EPZ020411 hydrochloride_2070015-25-5；1700663-41-7(freebase)_Absin
产品信息
抗原名称
PRMT6,PRMT1,PRMT8
商品描述
EPZ020411 is a potent and selective inhibitor of PRMT6 with IC50 of 10 nM, has ＞10 fold selectivity for PRMT6 over PRMT1 and PRMT8.
分子量
479.06
纯度
>98%
可溶性
DMSO : 50 mg/mL (104.37 mM; Need ultrasonic)
H2O : ≥ 41 mg/mL (85.58 mM)
H2O : ≥ 41 mg/mL (85.58 mM)
外观
Powder
In vitro(体外研究)
Treatment with EPZ020411 results in a dose-dependent decrease in H3R2 methylation in A375 human melanoma cells exogenously overexpressing PRMT6(IC50=0.637±0.241 μM). In biochemical assays EPZ020411 is over 100-fold selective for PRMT6/8/1 compared to other histone methyltransferases including four arginine methyltransferases (PRMT3, PRMT4, PRMT5, and PRMT7). The compound shows poor permeability in the parallel artificial membrane permeation assay.
In vivo(体内研究)
EPZ020411 shows good bioavailability following subcutaneous dosing in rats making it a suitable tool for in vivo studies. Male Sprague-Dawley rats administered a single dose of EPZ020411 at 1 mg/kg by i.v. bolus show a moderate clearance (CL) of 19.7±1.0 mL/min/kg, with a volume of distribution at steady state (Vss) of 11.1±1.6 L/kg, translating to a mean terminal half-life (t1/2) of 8.54±1.43 h. Following 5 mg/kg s.c. dosing, a good bioavailability of 65.6 ± 4.3% is observed, leading to EPZ020411 unbound blood concentration remaining above the PRMT6 biochemical IC50 value for more than 12 h.
背景
别名
EPZ 020411,EPZ-020411
分子式
C25H38N4O3·HCl
CAS号
2070015-25-5；1700663-41-7(freebase)
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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