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    CPI-360
    CPI-360

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0386
    CAS #: 1802175-06-9Purity ≥98%

    Description: CPI-360 is a novel, highly potent, selective, and SAM-competitive inhibitor of enhancer of zeste homolog 2 (EZH2) with potential antitumor activity. It inhibits wt EZH2 and Y641N EZH2 with an IC50 of 0.5 nM and 2.5 nM, respectively. CPI-360 exhibits excellent antiproliferative activity and high in vivo antitumor efficacy. It functions on the basis of S-adenosyl-Lmethionine (SAM)-competition, inhibits EZH1 about 100-fold less and shows exquisite selectivity across a large panel of histone lysine and arginine, and DNA methyltransferases. CPI-360 potently reduced global H3K27me3 and H3K27me2 levels in a dose dependent manner. CPI-360 effectively suppressed heavy H3K27me3 incorporation in KARPAS-422 cells without affecting total histone turnover.

    References: Chem Biol. 2014 Nov 20;21(11):1463-75.

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    Molecular Weight (MW)437.53
    FormulaC25H31N3O4
    CAS No.1802175-06-9
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 20 mg/mL (45.7 mM)
    Water: <1 mg/mL
    Ethanol: 18 mg/mL (41.1 mM)
    Solubility (In vivo)10% DMSO+60% PEG 400+ddH2O: 20 mg/mL
    SynonymsCPI360; CPI 360; CPI-360; (R)-N-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(tetrahydro-2H-pyran-4-yl)ethyl)-1H-indole-3-carboxamide


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    In Vitro

    In vitro activity: 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.


    Kinase Assay: CPI-360 is a potent, selectiveEZH2inhibitor with IC50 of 0.5 nM and 2.5 nM nM for wt EZH2 and Y641N EZH2, respectively.


    Cell Assay: CPI-360 functions on the basis of S-adenosyl-Lmethionine  (SAM)-competition, inhibits EZH1 about 100-fold less and shows exquisite selectivity across a large panel of histone lysine and arginine, and DNA methyltransferases. CPI-360 potently reduced global H3K27me3 and H3K27me2 levels in a dosedependent manner. CPI-360 effectively suppressed heavy H3K27me3 incorporation in KARPAS-422 cells without affecting total histone turnover. CPI-360 treatment causes time-dependent transcriptional changes in germinal center B cell-like diffuse large B cell lymphoma.

    In VivoIn mice bearing KARPAS-422 xenografts, CPI-360 (200 mg/kg, s.c.) reduces tumor growth by 44%.
    Animal modelMice bearing KARPAS-422 tumors
    Formulation & DosageDissolved in 10% DMSO + 60% polytheylene glycol 400 + 30% ddH2O;  200 mg/kg; s.c.injection
    References

    Chem Biol. 2014 Nov 20;21(11):1463-75.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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