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)。

EPZ020411 is an effective and specific small molecule PRMT6 inhibitor (IC50=10 nM).

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.

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.

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

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

T4334

C25H40Cl2N4O3

515.51

EPZ020411 2HCl (1700663-41-7(free base))

DMSO:93 mg/mL (180.4 mM)
Ethanol:93 mg/mL (180.4 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years