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PRT543 PRMT inhibitor

Name: PRT543
Brand: Selleck Chemicals
SKU: E1658
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.E1658

PRT543 is a potent and selective inhibitor of protein arginine methyltransferase 5 (PRMT5) with broad antitumor activity in vitro and in vivo. It also inhibits the methyltransferase activity of the PRMT5/MEP50 complex with an IC50 of 10.8 nM.

Chemical Structure

Molecular Weight: 376.79

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Quality Control

Batch: E165801 DMSO]75 mg/mL]false]Ethanol]75 mg/mL]false]Water]Insoluble]false Purity: 99.42%

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS
Datasheet

99.42

Related Targets	HDAC JAK BET Histone Methyltransferase PKC PARP HIF EZH2 AMPK Histone Acetyltransferase
Other PRMT Inhibitors	Pemrametostat (GSK3326595) LLY-283 Ralometostat (TNG908) C7280948 GSK3368715 3HCl TC-E 5003 BRD0639 Furamidine dihydrochloride LLY-284 TNG-462

Solubility

In vitro
Batch:

DMSO : 75 mg/mL (199.04 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 75 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.
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.	3.750mg/ml (9.95mM)	Taking the 1 mL working solution as an example, add 50 μL of 75 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.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.450mg/ml (1.19mM)	Taking the 1 mL working solution as an example, add 50 μL of 9 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. 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	376.79	Formula	C₁₇H₁₇ClN₄O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1989620-03-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Mechanism of Action

Targets/IC₅₀/Ki	PRMT5 PRMT5/MEP50 complex 10.8 nM
References	[1] https://aacrjournals.org/cancerres/article/80/16_Supplement/2915/642172/Abstract-2915-Preclinical-characterization-of

Clinical Trial Information

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

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03886831	Completed	Relapsed/Refractory Advanced Solid Tumors\|Relapsed/Refractory Diffuse Large B-cell Lymphoma\|Relapsed/Refractory Myelodysplasia\|Relapsed/Refractory Myelofibrosis\|Adenoid Cystic Carcinoma\|Relapsed/Refractory Mantle Cell Lymphoma\|Relapsed/Refractory Acute Myeloid Leukemia\|Refractory Chronic Myelomonocytic Leukemia	Prelude Therapeutics	February 11 2019	Phase 1

Tech Support

Handling Instructions

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