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EPZ020411 Sale

目录号 : GC15102

A PRMT6 inhibitor

EPZ020411 Chemical Structure

Cas No.:1700663-41-7

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1mg
¥574.00
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5mg
¥2,548.00
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10mg
¥4,480.00
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25mg
¥9,814.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

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产品描述

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
化学名 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
分子式 C25H38N4O3 分子量 442.59
溶解度 DMF: 1 mg/ml,DMSO: 5 mg/ml,Ethanol: 1 mg/ml,PBS (pH 7.2): 0.3 mg/ml 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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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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