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  3. Fulvestrant

Fulvestrant (Synonyms: ICI 182780; ZD 9238; ZM 182780)

製品番号: HY-13636 純度: 99.99%
取扱説明書

Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. 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.

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Fulvestrant 構造式

Fulvestrant 構造式

CAS 番号 : 129453-61-8

容量 価格(税別) 在庫状況 数量
無料サンプル (0.5-1 mg)   今すぐ申し込む  
10 mM * 1 mL in DMSO USD 66 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 60 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 151 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 276 在庫あり
Estimated Time of Arrival: December 31
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

カスタマーレビュー

Based on 28 publication(s) in Google Scholar

Other Forms of Fulvestrant:

Top Publications Citing Use of Products

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

    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.

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

    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.

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    製品説明

    Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. 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]

    体外実験

    Fulvestrant (ICI 182780; ZD 9238; ZM 182780) is a potent and specific inhibitor of estrogen action and demonstrates excellent growth-inhibitory effects in both cell and animal models of human breast cancer. Fulvestrant inhibits MCF-7 human breast cancer cells growth with IC50 of 290 nM. The relative binding affinities of Fulvestrant is 0.89. Fulvestrant has significantly increased antiestrogenic potency and retains pure estrogen antagonist activity[1]. Fulvestrant is the first of a new type of endocrine treatment-an oestrogen receptor (ER) antagonist that downregulates the ER[3]. Treatment of MCF-7 cells with 1 µM ICI 47699 has no effect on the expression of ERα, whereas 100 nM Fulvestrant completely inhibits ERα expression[4].

    体内実験

    When administered alone, parenterally (s.c.), to immature female rats Fulvestrant (ICI 182,780) is devoid of uterotropic activity. Complete antagonism of Estrogen action is achieved with a dose of 0.5 mg Fulvestrant/kg/day s.c. The effects of Fulvestrant administered p.o. are qualitatively similar but potency is reduced by an order of magnitude compare with s.c. dosing (ED50 0.46 and complete antagonism at 5 mg/kg/day p.o.)[1]. The anti-tumor activity of Fulvestrant is first demonstrated in two models of human breast cancer in nude mice. In one of these models, the growth of MCF-7 tumor xenografts is completely blocked for at least 4 weeks following a single injection of Fulvestrant 5 mg. Similar reductions in growth are seen in the Br10 human tumor model. In other studies in nude mice bearing MCF-7 xenografts, Fulvestrant suppresses the growth of established tumours for twice as long and tumor growth is delayed to a greater extent than is observed with ICI 47699 treatment. ICI 47699-resistant breast tumors, which grow in nude mice after long-term treatment with ICI 47699, remain ensitive to growth inhibition by Fulvestrant[3]. These are comparable to the tumor growth inhibition (TGI) observed for ICI 47699 and Fulvestrant, which on day 40 are 86 and 88%, respectively[4].

    臨床実験
    分子量

    606.77

    分子式

    C₃₂H₄₇F₅O₃S

    CAS 番号

    129453-61-8

    SMILES

    C[[email protected]@]12[[email protected]@H](O)CC[[email protected]@]1([H])[[email protected]]3([H])[[email protected]](CCCCCCCCCS(CCCC(F)(F)C(F)(F)F)=O)CC4=C(C=CC(O)=C4)[[email protected]@]3([H])CC2

    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : ≥ 29 mg/mL (47.79 mM)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    10 mM 0.1648 mL 0.8240 mL 1.6481 mL
    *Please refer to the solubility information to select the appropriate solvent.
    体内:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: 2.5 mg/mL (4.12 mM); Suspended solution; Need ultrasonic

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (4.12 mM); Suspended solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (4.12 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    参考文献
    細胞実験
    [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 はこれらの方法の精度を確認していません。 こちらは参照専用です。

    動物実験
    [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 はこれらの方法の精度を確認していません。 こちらは参照専用です。

    参考文献

    純度: 99.99%

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    Keywords:

    FulvestrantICI 182780ZD 9238ZM 182780ICI182780ICI-182780ZD9238ZD-9238ZM182780ZM-182780Estrogen Receptor/ERRAutophagyApoptosisInhibitorinhibitorinhibit

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    製品名:
    Fulvestrant
    製品番号:
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