化合物EPZ020411 2HCl T4334

Product Introduction
Bioactivity


英文名: EPZ020411 2HCl (1700663-41-7(free base))

描述: EPZ020411 2HCl (1700663-41-7(free base)) 是一种有效且特异性的小分子 PRMT6 抑制剂 (IC50=10 nM)。

细胞实验: A375 (CRL-1619) cells are incubated in the presence of increasing concentrations of EPZ020411 up to 20 μM for 48 hours.

动物实验: Sprague-Dawley rats are treated with EPZ020411(1 mg/kg i.v.) prepared in saline, pH 6.5.

体外活性: In A375 human melanoma cells exogenously overexpressing PRMT6,treatment with EPZ020411IC50=0.637±0.241 μM) results in a dose-dependent decrease in H3R2 methylation.

体内活性: Male Sprague-Dawley rats administered a single dose of EPZ020411 (1 mg/kg by i.v.) ,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. At dose of EPZ020411(5 mg/kg s.c.) a good bioavailability of 65.6 ± 4.3% is observed, resulting on EPZ020411 unbound blood concentration remaining above the PRMT6 biochemical IC50 value for more than 12 h.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : 93 mg/mL (180.4 mM)
DMSO : 93 mg/mL (180.4 mM)


关键字: EPZ020411 2HCl (1700663-41-7(free base)) | EPZ020411 2HCl (1700663417(free base)) | EPZ020411 2HCl (1700663 41 7(free base)) | EPZ-020411 2HCl (1700663-41-7(free base))

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