OP-1074

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

OP-1074  纯度: 99.47%

OP-1074，纯抗雌激素药，是一种选择性 ER 降解剂 (PA-SERD)，对 ERα 和 ERβ 具有特异性抗雌激素活性，可抑制 17β-estradiol (E2)-刺激的转录活性，IC50 分别为 1.6 和 3.2 nM。

OP-1074

OP-1074 Chemical Structure

CAS No. : 1443752-76-8

规格 价格 是否有货 数量
5 mg ￥8500 In-stock
10 mg ￥14500 In-stock
50 mg   询价  
100 mg   询价  

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OP-1074 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Anti-Cancer Compound Library
  • Anti-Breast Cancer Compound Library

生物活性

OP-1074 is a pure antiestrogen and a selective ER degrader (PA-SERD), shows specific antiestrogenic activity for ERα and ERβ, inhibits 17β-estradiol (E2)-stimulated transcriptional activity with IC50 of 1.6 and 3.2 nM, respectively[1].

IC50 & Target[1]

ERα

 

ERβ

 

体外研究
(In Vitro)

OP-1074 (0-100 nM; 24 hours) inhibits  MCF-7 cells  and CAMA-1 cells proliferation with IC50 values of 6.3 and 9.2 nM, respectively[1].
OP-1074 (100 nM; 24 hours) destabilizatizes ERα protein expression in MCF-7 and CAMA-1 cells[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: MCF-7 cells, CAMA-1 cells
Concentration: 0 nM, 10 nM,100 nM
Incubation Time: 24 hours
Result: Inhibited breast cancer cell proliferation.

Western Blot Analysis[1]

Cell Line: MCF-7 cells, CAMA-1 cells
Concentration: 100 nM
Incubation Time: 24 hours
Result: Downregulated ERα protein expression.

分子量

457.56

Formula

C29H31NO4
CAS 号

1443752-76-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

-20°C, stored under nitrogen, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
参考文献

  • [1]. Fanning SW, et al. Specific stereochemistry of OP-1074 disrupts estrogen receptor alpha helix 12 and confers pure antiestrogenic activity.Nat Commun. 2018 Jun 18;9(1):2368.

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