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Pemrametostat (GSK3326595) PRMT5 Inhibitor

Name: Pemrametostat (GSK3326595)
Brand: Selleck Chemicals
SKU: S8664
Availability: InStock
Rating: 5 (22 reviews)

Cat.No.S8664

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.

Chemical Structure

Molecular Weight: 452.55

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Quality Control

Batch: Purity: 99.85%

99.85

Products Often Used Together with Pemrametostat (GSK3326595)

Santacruzamate A (CAY10683)

Treatments with this compound and Santacruzamate A rescue the ZEB2-mediated E-cadherin promoter suppression in SW480-ZEB2 cells.

Related Targets	HDAC JAK BET Histone Methyltransferase PKC PARP HIF EZH2 AMPK Histone Acetyltransferase
Other PRMT Products	LLY-283 Ralometostat (TNG908) C7280948 GSK3368715 3HCl TC-E 5003 BRD0639 Furamidine dihydrochloride PRMT5 Antibody [N4N24] LLY-284 TNG-462

Solubility

In vitro
Batch:

DMSO : 91 mg/mL (201.08 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 32 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.550mg/ml (10.05mM)	Taking the 1 mL working solution as an example, add 50 μL of 91 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

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.

Chemical Information, Storage & Stability

Molecular Weight	452.55	Formula	C₂₄H₃₂N₆O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1616392-22-3	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	EPZ015938			Smiles	CC(=O)N1CCC(CC1)NC2=NC=NC(=C2)C(=O)NCC(CN3CCC4=CC=CC=C4C3)O

Mechanism of Action

Targets/IC₅₀/Ki	PRMT5
In vitro	In SW480-ZEB2 cells, Pemrametostat (GSK3326595) and Santacruzamate A treatments both rescue the ZEB2-mediated E-cadherin promoter suppression, confirming that the ZEB2-mediated repression of E-cadherin in CRC cells is facilitated by PRMT5 and HDAC2.
In vivo	Pemrametostat (GSK3326595) reduces liver metastasis of CRC cells and completely inhibits the distant metastasis of SW620 cells in nude mice.
References	[1] https://pubmed.ncbi.nlm.nih.gov/28067760/ [2] https://pubmed.ncbi.nlm.nih.gov/35884488/

Applications

Methods	Biomarkers	Images	PMID
Western blot	H4R3me2s MDM4		31439820

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04676516	Completed	Breast Cancer	Ottawa Hospital Research Institute\|Ontario Institute for Cancer Research\|GlaxoSmithKline\|London Regional Cancer Program Canada\|Hamilton Health Sciences Corporation	June 8 2021	Phase 2
NCT03614728	Terminated	Neoplasms	GlaxoSmithKline	October 16 2018	Phase 1\|Phase 2
NCT02783300	Completed	Neoplasms	GlaxoSmithKline	August 30 2016	Phase 1

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Handling Instructions

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