1. Vitamin D Related/Nuclear Receptor Autophagy Apoptosis
  2. Estrogen Receptor/ERR Autophagy Apoptosis
  3. Fulvestrant

Fulvestrant  (Synonyms: 氟维司群; ICI 182780; ZD 9238; ZM 182780)

目录号: HY-13636 纯度: 99.92%
COA 产品使用指南

Fulvestrant (ICI 182780) 是一种纯抗雌激素,也是一种有效的雌激素受体 (ER) 拮抗剂,IC50 为 9.4 nM。Fulvestrant 还是一种 GPR30 的激动剂。Fulvestrant 有效抑制 ER 阳性 MCF-7 细胞的生长,IC50 为 0.29 nM。Fulvestrant 还可诱导细胞自噬 (autophagy) 和凋亡 (apoptosis),并具有抗肿瘤功效。

MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Fulvestrant Chemical Structure

Fulvestrant Chemical Structure

CAS No. : 129453-61-8

1.  客户无需承担相应的运输费用。

2.  同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥506
In-stock
5 mg ¥248
In-stock
10 mg ¥361
In-stock
50 mg ¥950
In-stock
100 mg ¥1650
In-stock
500 mg ¥3690
In-stock
1 g ¥5850
In-stock
5 g   询价  
10 g   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Fulvestrant:

MCE 顾客使用本产品发表的 86 篇科研文献

WB

    Fulvestrant purchased from MCE. Usage Cited in: J Mol Med (Berl). 2019 Apr;97(4):541-552.  [Abstract]

    HK-2 cells treated with genistein (15 μM) and/or TGFβ (5 ng/ml) for 24 h are assayed with anti-acetylated and anti-total histone 3 antibodies byWestern blot. In a separate assay, cell lysates treated with TGFβ and genistein in the presence or absence of fulvestrant (Fulvest, 1 μM) under the same condition were also assayed. The quantifications are presented underneath the blots based on three independent experiments.

    Fulvestrant purchased from MCE. Usage Cited in: Biochem Cell Biol. 2018 Oct;96(5):672-681.  [Abstract]

    Rutin increases ERα and ERβ levels in both hippocampus and cerebral cortex. Western blotting is performed to measure the levels of ERα and ERβ in hippocampus and cerebral cortex. β-actin is used as an internal control.

    查看 Estrogen Receptor/ERR 亚型特异性产品:

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy[1].

    IC50 & Target

    IC50: 9.4 nM (Estrogen Receptor)[1]

    体外研究
    (In Vitro)

    FuLvestrant (ICI 182780;ZD 9238;ZM 182780) 是一种有效且特异性的雌激素作用抑制剂,在人类乳腺癌细胞和动物模型中均表现出优异的生长抑制作用。FuLvestrant 抑制 MCF-7 人乳腺癌细胞的生长,IC50 为 0.29 nM。Fulvestrant 的相对结合亲和力为 0.89。FuLvestrant 具有显著增强的抗雌激素效力并保留纯雌激素拮抗剂活性[1]。Fulvestrant 是第一种新型内分泌处理药物——雌激素受体 (ER) 拮抗剂,可下调 ER[3]。用 1 μM ICI 47699 处理 MCF-7 细胞对 ERα 的表达没有影响,而 100 nM FuLvestrant 完全抑制 ERα 表达[4]

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

    体内研究
    (In Vivo)

    Fulvestrant (ICI 182,780) 单独给药时,肠胃外 (s.c.) 在未成熟的雌性大鼠中没有促子宫活性。
    Fulvestrant (0.5 mg/kg/day s.c) 显示出对雌激素作用的完全拮抗作用。
    Fulvestrant 口服给药 (5 mg/kg/day) 在性质上与皮下给药相似[1]
    在两种人类乳腺癌裸鼠模型中。 在其中一个模型中,Fulvestrant (5 mg) 在单次注射后完全阻断 MCF-7 肿瘤异种移植物的生长至少 4 周。
    在对携带 MCF-7 异种移植物的裸鼠进行的其他研究中,与使用 ICI 47699 治疗观察到的情况相比,Fulvestrant 抑制已建立肿瘤的生长时间是其两倍,并且肿瘤生长延迟的程度更大 [3]
    Fulvestrant 在第 40 天表现出 88% 的肿瘤生长抑制 (TGI)[4]

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

    Clinical Trial
    分子量

    606.77

    Formula

    C32H47F5O3S

    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    氟维司群;氟维司琼

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性数据
    细胞实验: 

    DMSO 中的溶解度 : 250 mg/mL (412.02 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.6481 mL 8.2404 mL 16.4807 mL
    5 mM 0.3296 mL 1.6481 mL 3.2961 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (4.12 mM); 悬浊液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的均匀悬浊液,悬浊液可用于口服和腹腔注射。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

