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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-Estrogen Receptor/ERR-OP-1074
OP-1074

Chemical Structure : OP-1074

CAS No.: 1443752-76-8

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OP-1074 (OP1074)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    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.

    物理化学性质&存储条件

    分子量 457.57
    分子式 C29H31NO4
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20 °C 12 个月; 4°C 6 个月
    配置液
    -80 °C 6 个月; -20°C 6 个月
    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

    参考文献

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

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