CPI360是一种选择性EZH2抑制剂，作用于wt EZH2 和 Y641N EZH2时，IC50分别为0.5 nM和2.5 nM。

CPI-360 is a potent, selective, and SAM-competitive EZH1 inhibitor with IC50 of 102.3 nM, >100-fold selectivity over other methyltransferases.

In KARPAS-422 cells, CPI-360 potently reduces global H3K27me3 and H3K27me2 levels with EC50 of 56 nM and 65 nM, respectively. CPI-360 also causes time-dependent transcriptional changes, and affects the viability of Y641N mutant EZH2-containing KARPAS-422 cells. In addition, CPI-360 gradually arrests KARPAS-422 cells in the G1 cell cycle stage followed by the induction of apoptosis. [1]

In mice bearing KARPAS-422 xenografts, CPI-360 (200 mg/kg, s.c.) reduces tumor growth by 44%. [1]

1802175-06-9

C25H31N3O4

437.54

CPI 360;CPI360

Ethanol:15 mg/mL (34.3 mM)
H2O:<1 mgml
DMSO:16 mg/mL (36.6 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years