2. Vitamin D Related/Nuclear Receptor
  3. Estrogen Receptor/ERR
  4. Antiestrogenic agent-1

Antiestrogenic agent-1，一种有机磷 13α-雌酮衍生物，是一种抗雌激素剂。Antiestrogenic agent-1 可通过抑制雌激素 (estrogen) 介导的转录活性来破坏雌激素信号通路。Antiestrogenic agent-1 能够抑制癌细胞的增殖、迁移、侵袭，并诱导 G1 期阻滞。Antiestrogenic agent-1 可缓解雌激素诱导的未成熟大鼠子宫增生，并在小鼠三阴性乳腺癌模型中抑制肿瘤生长。Antiestrogenic agent-1 可用于癌症及内分泌学相关研究，例如乳腺癌、口咽鳞状细胞癌。

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Antiestrogenic agent-1

Antiestrogenic agent-1 Chemical Structure

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Antiestrogenic agent-1 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

Antiestrogenic agent-1, an organophosphorus 13α-estrone derivative, is an antiestrogenic agent. Antiestrogenic agent-1 can disrupt estrogen signaling by inhibiting estrogen-mediated transcriptional activity. Antiestrogenic agent-1 can inhibit cancer cells proliferation, migration, invasion and induce G1-phase arrest. Antiestrogenic agent-1 mitigates estrogen-induced uterine growth in immature rats and inhibits tumor growth in a murine triple-negative breast cancer mice model. Antiestrogenic agent-1 can be used for the researches of cancer and endocrinology,such as breast cancer, oropharyngeal squamous cell carcinoma[1].

体外研究
(In Vitro)

Antiestrogenic agent-1 (Compound EDPO) (0.4-60 μM；24 h) 可抑制 T47D-KBluc 细胞中雌激素介导的转录活性，其 IC50 为 10 μM[1]。
Antiestrogenic agent-1 对 T47D 乳腺癌细胞以及 UPCI-SCC-131 口咽鳞状细胞癌细胞显示出显著的抗增殖作用，其 IC50 值分别为 7.2μM 和 5.3μM[1]。

Antiestrogenic agent-1 (1.75-7 μM；12-72 h) 可在 T47D 细胞中诱导呈时间和剂量依赖性的 G1 期细胞周期阻滞[1]。
Antiestrogenic agent-1 (2.5-5 μM (UPCI-SCC-131 细胞)；3.5-7 μM (T47D 细胞)；24-48 h) 可呈时间和浓度依赖性抑制 UPCI-SCC-131 细胞与 T47D 细胞的迁移[1]。
Antiestrogenic agent-1 (3.5-7 μM；48 h) 可降低 T47D 细胞的侵袭能力[1]。

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

Antiestrogenic agent-1 相关抗体:

Cell Cycle Analysis[1]

Cell Line: T47D (ERα+ human breast cancer cell line)
Concentration: 1.75, 3.5 and 7 μM
Incubation Time: 12, 24, 48, 72 h
Result: Induced substantial time- and dose-dependent G1-phase cell cycle arrest.
Increased G1 population and decreased S phase population at all time intervals, showed most pronounced arrest at 24 h.

Cell Migration Assay [1]

Cell Line: UPCI-SCC-131 (human oropharyngeal squamous cell carcinoma cell line), T47D (ERα+ human breast cancer cell line)
Concentration: 2.5 and 5 μM (UPCI-SCC-131); 3.5 and 7 μM (T47D)
Incubation Time: 24, 48 h (UPCI-SCC-131); 24, 48 h (T47D)
Result: Significantly reduced cell migration in both cell lines in a time- and concentration-dependent manner.
Achieved significant effect at both concentrations at 24 h, and only at 5 μM at 48 h for UPCI-SCC-131.
Achieved significant effect at both concentrations at 24 and 48 h for T47D.
体内研究
(In Vivo)

Antiestrogenic agent-1 (Compound EDPO) (60-600 μg/g；皮下注射；每日 1 次，持续 3 天) 可有效抑制 21 日龄雌性未成熟 SD 大鼠中雌激素受体 α 介导的子宫组织生长[1]。
Antiestrogenic agent-1 (10-30 μg/g；腹腔注射；每日一次；连续 16 天) 对带有 4T1 三阴性乳腺癌的 BALB/c 小鼠表现出显著的剂量依赖性抗肿瘤活性[1]。

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

Animal Model: Sprague-Dawley (female, 21 days old, 35-47 g, 17β-estradiol-induced uterine growth)[1]
Dosage: 60, 600 μg/g
Administration: S.c.; daily; 3 days
Result: Mitigated 17β-estradiol-induced uterine growth in a dose-dependent manner.
Showed no significant difference in inhibitory effects on uterine tissue growth compared to Fulvestrant (HY-13636) at the higher dose.
Animal Model: BALB/c mice (female, 8-10 weeks old, orthotopic 4T1 murine breast cancer)[1]
Dosage: 10, 30 μg/g
Administration: I.p.; daily; 16 days
Result: Induced a significant and dose-dependent reduction in tumor growth throughout the 16-day treatment period.
Reduced tumor growth significantly from day 2 onwards at the higher dose.
分子量

498.59

Formula

C32H35O3P
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

Antiestrogenic agent-1 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:

Antiestrogenic agent-1Antiestrogenic agent1Antiestrogenic agent 1Estrogen Receptor/ERRERαoropharyngeal carcinoma cellsmurine triple-negative breast cancerT47D-KBlucUPCI-SCC-131T47D4T1Inhibitorinhibitorinhibit

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目录号：
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