CPI-360

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.Formal Name: N-[(1,2-dihydro-4-methoxy-6-methyl-2-oxo-3-pyridinyl)methyl]-2-methyl-1-[(1R)-1-(tetrahydro-2H-pyran-4-yl)ethyl]-1H-indole-3-carboxamide. CAS Number: 1802175-06-9. Molecular Formula: C25H31N3O4. Formula Weight: 437.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/mL, DMSO: 25 mg/mL, Ethanol: 30 mg/mL, Ethanol:PBS (pH7.2) (1:7): 0.12 mg/mL. lambdamax: 212, 292 nm. SMILES: CC(N1)=CC(OC)=C(CNC(C2=C(C)N([C@H](C)C3CCOCC3)C4=C2C=CC=C4)=O)C1=O. InChi Code: InChI=1S/C25H31N3O4/c1-15-13-22(31-4)20(24(29)27-15)14-26-25(30)23-17(3)28(21-8-6-5-7-19(21)23)16(2)18-9-11-32-12-10-18/h5-8,13,16,18H,9-12,14H2,1-4H3,(H,26,30)(H,27,29)/t16-/m1/s1. InChi Key: PFPSFENQCNMITC-MRXNPFEDSA-N.