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    InvivoChem Cat #: V0389
    CAS #: 1450655-76-1Purity ≥98%

    Description: CPI-169 (CPI169) is a novel, potent, and selective inhibitor of EZH2 (enhancer of zeste homolog 2) inhibitor with anticancer activity. It inhibits EZH2 WT, EZH2 Y641N, and EZH1 with IC50s of 0.24 nM, 0.51 nM, and 6.1 nM, respectively. CPI-169 exhibits excellent antiproliferative activity and high in vivo antitumor efficacy in a NHL xenograft model.

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

    Related CAS: 1802175-07-0 (R-isomer)

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    Molecular Weight (MW)528.66
    CAS No.1450655-76-1
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL (189.1 mM)
    Water: <1 mg/mL 
    Ethanol: 100 mg/mL (189.1 mM)
    Solubility (In vivo)10% DMSO+60% PEG 400+30% ddH2O: 30mg/mL
    SynonymsCPI 169; CPI169; CPI-169; (R,Z)-1-(1-(1-(ethylsulfonyl)piperidin-4-yl)ethyl)-N-((2-hydroxy-4-methoxy-6-methylpyridin-3-yl)methyl)-2-methyl-1H-indole-3-carbimidic acid

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    In Vitro

    In vitro activity: In KARPAS-422 cells, CPI-169 shows a dose-dependent inhibitory effect on cell viability, and produces synergy anti-proliferative activity when used in combination with ABT-199. In 16 out of 25 NHL cell lines, CPI-169 also suppresses cell growth with GI50 of<5 μM.

    Kinase Assay: Compound potency is also assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, PRC2 containing either EZH1 (160 pM), wt EZH2 (40 pM), or Y641N mutant EZH2 (80 pM, both EZH2 prepared in-house) is pre-incubated with 3H-SAM (0.9 µM), 2 µM H3K27me3 activating peptide (H2N-RKQLATKAAR(Kme3)SAPATGGVKKP-amide) and compounds (as 10 point duplicate dose response titrations) for 120 min in a buffer consisting of 50 mM Tris (pH 8.5), 1 mM DTT, 0.07 mM Brij-35, 0.1% BSA, and 0.8% DMSO in a total volume of 12.5 µl in a black 384 well plate. Reaction is initiated with biotinylated H3 substrate peptides (H3K27me1 for wt EZH2, H3K27me2 for Y641N mutant EZH2; H2N-RKQLATKAAR(Kmen)SAPATGGVKKP-NTPEGBiot) as a 2 µM stock in 12.5 µL and allowed to react at room temperature for 5 h. Quenching is accomplished by addition of 20 µl of STOP solution (50 mM Tris (pH 8.5), 200 mM EDTA, 2 mM SAH). 35 µL of the quenched solution is transferred to Streptavidin Flashplates, incubated overnight, washed, and read in a TopCount Reader. For titrations all compound dilutions are in DMSO, final DMSO concentrations are 0.8% (v/v), and turnover is kept to less than < 5%. IC50s are calculated using non-linear least square four parameter fits (GraphPad 6.0). 

    Cell Assay: Relative cell numbers are assessed by Cell Titer-Glo (CTG) luminescent cell viability assay using an Envision instrument. GraphPad Prism 6.0 is used for curve fitting, IC50/GI50 and Hill coefficient (H) calculations. The GI90 is calculated using the formula: EC90 = (90 /100-90)1/H * EC50. Cell line: 25 NHL cell lines

    In VivoIn mice bearing KARPAS-422 xenografts, CPI-169 (200 mg/kg, s.c.) effectively suppresses H3K27me3 levels and results in lymphoma tumor regression without affecting body weight or causing any overt adverse effects.
    Animal modelMice bearing KARPAS-422 subcutaneous xenografts
    Formulation & DosageDissolved in 10% DMSO + 60% polytheylene glycol 400 + 30% ddH2O;  200 mg/kg; s.c. injection

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

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

    Enhancer of Zeste Homolog 2 Inhibitors Cause Cell Killing in Various NHL Subtypes. Chem Biol. 2014, 21(11), 1463-1475.


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