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Fulvestrant

产品编号 T2146 CAS 129453-61-8

别名: ZM 182780, 氟维司群, ZD 9238, ICI 182780

Fulvestrant 是纯抗雌激素，也是一种雌激素受体拮抗剂，IC50为 9.4 nM。它抑制ER 阳性 MCF-7 细胞的生长，IC50为 0.29 nM。它还是一种GPR30的激动剂。它可诱导细胞自噬和凋亡，有抗肿瘤作用。

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Fulvestrant, CAS 129453-61-8

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Fulvestrant is a potent Estrogen Receptor antagonist (IC50: 9.4 nM).
靶点活性	Estrogen Receptor:9.4 nM (cell free)
体外活性	The in vitro growth-inhibitory potency of Fulvestrant (ICI 182,780) exceeded that of ICI 164,384 in MCF-7 human breast cancer cells, where 50% inhibitory concentrations of 0.29 and 1.3 nM, respectively, were recorded [1]. The antiestrogen ICI 182780 (ICI) at 10 nM decreases Insulin-like growth factor I (IGF-I) receptor (IGF-IR) mRNA levels by 70% after treatment for 48 h [2]. ICI 182,780, in a concentration-dependent manner, significantly promoted neuron survival following exposure to either excitotoxic glutamate (200 muM)- or beta-amyloid(1-42) (1.5 muM)-induced neurodegeneration of hippocampal neurons [3].
体内活性	When administered alone, parenterally (s.c.), to immature female rats ICI 182,780 was devoid of uterotropic activity and, when coadministered with estradiol, it effectively blocked the uterotropic action of estradiol in a dose-dependent manner [ED50 0.06 mg/kg/day s.c.]. Complete antagonism of estrogen action was achieved with a dose of 0.5 mg ICI 182,780/kg/day s.c [1]. Cylindrical epithelial cells slightly taller, epithelial dysplasia and an increase in smooth muscle layer were observed in the ventral prostate from ICI 182,780 ((10 mg/rat, s.c.)-treated rats. ICI 182,780 did not change the mRNA but decreased the protein levels for AR in the ventral prostate. The expression of ESR1 (mRNA and protein) was upregulated by ICI 182,780. ICI 182,780 decreased the phosphorylation state of ERK1/2, with no changes in total ERK1/2 levels. Ki-67-positive cells in the ventral prostate were also decreased by ICI 182,780 [4].
细胞实验	In brief, hippocampi were dissected from the brains of embryonic day 18 Sprague-Dawley rat fetuses, treated with 0.02% trypsin in Hanks' balanced salt solution (137 mM NaCl, 5.4 mM KCl, 0.4 mM KH2PO4, 0.34 mM Na2HPO4·7H2O, 10.0 mM glucose, and 10.0 mM HEPES) at 37°C for 5 min and dissociated by repeated passage through a series of fire-polished constricted Pasteur pipettes. For intracellular Ca2+ imaging analyses, approximately 10^4 cells were seeded onto poly-D-lysine (10 μg/ml)-coated 22-mm coverslips in covered 35-mm Petri dishes. For neuroprotection and Western immunoblotting analyses, approximately 10^6 cells/ml were seeded onto poly-D-lysine-coated solid black and clear bottom 96-well culture plates and 60-mm Petri dishes, respectively. Cells were grown in phenol-red free neurobasal medium supplemented with B27, 5 U/ml penicillin, 5 μg/ml streptomycin, 0.5 mM glutamine, and 25 μM glutamate at 37°C in 10% CO2 for the first 3 days and NBM without glutamate afterward. Cultures grown in serum-free NBM yields approximately 99.5% neurons and 0.5% glial cells [2].
动物实验	MCF-7 cells were suspended in culture medium (no serum) and inoculated s.c. into the flank of adult female nude mice (0.1 ml/approximately 5 x 10^6 cells). Mice were maintained in a clean environment and were given sterile food and water. Estrogen supplementation was provided by ethynyl estradiol at 1 μg/ml in the water. Antiestrogen treatment was initiated when tumor diameter attained a minimum of 0.5 cm. The Br10 tumor at passage 49 was established by implantation of 1-2-mm^3 tumor fragments into the flank of anesthetized intact adult female nude mice. After 3 passages a reproducible pattern of growth was established without additional estrogen supplementation. Approximately two-thirds of animals established progressively growing tumors which attained measurable size (area, ≥70 mm2) after 6-7 weeks. Antiestrogen treatment was initiated at the time of transplantation. Tamoxifen was administered once daily p.o. at a dose of 10 mg/kg (1 ml/100 g body weight of aqueous dispersion in 0.5% Tween 80) and ICI 182,780 as a single s.c. injection of 5 mg/mouse (50 mg/ml in arachis oil). Tumor size was assessed weekly as the product of caliper measurements of the largest diameter and the axis perpendicular to it [1].

