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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-Glucocorticoid receptor (GR)-ORIC-101
ORIC-101

Chemical Structure : ORIC-101

CAS No.: 2222344-98-9

ORIC-101 (ORIC101)

货号: PC-35571Not For Human Use, Lab Use Only.

ORIC-101 (ORIC101) is a highly potent, selective steroidal glucocorticoid receptor (GR) antagonist (IC50=5.6 nM) with reduced androgen receptor (AR) agonistic activity.

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

    生物&药学活性

    ORIC-101 (ORIC101) is a highly potent, selective steroidal glucocorticoid receptor (GR) antagonist (IC50=5.6 nM) with reduced androgen receptor (AR) agonistic activity.
    ORIC-101 dose-dependently reduces the expression levels of two established GR target genes, GILZ and FKBP5 with IC50 of 24.9 and 19.5 nM in human PBMCs.
    ORIC-101 demonstrates in vivo antitumor activity by enhancing response to chemotherapy in the GR+ OVCAR5 ovarian cancer xenograft model.

    物理化学性质&存储条件

    分子量 501.755
    分子式 C34H47NO2
    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

    (8R,9S,10R,11S,13S,14S,17S)-17-(3,3-Dimethylbut-1-yn-1-yl)-17-hydroxy-11-(4-(isopropyl(methyl)amino)phenyl)-13-methyl-1,2,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-3H-cyclopenta[a]phenanthren-3-one

    参考文献

    1. Rew Y, et al. J Med Chem. 2018 Aug 9. doi: 10.1021/acs.jmedchem.8b00743.

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