2. Vitamin D Related/Nuclear Receptor
  3. Estrogen Receptor/ERR
  4. Fulvestrant-3-boronic acid

Fulvestrant-3-boronic acid  (Synonyms: ZB716)

目录号: HY-137144
产品使用指南

摩尔计算器

Fulvestrant-3-boronic acid 是一种有口服活性的 ERα 抑制剂，可与 ERα 竞争性结合 (IC50 = 4.1 nM)，并有效降解乳腺癌细胞中的 ERα。

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Fulvestrant-3-boronic acid Chemical Structure

Fulvestrant-3-boronic acid Chemical Structure

CAS No. : 1853279-29-4

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Fulvestrant-3-boronic acid 相关抗体

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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

Fulvestrant-3-boronic acid is an orally active ERα inhibitor, which binds to ERα competitively (IC50 = 4.1 nM) and effectively degrades ERα in breast cancer cells[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
MCF7 IC50
0.0032 μM
Compound: 5; ZB716
Antiproliferative activity against human MCF7 cells after 5 days by coulter counter analysis
Antiproliferative activity against human MCF7 cells after 5 days by coulter counter analysis
[PMID: 27529700]
MCF7 IC50
0.069 μM
Compound: 5; ZB716
Antiproliferative activity against human tamoxifen-resistant MCF7 cells after 5 days by coulter counter analysis
Antiproliferative activity against human tamoxifen-resistant MCF7 cells after 5 days by coulter counter analysis
[PMID: 27529700]
T47D IC50
0.0061 μM
Compound: 5; ZB716
Antiproliferative activity against human T47D cells after 5 days by coulter counter analysis
Antiproliferative activity against human T47D cells after 5 days by coulter counter analysis
[PMID: 27529700]
T47D IC50
0.037 μM
Compound: 5; ZB716
Antiproliferative activity against human tamoxifen-resistant T47D cells over-expressing PKC-alpha after 5 days by coulter counter analysis
Antiproliferative activity against human tamoxifen-resistant T47D cells over-expressing PKC-alpha after 5 days by coulter counter analysis
[PMID: 27529700]
T47D IC50
12.7 nM
Compound: 5; ZB716
Downregulation of ER-alpha expression in human tamoxifen-resistant T47D cells over-expressing PKC-alpha measured after 5 days by Western blot analysis
Downregulation of ER-alpha expression in human tamoxifen-resistant T47D cells over-expressing PKC-alpha measured after 5 days by Western blot analysis
[PMID: 27529700]
T47D IC50
7.8 nM
Compound: 5; ZB716
Downregulation of ER-alpha expression in human T47D cells measured after 5 days by Western blot analysis
Downregulation of ER-alpha expression in human T47D cells measured after 5 days by Western blot analysis
[PMID: 27529700]
体外研究
(In Vitro)

Fulvestrant-3-boronic acid (1-27 nM, 5 d) 剂量依赖性地显著下调 T47D 和 T47D/PKCα 细胞中的 ERα 蛋白[1]。

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

Fulvestrant-3-boronic acid 相关抗体:
体内研究
(In Vivo)

Fulvestrant-3-boronic acid (8.3 mg/kg, 口服) 显示出的 T /2 为 23.5 小时，Cmax 为 169.8 ng/mL, AUC 为 2547.1 ng•h/mL[1]。

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

634.59

Formula

C32H48BF5O4S
CAS 号
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

Fulvestrant-3-boronic acid 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

Fulvestrant-3-boronic acid1853279-29-4ZB716ZB 716ZB-716Estrogen Receptor/ERRorally activeERαdegraderbreast cancerInhibitorinhibitorinhibit

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