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    GNE-781
    GNE-781

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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 #: V4553
    CAS #: 1936422-33-1Purity ≥98%

    Description: GNE-781 is a novel, highly potent and selective CBP (Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein) inhibitor with an IC50 of 0.94 nM in TR-FRET assay. GNE-781 also inhibits BRET and BRD4(1) with IC50s of 6.2 nM and 5100 nM, respectively. GNE-781 showed TR-FRET IC50 = 0.94 nM, BRET IC50 = 6.2 nM, BRD4(1) IC50 = 5,100 nΜ) that maintained good in vivo PK properties in multiple species. GNE-781 displays anti-tumor activity in an AML tumor model and was also shown to decrease Foxp3 transcript levels in a dose dependent manner.

    References:  2017 Nov 22;60(22):9162-9183.


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    GNE-781

    Name: GNE-781
    CAS#: 1936422-33-1
    Chemical Formula: C27H33F2N7O2
    Exact Mass: 525.2664
    Molecular Weight: 525.6048
    Elemental Analysis: C, 61.70; H, 6.33; F, 7.23; N, 18.65; O, 6.09
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Technical InformationSynonym: GNE-781; GNE 781; GNE781.
    IUPAC/Chemical Name: 3-[7-(difluoromethyl)-6-(1-methylpyrazol-4-yl)-3,4-dihydro-2H-quinolin-1-yl]-N-methyl-1-tetrahydropyran-4-yl-6,7-dihydro-4H-pyrazolo[4,3-c]pyridine-5-carboxamide
    InChi Key: CQCWHSDMJBAGDC-UHFFFAOYSA-N
    InChi Code: InChI=1S/C27H33F2N7O2/c1-30-27(37)34-9-5-23-22(16-34)26(32-36(23)19-6-10-38-11-7-19)35-8-3-4-17-12-20(18-14-31-33(2)15-18)21(25(28)29)13-24(17)35/h12-15,19,25H,3-11,16H2,1-2H3,(H,30,37)
    SMILES Code: O=C(N1CCC(N(C2CCOCC2)N=C3N4CCCC5=C4C=C(C(F)F)C(C6=CN(C)N=C6)=C5)=C3C1)NC


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