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EPZ020411

Catalog No.GC15102

PRMT6 inhibitor

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EPZ020411 Chemical Structure

Cas No.: 1700663-41-7

Size Price Stock Qty
1mg
$57.00
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5mg
$255.00
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10mg
$448.00
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25mg
$981.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

IC50: 10 nM

EPZ020411 is an inhibitor of PRMT6.

PRMT6, a member of the protein arginine methyltransferasefamily, comprises 45 enzymes. The post-translational modifications of PRMT6 are important regulators of RNA processing, transcriptional regulation, and signal transduction.

In vitro: In biochemical assays, EPZ020411 was found to be over 100-fold selective for PRMT6/8/1 compared to other histone methyltransferases, such as PRMT3, PRMT4, PRMT5 and PRMT7. In addition, EPZ020411 treatment led to a dose-dependent decrease in H3R2 methylation, while treatment with its PRMT6-inactive analog did not generate an IC50 at concentrations up to 20 μM [1].

In vivo: Animal study found that male SD rats i.v. administered a single dose of EPZ020411 at 1 mg/kg showed a moderate clearance of 19.7 mL/min/kg, with a volume of distribution at steady state of 11.1 L/kg, and a mean terminal half-life of 8.54 h. Following 5 mg/kg s.c. dosing, a good bioavailability of 65.6 was observed, resulting in EPZ020411 unbound concentration remaining over the PRMT6 IC50 for more than 12 h [1].

Clinical trial: Up to now, EPZ020411 is still in the preclinical development stage.

Reference:
[1] Mitchell LH, et al.  Aryl Pyrazoles as Potent Inhibitors of Arginine Methyltransferases: Identification of the First PRMT6 ToolCompound. ACS Med Chem Lett. 2015 Apr 6;6(6):655-659.

Chemical Properties

Cas No. 1700663-41-7 SDF
Chemical Name N1,N2-dimethyl-N1-((3-(4-((1r,3r)-3-(2-(tetrahydro-2H-pyran-4-yl)ethoxy)cyclobutoxy)phenyl)-1H-pyrazol-4-yl)methyl)ethane-1,2-diamine
Canonical SMILES CN(CC1=CNN=C1C2=CC=C(O[C@@H]3C[C@@H](OCCC4CCOCC4)C3)C=C2)CCNC
Formula C25H38N4O3 M.Wt 442.59
Solubility DMF: 1 mg/ml,DMSO: 5 mg/ml,Ethanol: 1 mg/ml,PBS (pH 7.2): 0.3 mg/ml Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.2594 mL 11.2971 mL 22.5943 mL
5 mM 0.4519 mL 2.2594 mL 4.5189 mL
10 mM 0.2259 mL 1.1297 mL 2.2594 mL
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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.
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3. All of the above co-solvents are available for purchase on the GlpBio website.

Reviews

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Average Rating: 5 ★★★★★ (Based on Reviews and 29 reference(s) in Google Scholar.)

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