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    Pinometostat (EPZ-5676)
    Pinometostat (EPZ-5676)

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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 #: V0378
    CAS #: 1380288-87-8Purity ≥98%

    Description: Pinometostat (formerly EPZ 5676) is a potent and SAM (S-adenosyl methionine) competitive DOT1L protein methyltransferase (PMT) inhibitor with potential antitumor activity. It inhibits DOT1L with a Ki of 80 pM in a cell-free assay, and exhibits >37,000-fold higher selectivity for DOT1L over other PMTs. It exhibits excellent antiproliferative activity and high in vivo antitumor efficacy.

    References: Blood. 2013 Aug 8;122(6):1017-25.

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    Molecular Weight (MW)562.71
    FormulaC30H42N8O3
    CAS No.1380288-87-8
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL (177.71mM)
    Water: <1 mg/mL
    Ethanol: 92 mg/mL (163.5 mM)
    Solubility (In vivo)2% DMSO+30% PEG 300+5% Tween 80+ddH2O: 5 mg/mL
    Synonyms

    EPZ 5676; Pinometostat; EPZ-5676; EPZ5676

    Chemical Name: (2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol

    InChi Key: LXFOLMYKSYSZQS-LURJZOHASA-N

    InChi Code: InChI=1S/C30H42N8O3/c1-16(2)37(13-22-25(39)26(40)29(41-22)38-15-34-24-27(31)32-14-33-28(24)38)19-10-17(11-19)6-9-23-35-20-8-7-18(30(3,4)5)12-21(20)36-23/h7-8,12,14-17,19,22,25-26,29,39-40H,6,9-11,13H2,1-5H3,(H,35,36)(H2,31,32,33)/t17-,19+,22-,25-,26-,29-/m1/s1

    SMILES Code: O[[email protected]]1[[email protected]](N2C=NC3=C(N)N=CN=C23)O[[email protected]](CN([[email protected]]4C[[email protected]@H](CCC5=NC6=CC(C(C)(C)C)=CC=C6N5)C4)C(C)C)[[email protected]]1O 


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    In Vitro

    In vitro activity: EPZ-5676 reduces H3K79 dimethylation with a cellular IC50 of 2.6 nM in MV4-11 cells. EPZ-5676 treatment results in concentration- and time-dependent reduction of H3K79 methylation without effect on the methylation status of other histone sites, which leads to inhibition of key MLL target genes and selective, apoptotic cell killing in MLL-rearranged leukemia cells. EPZ-5676 inhibits proliferation of MLL-AF4 rearranged cell line MV4-11 with an IC50 of 9 nM.


    Kinase Assay: The enzyme inhibition constant (Ki) value for EPZ5676 was determined by fitting inhibition data to the Morrison quadratic equation. Residence time for EPZ5676 was calculated as the reciprocal of the enzymatic-ligand dissociation rate, determined by surface plasmon resonance.


    Cell Assay: EPZ5676 potently inhibited MV4-11 cell proliferation with an IC50 value of 3.5 nM. Antiproliferative activity was realized after 4 days and was most clear after 7 days of EPZ-5676 treatment.

    In VivoIn nude rats bearing MV4-11 xenografts, EPZ5676 caused complete tumor regressions that were sustained well beyond the compound infusion period with no significant weight loss or signs of toxicity.
    Animal modelNude rats bearing MV4-11 xenografts
    Formulation & Dosage35, 67 or 70 mg/kg/day; i.v.
    References

    Blood. 2013 Aug 8;122(6):1017-25


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

    EPZ5676
    EPZ-5676 causes tumor regressions and demonstrates in vivo target inhibition in tumor and surrogate tissue in a rat model of MLL-rearranged leukemia. Blood. 2013 Aug 8; 122(6): 1017–1025.




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