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CPI-360

Chemical Structure : CPI-360

CAS No.: 1802175-06-9

CPI-360 (CPI 360)

Catalog No.: PC-21930Not For Human Use, Lab Use Only.

CPI-360 is a potent, selective EZH2 inhibitor with IC50 of 0.5 and 2.5 nM for wild-type EZH2 and Y641N mutant EZH2, respectively.

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Biological Activity

CPI-360 is a potent, selective EZH2 inhibitor with IC50 of 0.5 and 2.5 nM for wild-type EZH2 and Y641N mutant EZH2, respectively.
CPI-360 decreases cellular levels of H3K27me3 and H3K27me2 (EC50, 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.
CPI-360 (200 mg/kg) reduced tumor growth of KARPAS-422 xenografts in mice.

Physicochemical Properties

M.Wt 437.54
Formula C25H31N3O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

References

1. Gehling VS, et al. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3644-9.

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