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    EPZ015666 (GSK3235025; EPZ015866)
    EPZ015666 (GSK3235025; EPZ015866)

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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 #: V0390
    CAS #: 1616391-65-1Purity ≥98%

    Description: EPZ015666 (GSK-3235025; EPZ-015866), an analog of EPZ-015866, is a potent, selective and orally bioavailable inhibitor of PRMT5 (protein arginine methyltransferase) with antineoplastic activity. It inhibits the enzymatic activity of PRMT5 with Ki of 5-22 nM in biochemical assays, and displays >20,000-fold selectivity for PRMT5 over other PMTs.  

    References: Nat Chem Biol. 2015 Jun;11(6):432-7.

    Related CAS: 1616391-87-7 (EPZ015866)

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    Molecular Weight (MW)383.44
    FormulaC20H25N5O3
    CAS No.1616391-65-1; 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 60 mg/mL (156.5 mM)          
    Water: <1 mg/mL
    Ethanol: 48 mg/mL (125.2 mM)
    Solubility (In vivo)2% DMSO+30% PEG 300+ddH2O: 5 mg/mL
    Synonyms

    GSK-3235025; GSK 3235025; GSK3235025; EPZ-015666; EPZ 015666; EPZ015666.

    Chemical Name: (S)-N-(3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)-6-(oxetan-3-ylamino)pyrimidine-4-carboxamide

    InChi Key: ZKXZLIFRWWKZRY-KRWDZBQOSA-N

    InChi Code: InChI=1S/C20H25N5O3/c26-17(10-25-6-5-14-3-1-2-4-15(14)9-25)8-21-20(27)18-7-19(23-13-22-18)24-16-11-28-12-16/h1-4,7,13,16-17,26H,5-6,8-12H2,(H,21,27)(H,22,23,24)/t17-/m0/s1

    SMILES Code: O=C(C1=NC=NC(NC2COC2)=C1)NC[[email protected]](O)CN3CC4=C(C=CC=C4)CC3 


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    In Vitro

    In vitro activity: EPZ015666 (also known as GSK3235025, an analog of EPZ015866) is a potent, selective and orally bioavailable inhibitor of PRMT5 (protein arginine methyltransferase) enzymatic activity in biochemical assays with Ki of 5-22 nM, and shows >20,000-fold selectivity over other PMTs. EPZ015666 demonstrates broad selectivity against a panel of other histone methyltransferases. Treatment of MCL cell lines with EPZ015666 led to inhibition of SmD3 methylation and cell death, with IC50 values in the nanomolar range. Oral dosing with EPZ015666 demonstrated dose-dependent antitumor activity in multiple MCL xenograft models. EPZ015666 represents a validated chemical probe for further study of PRMT5 biology and arginine methylation in cancer and other diseases. 


    Kinase Assay: EPZ015666 (also known as GSK3235025, an analog of EPZ015866) is a potent, selective and orally bioavailable inhibitor of PRMT5 (protein arginine methyltransferase) enzymatic activity in biochemical assays with Ki of 5-22 nM, and shows >20,000-fold selectivity over other PMTs. EPZ015666 demonstrates broad selectivity against a panel of other histone methyltransferases.


    Cell Assay: EPZ015666 shows potent cellular activity that blocks symmetric dimethylation of SmD3 and inhibit proliferation of MCL cell lines (Z-138, Granta-519, Maver-1, Mino, and Jeko-1) with IC50 of 96-904 nM. Treatment of MCL cell lines with EPZ015666 led to inhibition of SmD3 methylation and cell death, with IC50 values in the nanomolar range.

    In VivoEPZ015666 (200 mg/kg, p.o.) displays robust anti-tumor activity in MCL xenograft animal models
    Animal modelMCL (Z-138, and Maver-1) xenograft models
    Formulation & DosageDissolved in 0.5 % MC; 200 mg/kg; p.o.
    ReferencesNat Chem Biol. 2015 Jun;11(6):432-7.


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

    EPZ015666

    Co-crystal structures of PRMT5:MEP50 (green) with compound 8 (A, magenta), compound 9 (B, orange), compound 10 (C, yellow), and compound 15 (D, cyan).   2015 Dec 2;7(2):162-6.

    EPZ015666

    Plot of cLogD vs scaled clearance (CL) from human microsomes (A) and mouse liver microsomes (B). Plot of proliferation IC50in Z-138 cells vs observed CL in mouse PK (C) and percentage oral bioavailability %F from mouse PK (D) dosed at 2 mg/kg IV and 10 mg/kg PO. 2015 Dec 2;7(2):162-6.

    EPZ015666

    Plasma PK profile of EPZ015666 in male CD-1 mouse following single dose administration at 10 and 100 mg/kg p.o. Methyl mark IC90 corrected for PPB shown as dotted line.

     2015 Dec 2;7(2):162-6.



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