首页 工具
登录
购物车
Fulvestrant

Fulvestrant

产品编号 T2146   CAS 129453-61-8
别名: 氟维司群, ZM 182780, ZD 9238, ICI 182780

Fulvestrant (ZM 182780) 是一种雌激素受体 (ER) 拮抗剂 (IC50=9.4 nM),也是一种 GPR30 的激动剂。Fulvestrant 具有抗肿瘤活性,可以抑制细胞增殖,诱导细胞凋亡自噬

TargetMol的所有产品和服务仅用于科学研究,不能被用于人体,我们也不向个人提供产品和服务。
Fulvestrant Chemical Structure
Fulvestrant, CAS 129453-61-8
规格 价格/CNY 货期 数量
1 mg ¥ 112 现货
5 mg ¥ 198 现货
10 mg ¥ 289 现货
25 mg ¥ 468 现货
50 mg ¥ 788 现货
100 mg ¥ 1,370 现货
200 mg ¥ 1,930 现货
500 mg ¥ 2,970 现货
1 g ¥ 4,870 现货
1 mL * 10 mM (in DMSO) ¥ 418 现货
产品目录号及名称: Fulvestrant (T2146)
点击图片重新获取验证码
选择批次  
纯度: 100%
纯度: 99.87%
纯度: 99.77%
纯度: 99.09%
更多批次查询请联系客服
生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Fulvestrant (ZM 182780) is an estrogen receptor (ER) antagonist (IC50=9.4 nM) and an agonist of GPR30. Fulvestrant has antitumor activity, inhibiting cell proliferation and inducing apoptosis and autophagy.
靶点活性 Estrogen Receptor:9.4 nM (cell free)
体外活性 方法:ER 阳性 MCF-7 和 ER 阴性 MDA-MB-231 细胞用 Fulvestrant (0.01-10000 nM) 处理 6 天,使用 crystal violet staining 检测细胞生长速率。
结果:Fulvestrant 抑制 MCF-7 细胞的生长,IC50 为 0.8 nM。Fulvestrant 不抑制 MDA-MB-231 细胞的生长,IC50 大于 1 µM。[1]
方法:人乳腺癌细胞 MCF-7 用 Fulvestrant (100 nM) 处理 0.25-6 h,使用 Western Blot 检测靶点蛋白表达水平。
结果:当 MCF-7 细胞暴露于 Fulvestrant 时,ERα 蛋白的表达以时间依赖的方式减少。[2]
体内活性 方法:为检测体内抗肿瘤活性,将 Fulvestrant (25-200 mg/kg,5% DMSO/95% corn oil) 皮下注射给携带 tamoxifen-resistant (TamR) 肿瘤的 Nu/J 小鼠,每周四次,持续四周。
结果:所有剂量的 Fulvestrant 对肿瘤生长的显著抑制,并且在剂量之间没有检测到显著差异。[3]
方法:为检测体内抗肿瘤活性,将 Fulvestrant (5 mg/mouse) 皮下注射给原位建立 ER+ 乳腺癌的裸鼠,每周两次,持续二十四天。
结果:Fulvestrant 治疗导致肿瘤生长显著降低。[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 氟维司群, ZM 182780, ZD 9238, ICI 182780
化合物与蛋白结合的复合物

T2146_1

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 1 year

溶解度

Ethanol: 30.3 mg/mL (50 mM)

DMSO: 60.7 mg/mL (100 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 1.6481 mL 8.2404 mL 16.4807 mL 41.2018 mL
5 mM 0.3296 mL 1.6481 mL 3.2961 mL 8.2404 mL
10 mM 0.1648 mL 0.824 mL 1.6481 mL 4.1202 mL
20 mM 0.0824 mL 0.412 mL 0.824 mL 2.0601 mL
50 mM 0.033 mL 0.1648 mL 0.3296 mL 0.824 mL
DMSO 100 mM 0.0165 mL 0.0824 mL 0.1648 mL 0.412 mL

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
=
X
X
X
=
X
=
/
g/mol

输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Nukatsuka M, et al. Estrogen Down-regulator Fulvestrant Potentiates Antitumor Activity of Fluoropyrimidine in Estrogen-responsive MCF-7 Human Breast Cancer Cells. In Vivo. 2019 Sep-Oct;33(5):1439-1445. 2. Nukatsuka M, et al. Estrogen Down-regulator Fulvestrant Potentiates Antitumor Activity of Fluoropyrimidine in Estrogen-responsive MCF-7 Human Breast Cancer Cells. In Vivo. 2019 Sep-Oct;33(5):1439-1445. 3. Wardell SE, et al. Pharmacokinetic and pharmacodynamic analysis of fulvestrant in preclinical models of breast cancer to assess the importance of its estrogen receptor-α degrader activity in antitumor efficacy. Breast Cancer Res Treat. 2020 Jan;179(1):67-77. 4. Abrahamsson A, et al. Fulvestrant-Mediated Attenuation of the Innate Immune Response Decreases ER+ Breast Cancer Growth In Vivo More Effectively than Tamoxifen. Cancer Res. 2020 Oct 15;80(20):4487-4499. 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.
Columbianadin Solamargine Triptolide Tubulin polymerization-IN-43 Cyasterone Moexipril hydrochloride AKT inhibitor VIII Ro-3306

相关化合物库

该产品包含在如下化合物库中:
抗癌活性化合物库 抗癌临床化合物库 抗癌药物库 抗癌上市药物库 抗癌化合物库 抑制剂库 自噬库 抗肺癌化合物库 抗卵巢癌化合物库 NO PAINS 化合物库

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
g
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
计算 重置

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 Receptor/ERR Estrogen/progestogen Receptor 氟维司群 Inhibitor ICI-182780 ZM 182780 inhibit ZM182780 ZD9238 ICI182780 ZM-182780 ZD-9238 ZD 9238 ICI 182780 inhibitor

 

陶术
生物
TargetMol®中国区唯一合作伙伴
点击进入陶术生物官网陶术生物
联系我们
400-820-0310

上海市静安区江场三路238号8楼