Lirametostat (CPI-1205)

InformationLirametostat (CPI-1205) Lirametostat (CPI-1205) is an orally available selective inhibitor of the histone lysine methyltransferase EZH2 with IC50 values of 2 nM and 52 nM for EZH2 and EZH1 respectively. It has potential antineoplastic activity.In vitroTreatment with EZH2 inhibitor CPI-1205 cause apoptosis in multiple myeloma and plasmacytoma cell models.In vivoCPI-1205 shows excellent oral bioavailability. It was well-tolerated for repeat dosing as demonstrated by the absence of significant body weight loss. CPI-1205 shows relatively high clearance in both rats and dogs (3.19 L/h/kg and 1.41 L/h/kg, respectively) but demonstrates good oral bioavailability in both species(44.6% F in rats and 46.2% F in dogs). CPI-1205 was well-tolerated in the 28-day GLP toxicology studies, and any findings were reversible over the recovery period.Cell Datacell lines：Concentrations：Incubation Time：Powder Purity:≥99%. Specification: 10mM in DMSO Molecular Formula: C27H33F3N4O3 Molecular Weight: 518.57