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OP-1074

Chemical Structure : OP-1074

CAS No.: 1443752-76-8

OP-1074 (OP1074)

Catalog No.: PC-35243Not For Human Use, Lab Use Only.

OP-1074 (OP1074) is a potent, selective ER degrader (SERD), shows specific antiestrogenic activity for both ERα and ERβ, inhibits 17β-estradiol (E2)-stimulated transcriptional activity with IC50 of 1.6 and 3.2 nM, respectively.

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    Biological Activity

    OP-1074 (OP1074) is a potent, selective ER degrader (SERD), shows specific antiestrogenic activity for both ERα and ERβ, inhibits 17β-estradiol (E2)-stimulated transcriptional activity with IC50 of 1.6 and 3.2 nM, respectively.
    OP-1074 displays no activity on other steroid receptors.
    OP-1074 inhibits E2-induced proliferation of breast cells (MCF-7 cell IC50=7 nM) and degrades ERα, inhibiting ER-mediated signaling with IC50 of 3.2 nM.
    OP-1074 shrinks tumors in tamoxifen-resistant xenograft model.

    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

    (2S)-3-(4-hydroxyphenyl)-4-methyl-2-(4-{2-[(3R)-3-methylpyrrolidin-1-yl]ethoxy}phenyl)-2H-1-benzopyran-7-ol

    References

    1. Fanning SW, et al. Nat Commun. 2018 Jun 18;9(1):2368.

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