别名	ZM 182780, 氟维司群, ZD 9238, ICI 182780
化合物与蛋白结合的复合物	Crystal structure of human soluble epoxide hydrolase complexed with fulvestrant
分子量	606.77
分子式	C32H47F5O3S
CAS No.	129453-61-8

存储

Powder: -20°C for 3 years | In solvent: -80°C for 2 years

溶解度

Ethanol: 30.3 mg/mL (50 mM)

DMSO: 60.7 mg/mL (100 mM)

( < 1 mg/mL refers to the product slightly soluble or insoluble )

参考文献

1. Wakeling AE, et al. A potent specific pure antiestrogen with clinical potential. Cancer Res. 1991 Aug 1;51(15):3867-73. 2. Huynh H, et al. Regulation of insulin-like growth factor I receptor expression by the pure antiestrogen ICI 182780. Clin Cancer Res. 1996 Dec;2(12):2037-42. 3. Zhao L, et al. Estrogenic agonist activity of ICI 182,780 (Faslodex) in hippocampal neurons: implications for basic science understanding of estrogen signaling and development of estrogen modulators with a dual therapeutic profile. J Pharmacol Exp Ther. 2006 Dec;319(3):1124-32. 4. Fernandes SA, et al. The anti-oestrogen fulvestrant (ICI 182,780) reduces the androgen receptor expression, ERK1/2 phosphorylation and cell proliferation in the rat ventral prostate. Int J Androl. 2011 Oct;34(5 Pt 1):486-500. 5. Chen D, Tan Y, Li Z, et al. Organoid cultures derived from patients with papillary thyroid cancer[J]. The Journal of Clinical Endocrinology & Metabolism. 2021, 106(5): 1410-1426. 6. Chen D, Tan Y, Li Z, et al. Organoid cultures derived from patients with papillary thyroid cancer[J]. The Journal of Clinical Endocrinology & Metabolism. 2021 7. Zhao Z, Xue F, Gu Y, et al. Crosstalk between the muscular estrogen receptor α and BDNF/TrkB signaling alleviates metabolic syndrome via 7, 8-dihydroxyflavone in female mice[J]. Molecular Metabolism. 2020: 101149.

文献引用

1. Yang R, Wang X, Wang J, et al. Insights into the sex-dependent reproductive toxicity of 2-ethylhexyl diphenyl phosphate on zebrafish (Danio rerio). Environment International. 2022, 158: 106928. 2. Zhao Z, Xue F, Gu Y, et al. Crosstalk between the muscular estrogen receptor α and BDNF/TrkB signaling alleviates metabolic syndrome via 7, 8-dihydroxyflavone in female mice. Molecular Metabolism. 2020: 101149. 3. Chen D, Tan Y, Li Z, et al. Organoid cultures derived from patients with papillary thyroid cancer. The Journal of Clinical Endocrinology & Metabolism. 2021 Apr 23;106(5):1410-1426. doi: 10.1210/clinem/dgab020. 4. Wang, Zixiang, et al. EVI1 overexpression promotes ovarian cancer progression by regulating estrogen signaling. Molecular and Cellular Endocrinology. (2021): 111367. 5. Xiao Y, Chen D. ERα, but not ERβ and GPER, Mediates Estradiol‑Induced Secretion of TSH in Mouse Pituitary. Applied Biochemistry and Biotechnology. 2022: 1-11 6. Huang C S, Deng H F, Zhou L, et al.Undesirable ER stress induced by bavachin contributed to follicular atresia in zebrafish ovary.Biomedicine & Pharmacotherapy.2023, 166: 115322. 7. Cui S, Suo N, Yang Y, et al.The aminosteroid U73122 promotes oligodendrocytes generation and myelin formation.Acta Pharmacologica Sinica.2023: 1-12.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

bottom

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Fulvestrant 129453-61-8 Apoptosis Autophagy Endocrinology/Hormones Estrogen/progestogen Receptor Estrogen Receptor/ERR ZM 182780 氟维司群 ICI-182780 ICI182780 ZD-9238 ZD 9238 Inhibitor inhibit ZD9238 ZM-182780 ICI 182780 ZM182780 inhibitor

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Fulvestrant

存储

溶解度

参考文献

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剂量换算

体内实验配液计算器

计算器

输入分子式，点击计算，可计算出产品的分子量。

技术支持

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