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EPZ020411
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
EPZ020411图片
CAS NO:1700663-41-7
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
EPZ020411 是一种选择性的 PRMT6 抑制剂,IC50 为 10 nM,对 PRMT6 的选择性是 PRMT1 和 PRMT8 的 10 倍以上。 EPZ020411可用于癌症研究。
Cas No.1700663-41-7
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 SMILESCN(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
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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.