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    GNE-272
    GNE-272

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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 #: V4552
    CAS #: 1936428-93-1Purity ≥98%

    Description: GNE-272 is a novel, potent and selective in vivo chemical probe for and inhibitor of the CBP/EP300 bromodomains with IC50 values of 0.02, 0.03 and 13 μM for CBP, EP300 and BRD4, respectively. The single bromodomain of the closely related transcriptional regulators CBP/EP300 is a target of much recent interest in cancer and immune system regulation. A co-crystal structure of a ligand-efficient screening hit and the CBP bromodomain guided initial design targeting the LPF shelf, ZA loop, and acetylated lysine binding regions. Structure-activity relationship studies allowed us to identify a more potent analogue. Optimization of permeability and microsomal stability and subsequent improvement of mouse hepatocyte stability afforded 59 (GNE-272, TR-FRET IC50 = 0.02 μM, BRET IC50 = 0.41 μM, BRD4(1) IC50 = 13 μM) that retained the best balance of cell potency, selectivity, and in vivo PK. GNE-272 showed a marked antiproliferative effect in hematologic cancer cell lines and modulates MYC expression in vivo that corresponds with antitumor activity in an AML tumor model.

    References:  2016 Dec 8;59(23):10549-10563.


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    GNE-272

    Name: GNE-272
    CAS#: 1936428-93-1
    Chemical Formula: C22H25FN6O2
    Exact Mass: 424.2023
    Molecular Weight: 424.4804
    Elemental Analysis: C, 62.25; H, 5.94; F, 4.48; N, 19.80; O, 7.54
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Technical InformationSynonym: GNE-272; GNE 272; GNE272.
    IUPAC/Chemical Name: (S)-1-(3-((2-fluoro-4-(1-methyl-1H-pyrazol-4-yl)phenyl)amino)-1-(tetrahydrofuran-3-yl)-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)ethan-1-one
    InChi Key: NKOJNOBJGYTLLZ-KRWDZBQOSA-N
    InChi Code: InChI=1S/C22H25FN6O2/c1-14(30)28-7-5-21-18(12-28)22(26-29(21)17-6-8-31-13-17)25-20-4-3-15(9-19(20)23)16-10-24-27(2)11-16/h3-4,9-11,17H,5-8,12-13H2,1-2H3,(H,25,26)/t17-/m0/s1
    SMILES Code: CC(N1CCC2=C(C(NC3=C(F)C=C(C4=CN(C)N=C4)C=C3)=NN2[[email protected]]5CCOC5)C1)=O


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