CPI 360 Chemical Properties

Boiling point:

712.2±60.0 °C(Predicted)

Density 

1.26±0.1 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMF: 10 mg/mL; DMSO: 25 mg/mL; Ethanol: 30 mg/mL; Ethanol:PBS (pH7.2) (1:7): 0.12 mg/mL

form 

A crystalline solid

pka

11.01±0.10(Predicted)

InChIKey

PFPSFENQCNMITC-MRXNPFEDSA-N

SMILES

N1([C@@H](C2CCOCC2)C)C2=C(C=CC=C2)C(C(NCC2=C(OC)C=C(C)NC2=O)=O)=C1C

CPI 360 Usage And Synthesis

Description

CPI-360 is a selective EZH2 inhibitor with IC₅₀ values of 0.5 and 2.5 nM for wild-type EZH2 and Y641N mutant EZH2, respectively. It decreases cellular levels of H3K27me3 and H3K27me2 (EC₅₀s = 56 and 65 nM, respectively), triggering cell cycle arrest and ultimately resulting in apoptosis in a large panel of non-Hodgkin’s lymphoma (NHL) cell lines. Twice daily, subcutaneous administration of 200 mg/kg of CPI-360 reduced tumor growth of KARPAS-422 xenografts in mice.