      20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: 2.08 mg/mL (3.43 mM); 悬浊液; 超声助溶

      此方案可获得 2.08 mg/mL的均匀悬浊液,悬浊液可用于口服和腹腔注射。

      1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。

    以下溶解方案,请直接配制工作液。建议现用现配,在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比; 如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶。

    • 方案 一

      请依序添加每种溶剂: 15% Solutol HS 15    10% Cremophor EL    35% PEG400    40% Water

      Solubility: 2.5 mg/mL (4.12 mM); 悬浊液; 超声助溶

    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    请输入您的动物体内配方组成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.95%

    参考文献
    Cell Assay
    [3]

    MCF-7 or T47D cells are cultured in 10 cm dishes to ~75% confluence in EMEM growth medium. Twenty-four hours before treatment, the growth medium is replaced with phenol red-free RPMI-1640 growth medium. A stock solution of 10 mM RAD1901 is prepared in DMSO. Dilutions of RAD1901 are prepared in RPMI growth medium (doses ranging from 10 to 0.5 nM). Controls include 0.1% DMSO alone (vehicle), 100 nM Fulvestrant, and 1 µM ICI 47699. Plated cells are treated with RAD1901 or controls for 48 h, and then incubated for 15 min with ice-cold lysis buffer [1 mM EDTA, 0.5% Triton X-100, 5 mM NaF, 6 M urea, 1 mM sodium orthovanadate, 2.5 mM sodium pyrophosphate, and 1× HALT protease inhibitor cocktail]. Lysates are centrifuged at 2000g for 5 min, and the supernatant is diluted 1 : 1 in lysis buffer. Ninety-six-well plates are coated overnight with capture antibody (1 µg/mL), washed three times in the manufacturer’s wash buffer, blocked with blocking buffer for 2 h, and washed again. The prepared plates are incubated with 100 µL of the prepared cell lysate for 2 h, washed, incubated with biotinylated detection antibody for 2 h, and washed again. After a 20 min incubation with streptavidin-horseradish peroxidase, the plates are washed and incubated with substrate solution for 20 min. The reaction is stopped with stop solution, and the plates are analyzed on a microplate reader (OD450)[3].

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

    Animal Administration
    [1][3]

    Rats[1]
    In studies with OVX rats, surgical preparation is performed at least 2 weeks before treatment began. To measure the duration of action of a single large dose of Fulvestrant, OVX rats are treated with a daily s.c. dose of 0.5 μg of estradici benzoate beginning on the day of Fulvestrant administration and continued until vaginal smears showed evidence of cornification. At that point the experiment is terminated and uterine weight is recorded. The arachis oil formulation used in these single dose duration of action studies contained 50 mg Fulvestrant/mL.
    Mice[3]
    Female athymic nude mice [Crl:NU(NCr)-Foxn1nu] are used for tumor xenograft studies. Fourteen days after tumor cell implantation (designated as day 1 of the study), mice are 9 weeks of age, with body weights ranging from 21.4 to 32.5 g, individual tumor volumes ranging from 75 to 144 mm3, and a group mean tumor volume (MTV) of 108 mm3. The mice are randomized into nine groups of 15 animals each and treated with vehicle, ICI 47699 (1 mg/animal every other day), Fulvestrant (0.5 mg/animal daily), or RAD1901 (0.3, 1, 3, 10, 30, 60, 90, and 120 mg/kg daily). Tumor volumes are evaluated twice per week. The tumor endpoint is defined as an MTV of 1500 mm3 in the control group. Animals are also monitored for partial regression (PR) and complete regression responses.

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

    参考文献

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    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 0.8240 mL 1.6481 mL 4.1202 mL
    15 mM 0.1099 mL 0.5494 mL 1.0987 mL 2.7468 mL
    20 mM 0.0824 mL 0.4120 mL 0.8240 mL 2.0601 mL
    25 mM 0.0659 mL 0.3296 mL 0.6592 mL 1.6481 mL
    30 mM 0.0549 mL 0.2747 mL 0.5494 mL 1.3734 mL
    40 mM 0.0412 mL 0.2060 mL 0.4120 mL 1.0300 mL
    50 mM 0.0330 mL 0.1648 mL 0.3296 mL 0.8240 mL
    60 mM 0.0275 mL 0.1373 mL 0.2747 mL 0.6867 mL
    80 mM 0.0206 mL 0.1030 mL 0.2060 mL 0.5150 mL
    100 mM 0.0165 mL 0.0824 mL 0.1648 mL 0.4120 mL
    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.

    您最近查看的产品:

    Your information is safe with us. * Required Fields.

       产品名称:

     

    * 需求量:

    * 客户姓名:

     

    * Email:

    * 电话:

     

    * 公司或机构名称:

       留言给我们:

    Bulk Inquiry

    Inquiry Information

    产品名称:
    Fulvestrant
    目录号:
    HY-13636
    需求量: