2. Vitamin D Related/Nuclear Receptor
  3. Estrogen Receptor/ERR
  4. ERα degrader 10

ERα degrader 10 是一种强效、选择性且具有口服活性的雌激素受体 α (ERα) 降解剂。ERα degrader 10 表现出强效的 ERα 结合亲和力 (IC50 为 24.0 nM) 和降解能力 (EC50 为 5.3 nM)。ERα degrader 10 通过蛋白酶体介导的途径降解 ERα。ERα degrader 10 可用于乳腺癌的研究。

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ERα degrader 10 Chemical Structure

ERα degrader 10 Chemical Structure

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ERα degrader 10 相关抗体

Top Publications Citing Use of Products

查看 Estrogen Receptor/ERR 亚型特异性产品:

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Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ERα degrader 10 is a selective and orally active estrogen receptor α (ERα) degrader. ERα degrader 10 exhibits potent ERα binding affinity (IC50 of 24.0 nM) and degradation ability (EC50 of 5.3 nM). ERα degrader 10 degrades ERα through the proteasome-mediated pathway. ERα degrader 10 can be used for the study of breast cancer[1].

IC50 & Target[1]

ERα

24 nM (IC50)

体外研究
(In Vitro)

ERα degrader 10（化合物 A20) 对 MCF-7 细胞具有突出的抗增殖作用 (IC50 of 0.28 nM)。 ERα degrader 10（化合物 A20；0.1-1000 nM；1-48 h）表现出浓度依赖性 ERα 降解，24 h 降解效果最佳，通过蛋白酶体介导的蛋白质降解途径[1]。
ERα degrader 10（10-100 nM；24 h）可抑制 ERα 信号转导，诱导 MCF-7 细胞周期停滞于 G1 期[1]。
MCF-7 cells[1] 10 nM, 50 nM, 100 nM 24 h Could induce cell cycle arrest in G1 phase.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

ERα degrader 10 相关抗体:

Western Blot Analysis[1]

Cell Line: MCF-7 cells
Concentration: 0.1 nM, 1 nM, 10 nM, 50 nM, 100 nM, 500 nM, 1000 nM
Incubation Time: 1 h, 3 h, 6 h, 12 h, 24 h, 48 h
Result: ERα protein level decreased significantly.

Cell Cycle Analysis[1]

Cell Line: MCF-7 cells
Concentration: 10 nM, 50 nM, 100 nM
Incubation Time: 24 h
Result: Could induce cell cycle arrest in G1 phase.
体内研究
(In Vivo)

ERα degrader 10（10-30 mg/kg；口服灌胃；每日一次；持续 30 天）在体内 MCF-7 异种移植模型中表现出优异的抗肿瘤作用[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female nude mice injected with MCF-7 cells and estrogen (0.15 mg/mL)[1]
Dosage: 10 mg/kg and 30 mg/kg
Administration: Oral gavage; daily; for 30 days
Result: Showed excellent antitumor effect in the MCF-7 xenograft model in vivo
分子量

468.97

Formula

C29H25ClN2O2
运输条件

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

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

ERα degrader 10 相关分类

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  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ERα degrader 10ERα degrader10ERα degrader-10Estrogen Receptor/ERRERα degraderproteasome-mediated pathwaybreast cancerG1 phaseInhibitorinhibitorinhibit

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ERα degrader 10
目录号：
HY-168099
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