2. Vitamin D Related/Nuclear Receptor
  3. Estrogen Receptor/ERR
  4. VPC-16606

VPC-16606 是一种选择性雌激素受体 α (ERα) 激活功能区 2 (AF2) 位点的抑制剂。VPC-16606 可阻断 ERα 与共激活因子的相互作用，抑制野生型及临床耐药突变型 ERα 活性，对激素耐药乳腺癌细胞具有抑制作用。VPC-16606 可用于乳腺癌的研究。

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VPC-16606

VPC-16606 Chemical Structure

CAS No. : 2027540-49-2

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VPC-16606 相关抗体

Top Publications Citing Use of Products

查看 Estrogen Receptor/ERR 亚型特异性产品:

查看所有亚型
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

VPC-16606 is a selective inhibitor targeting the activation function 2 (AF2) domain of estrogen receptor α (ERα). VPC-16606 blocks the interaction between ERα and coactivators, inhibits the activity of both wild-type and clinically drug-resistant mutant ERα, and exerts inhibitory effects on hormone-resistant breast cancer cells. VPC-16606 can be used in breast cancer research[1].

体外研究
(In Vitro)

VPC-16606 (24 h) 可强效抑制 T47D-KBluc 人乳腺癌细胞中 ERα 的转录活性，其 IC50 为 0.31 μM[1]。
VPC-16606 (1.6-50 μM; 24 h) 可阻断 MDA-MB-231 细胞中 ERα 与共激活因子 SRC-3 之间的相互作用[1]。
VPC-16606 (0-50 μM；96 h) 对 ERα 阳性且 Tamoxifen (HY-13757A) 耐药的人乳腺癌细胞发挥 ERα 特异性抗增殖作用[1]。
VPC-16606 (0.38-6 μM; 24 h) 可下调 MCF7 细胞和 Tamoxifen (HY-13757A) 耐药的 TamR3 人乳腺癌细胞中 ERα 依赖的基因表达[1]。

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

VPC-16606 相关抗体:

Cell Viability Assay[1]

Cell Line: ERα-positive (MCF7, T47D, TamR3) human breast cancer cells; ERα-negative MDA-MB-231 cells
Concentration: Up to 50 μM (2-fold dilution range)
Incubation Time: 96 h
Result: Significantly reduced the growth of ERα-positive MCF7, T47D, and Tamoxifen-resistant TamR3 cells in a dose-dependent manner, with no effect on ERα-negative MDA-MB-231 cells.

Real Time qPCR[1]

Cell Line: MCF7 and TamR3 human breast cancer cells
Concentration: 0.38, 0.75, 1.5, 3, 6 μM
Incubation Time: 24 h
Result: Significantly down-regulated the mRNA expression of ERα target genes pS2, PR, Cyclin D1, and CDC2 in both MCF7 and TamR3 cells at all tested concentrations.
体内研究
(In Vivo)

VPC-16606 (51 mg；腹腔注射) 可降低雌性 Rag2 小鼠的腹膜内乳腺癌肿瘤负荷[1]。

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

Animal Model: Rag2 (female, 10-12 weeks old, intraperitoneal implantation of luciferase-modified MCF7LUC ERα-positive human breast cancer cells, pre-implantation 60-day release estradiol pellet supplementation)[1]
Dosage: 51 mg
Administration: i.p. (via implanted Alzet pump); continuous
Result: Reduced total light emission from tumors at 60 days post-cell injection compared to vehicle-treated controls.
Reduced tumor burden compared to vehicle-treated controls.
Achieved median survival time of 60 days, with 100% survival to study termination at day 61.
分子量

344.81

Formula

C17H13ClN2O2S
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

VPC-16606 相关分类

  • 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.

Keywords:

VPC-166062027540-49-2VPC16606VPC 16606Estrogen Receptor/ERRestrogen receptortamoxifen-resistant cellsERαAF2 siteMCF7 human breast cancer cellsRag2 miceT47D-KBluc human breast cancer cellsMDA-MB-231 cellsInhibitorinhibitorinhibit

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目录号：
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