| Identification | Back Directory | [Name]
CPI 360 | [CAS]
1802175-06-9 | [Synonyms]
CPI360
CPI-360
CPI 360
CPI-360 (R)
CPI360;CPI 360
1H-Indole-3-carboxamide, N-[(1,2-dihydro-4-methoxy-6-methyl-2-oxo-3-pyridinyl)methyl]-2-methyl-1-[(1R)-1-(tetrahydro-2H-pyran-4-yl)ethyl]- | [Molecular Formula]
C25H31N3O4 | [MDL Number]
MFCD28167834 | [MOL File]
1802175-06-9.mol | [Molecular Weight]
437.53 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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. | [References]
[1] WILLIAM D BRADLEY. EZH2 inhibitor efficacy in non-Hodgkin’s lymphoma does not require suppression of H3K27 monomethylation.[J]. Chemistry & biology, 2014: 1463-1475. DOI: 10.1016/j.chembiol.2014.09.017 |
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