzZZk> MoXwTWM2OD1{LkKg{txO NHXncFQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEm1O|k5QCd-M{C5OVc6QDh:L3G+
MCF7 MkPaR4VtdCC4aXHibYxqfHliYYPzZZk> M4DDRmlEPTB;Mj62JO69VQ>? MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODl3N{m4PEc,OzB7NUe5PFg9N2F-
SKBR3 NUD1Z4x1S2WubDD2bYFjcWyrdImgZZN{[Xl? MX3JR|UxRTNwOTFOwG0> NUK0XHk4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C5OVc6QDhpPkOwPVU4QTh6PD;hQi=>
Sf9 NFnlTVlHfW6ldHnvckBie3OjeR?= NXLrXYQ4UW6qaXLpeIlwdiCxZjDmeYxtKGynbnf0bEBz\WOxbXLpcoFvfCCqdX3hckBHVEGJLYTh[4dm\CCSUl3UOU9nfWyuIHzlcod1cCC{ZXPvcYJqdmGwdDDoeY1idiCKaYO2MZRi\2enZDDNSXA2OCCneIDy[ZN{\WRiaX6gZoFkfWyxdnnyeZMhcW6oZXP0[YQhW2Z7IHnud4VkfCClZXzsd{B2e2mwZzDibY91cW67bHH0[YQhcGm|dH;u[UBx\XC2aXTlJIF{KHO3YoP0doF1\SCrbjDwdoV{\W6lZTDv[kBcO0ifLWPBUUBjgSCWb4Djc5VvfCCvZYToc4QtKEmFNUC9NE4xOjMQvF2= NYPRR3F6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm2Nlg{OjZpPkK5OlI5OzJ4PD;hQi=>
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Assay
Methods Test Index PMID
Western blot PRMT5 / H3R8me2s ; H4R3me2s 30957988 28945229
Immunofluorescence IKKβ 29158558
Growth inhibition assay Cell viability 30957988
In vivo EPZ015666 (200 mg/kg, p.o.) displays robust anti-tumor activity in MCL xenograft animal models. [1]

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: MCL cell lines (Z-138, Granta-519, Maver-1, Mino, and Jeko-1)
  • Concentrations: 5 μM
  • Incubation Time: 12 days
  • Method:

    --

  • (Only for Reference)
Animal Research:

[1]

  • Animal Models: MCL (Z-138, and Maver-1) xenograft models
  • Dosages: 200 mg/kg BID
  • Administration: p.o.
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 60 mg/mL warmed
(156.47 mM)
Water Insoluble
Ethanol '48 mg/mL warmed

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing.

5mg/mL

* 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 Information

Molecular Weight 383.44
Formula

C20H25N5O3

CAS No. 1616391-65-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CN(CC2=CC=CC=C21)CC(CNC(=O)C3=CC(=NC=N3)NC4COC4)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

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
If you have any other enquiries, please leave a message.

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Frequently Asked Questions

Question 1:
I want to use this compound for injection, how to reconstitute it?

Answer:
S7748, EPZ015666 is a clear solution in 2% DMSO+30% PEG300+68% water and it can be used for tail vein injection.

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