EPZ020411 hydrochloride
目录号: PL15060 纯度: ≥97%
CAS No. :2070015-25-5
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中文名称
EPZ020411 hydrochloride
英文名称
EPZ020411 hydrochloride
英文别名
EPZ020411 hydrochloride;EPZ020411 HCl;EPZ020411 (hydrochloride);BCP29979;N,N'-dimethyl-N'-[[5-[4-[3-[2-(oxan-4-yl)ethoxy]cyclobutyl]oxyphenyl]-1H-pyrazol-4-yl]methyl]ethane-1,2-diamine;hydrochloride;N1,N2-Dimethyl-N1-((3-(4-(3-(2-(tetrahydro-2H-pyran-4-yl)ethoxy)cyclobutoxy)phenyl)-1H-pyrazol-4-yl)methyl)ethane-1,2-diamine hydrochloride
Cas No.
2070015-25-5
分子式
C25H39ClN4O3
分子量
479.06
包装储存
4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
产品详情
EPZ020411 hydrochloride 是一种选择性的 PRMT6 抑制剂,其 IC50 值为 10 nM,比作用于 PRMT1 和 PRMT8 选择性高 10 倍多。EPZ020411 hydrochloride 可用于癌症的研究。
生物活性
EPZ020411 hydrochloride is a selective inhibitor of PRMT6 with an IC 50 of 10 nM, it has >10 folds selectivity for PRMT6 over PRMT1 and PRMT8. EPZ020411 hydrochloride can be used for the research of cancer.
性状
Solid
IC50 & Target[1][2]
PRMT6 0.01 μM (IC50) PRMT1 0.119 μM (IC
体外研究(In Vitro)
EPZ020411 hydrochloride (0-20 μM; 24 h) decreases H3R2 methylation in A375 cells.
EPZ020411 hydrochloride (20-40 μM; 6 h) reduces neomycin- and cisplatin-induced cell apoptosis and increases hair cell survival. has not independently confirmed the accuracy of these methods. They are for reference only.Western Blot Analysis
体内研究(In Vivo)
EPZ020411 hydrochloride (10 mg/kg; i.p. once) reduces neomycin- and cisplatin-induced hearing loss in C57BL/6J wild-type mice with acute ototoxicity model.
1.19 Pharmacokinetic Parameters of EPZ020411 hydrochloride in rats.
Rats
IV 1 mg/kg
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
参考文献
[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.
[2]. He Y, et al. Inhibition of Protein arginine methyltransferase 6 reduces reactive oxygen species production and attenuates aminoglycoside- and cisplatin-induced hair cell death. Theranostics. 2020 Jan 1;10(1):133-150.
溶解度数据
In Vitro: 0.1 M HCL : 50 mg/mL (104.37 mM; ultrasonic and warming and adjust pH to 2 with HCl and heat to 60°C)DMSO : 50 mg/mL (104.37 mM; Need ultrasonic)H2O : 20 mg/mL (41.75 mM; ultrasonic and warming and heat to 60°C)
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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