EPZ031686 是一种有效的 SMYD3 抑制剂，IC50 为 3 nM，可用于癌症研究。

EPZ031686 is an effective inhibitor of SMYD3 inhibitor with an IC50 of 3 nM and can be used in studies about cancer.

In male CD-1 mice, EPZ031686 (1 mg/kg; i.v.) shows a moderate clearance (CL) of 27 ± 3.9 mL/min/kg, in very good agreement with the mouse microsomal data, with a volume of distribution at steady state (Vss) of 2.3 ± 0.29 L/kg, translating to a mean terminal half-life (t1/2) of 1.7 ± 0.13 h. After the treatment of EPZ031686 (5 and 50 mg/kg; p.o.), both Cmax and AUC0-last increased in a slightly higher than dose-proportional manner, while t1/2 remained unchanged. Bioavailability (F) of 48 ± 5.4% and 69 ± 8.2%, respectively, leading to EPZ031686 unbound blood concentration remaining above the SMYD3 ICW IC50 value for more than 12 h after a 50 mg/kg p.o.[1].

1808011-22-4

C26H34ClF3N4O4S

591.09

EPZ-031686

DMSO:30 mg/mL (50.8 mM),ultrasonic and warming and heat to 60°C
Powder: -20°C for 3 years
In solvent: -80°C for 2 years