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  • 氟维司群|T2146

氟维司群|T2146

Fulvestrant
129453-61-8
￥112 1mg 起订
￥198 5mg 起订
￥289 10mg 起订
上海 更新日期：2024-12-02

TargetMol中国（陶术生物）

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联系人：邵小姐
电话：021-021-33632979拨打
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邮箱：marketing@targetmol.com

产品详情:

中文名称：
氟维司群
英文名称：
Fulvestrant
CAS号：
129453-61-8
品牌：
TargetMol
产地：
美国
保存条件：
keep away from direct sunlight,keep away from moisture,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
纯度规格：
99.87%
产品类别：
抑制剂
货号：
T2146

Product Introduction

Bioactivity

名称Fulvestrant
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.
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keep away from direct sunlight,keep away from moisture,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度Ethanol : 30.3 mg/mL (50 mM)
DMSO : 45 mg/mL (74.16 mM)
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 6.07 mg/mL (10 mM), Suspension. Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
关键字Estrogen Receptor/ERR | Inhibitor | Autophagy | ICI-182780 | inhibit | ZM182780 | Fulvestrant | ZD9238 | Apoptosis | ICI182780 | ZM-182780 | ZD-9238
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氟维司群|||ZM 182780|||ZD 9238|||ICI 182780|TargetMol

公司简介

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。 从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。 经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期 (12年)
注册资本 566.2651万人民币
员工人数 100-500人
年营业额 ￥ 1亿以上
经营模式 贸易,试剂,定制,服务
主营行业 化学试剂,生物活性小分子

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