Pemrametostat (GSK3326595)

Catalog No.S8664 Synonyms: EPZ015938

For research use only.

Pemrametostat (GSK3326595, EPZ015938) is an orally active, potent and selective inhibitor of protein arginine methyltransferase 5 (PRMT5) and potently inhibits tumor growth in vitro and in vivo in animal models.

Pemrametostat (GSK3326595) Chemical Structure

CAS No. 1616392-22-3

Selleck's Pemrametostat (GSK3326595) has been cited by 5 Publications

Purity & Quality Control

Choose Selective Histone Methyltransferase Inhibitors

Biological Activity

Description Pemrametostat (GSK3326595, EPZ015938) is an orally active, potent and selective inhibitor of protein arginine methyltransferase 5 (PRMT5) and potently inhibits tumor growth in vitro and in vivo in animal models.
Targets
PRMT5 [1]
()
Assay
Methods Test Index PMID
Western blot H4R3me2s ; MDM4 31439820

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 90 mg/mL
(198.87 mM)
Water Insoluble
Ethanol '90 mg/mL

Chemical Information

Molecular Weight 452.55
Formula

C24H32N6O3

CAS No. 1616392-22-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(=O)N1CCC(CC1)NC2=NC=NC(=C2)C(=O)NCC(CN3CCC4=CC=CC=C4C3)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

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04676516 Not yet recruiting Drug: GSK3326595 Breast Cancer Ottawa Hospital Research Institute|Ontario Institute for Cancer Research|GlaxoSmithKline|London Regional Cancer Program Canada|Hamilton Health Sciences Corporation March 21 2021 Phase 2
NCT03614728 Recruiting Drug: GSK3326595|Drug: 5-Azacitidine Neoplasms GlaxoSmithKline October 16 2018 Phase 1|Phase 2
NCT02783300 Recruiting Drug: GSK3326595|Drug: Pembrolizumab Neoplasms GlaxoSmithKline August 30 2016 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Pemrametostat (GSK3326595) | Pemrametostat (GSK3326595) supplier | purchase Pemrametostat (GSK3326595) | Pemrametostat (GSK3326595) cost | Pemrametostat (GSK3326595) manufacturer | order Pemrametostat (GSK3326595) | Pemrametostat (GSK3326595) distributor