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GNE-274

Chemical Structure : GNE-274

CAS No.: 2369048-69-9

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GNE-274 (GNE274)

Catalog No.: PC-73046Not For Human Use, Lab Use Only.

GNE-274 (GNE274) is a small molecule non-degrader, partial agonist of estrogen receptor (ER), failed to trigger increased ER turnover in tested cell line.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    GNE-274 (GNE274) is a small molecule non-degrader, partial agonist of estrogen receptor (ER), failed to trigger increased ER turnover in tested cell line.
    GNE-274 potently inhibited cellular proliferation of ER+ HER2-negative cell lines, induced an LBD antagonist conformation similar to GDC-0927, neither promotes the degree of anti-proliferative activity achieved by GDC-0927.
    GNE-274 displays considerable transcriptional agonism, GNE-274 increased chromatin accessibility at 373 induced ER binding site.

    Physicochemical Properties

    M.Wt 457.57
    Formula C29H31NO4
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO
    Chemical Name/SMILES

    (S)-3-(3-hydroxyphenyl)-4-methyl-2-(4-((1-propylazetidin-3-yl)methoxy)phenyl)-2H-chromen-6-ol

    References

    1. Guan J, et al. Cell. 2019 Aug 8;178(4):949-963.e18.

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