1. Vitamin D Related/Nuclear Receptor
  2. Estrogen Receptor/ERR
  3. ERα degrader 7

ERα degrader 7 (化合物 B1) 是一种有效的 ERα 降解剂,其 IC50 为 14.6 nM, DC 50 为 9.7 nM。ERα degrader 7 展现出优秀的抗肿瘤活性,表明其有潜力成为一种可用于乳腺癌研究的选择性雌激素受体降解剂 (SERD) 。

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ERα degrader 7 Chemical Structure

ERα degrader 7 Chemical Structure

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Customer Review

查看 Estrogen Receptor/ERR 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ERα degrader 7 (compound B1) is a potent ERα degrader with an IC50 of 14.6 nM and a DC50 of 9.7 nM, respectively. ERα degrader 7 shows excellent antitumor activity, indicating its potential to evolve as a promising selective estrogen-receptor degrader (SERD) for breast cancer research[1].

IC50 & Target

IC50: 14.6 nM (ERα)[1]

体外研究
(In Vitro)

ERα degrader 7 (10-5-10 μM, 5 d) 对乳腺癌细胞表现出抗肿瘤活性 (IC50 = 4.21 nM) 且对正常乳腺上皮细胞无细胞毒性[1]
ERα degrader 7 (50-1000 nM, 5 d)对 MCF-7 中 ERα 表现出显著的浓度依赖性降解效果[1]

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

Cell Proliferation Assay[1]

Cell Line: MCF-10 (normal breast epithelial cell)
Concentration: 10-5-10 μM
Incubation Time: 5 d
Result: Demonstrated low inhibition against MCF-10A, cell proliferation rate of each concentration are all above 80%.

Cell Proliferation Assay[1]

Cell Line: MCF-7 (breast cancer cell)
Concentration: 10-5-10 μM
Incubation Time: 5 d
Result: ERα degrader 7 (10-3-10 μM) demonstrated excellent antitumor activity against the MCF-7 cell, caused an inhibition rate ranged from 60% to 75%, results were evaluated using GDC-9545 as a positive control.

Western Blot Analysis[1]

Cell Line: MCF-7 (breast cancer cell)
Concentration: 1, 10, 50, 100, 200, 500, 1000 nM
Incubation Time: 5 d
Result: Showed a concentration-dependent degradation effect of ERα. Demonstrated a significant ERα-degradation effect (ERα expression rate < 50%) at a concentration of 50 nM, results were evaluated using GDC-9545 as a positive control.
分子量

512.50

Formula

C28H24F4N2O3

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
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

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产品名称:
ERα degrader 7
目录号:
HY-155492
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