氟维司群 T2146

Product Introduction
Bioactivity


英文名: Fulvestrant

描述: 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，诱导细胞凋亡和自噬。

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].

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]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: 5% DMSO+95% Saline : 3.04 mg/mL (5 mM, suspension)
Ethanol : 30.3 mg/mL (50 mM)
DMSO : 45 mg/mL (74.16 mM)


关键字: Estrogen Receptor/ERR | Inhibitor | Autophagy | ICI-182780 | inhibit | ZM182780 | Fulvestrant | ZD9238 | Apoptosis | ICI182780 | ZM-182780 | ZD-9238

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相关库: Approved Drug Library | Anti-Breast Cancer Compound Library | Anti-Cancer Drug Library | Anti-Lung Cancer Compound Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Pediatric Drug Library | Anti-Cancer Approved Drug Library | Anti-Cancer Active Compound Library | EMA Approved Drug Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途