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  3. Fulvestrant

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

Cat. No.: HY-13636 Purity: 99.99%
Handling Instructions

Fulvestrant is a potent Estrogen Receptor antagonist with an IC50 of 9.4 nM.

For research use only. We do not sell to patients.

Fulvestrant Chemical Structure

Fulvestrant Chemical Structure

CAS No. : 129453-61-8

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10 mM * 1 mL in DMSO USD 66 In-stock
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Customer Review

Based on 9 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.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Fulvestrant is a potent Estrogen Receptor antagonist with an IC50 of 9.4 nM.

    IC50 & Target

    IC50: 9.4 nM (Estrogen Receptor)[1]

    In Vitro

    Fulvestrant (ICI 182,780) 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 compare with that of Estradiol. 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[2]. Treatment of MCF-7 cells with 1 µM Tamoxifen has no effect on the expression of ERα, whereas 100 nM Fulvestrant completely inhibits ERα expression[3].

    In Vivo

    When administered alone, parenterally (s.c.), to immature female rats Fulvestrant (ICI 182,780) is devoid of uterotropic activity and, when coadministered with Estradiol, it effectively blocks the uterotropic action of Estradiol in a dose-dependent manner (ED50: 0.06 mg/kg/day s.c.). 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 antitumour 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 tumour xenografts, supported by continuous treatment with oestradiol, 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 tumour model. In other studies in nude mice bearing MCF-7 xenografts, Fulvestrant suppresses the growth of established tumours for twice as long and tumour growth is delayed to a greater extent than is observed with Tamoxifen treatment. Tamoxifen-resistant breast tumours, which grow in nude mice after long-term treatment with Tamoxifen, remain ensitive to growth inhibition by Fulvestrant[2]. These are comparable to the tumor growth inhibition (TGI) observed for Tamoxifen and Fulvestrant, which on day 40 are 86 and 88%, respectively[3].

    Clinical Trial
    Storage

    4°C, protect from light

    Solvent & Solubility
    In Vitro: 

    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.
    In Vivo:
    • 1.

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

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

    • 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    40% PEG300    5% Tween-80    45% saline

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

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [3]

    MCF-7 or T47D cells are cultured in 10 cm dishes to ~75% confluence in EMEM growth medium supplemented with 10% FBS and 10 µg/mL human insulin. 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), 1 nM Estradiol (E2), 100 nM Fulvestrant, and 1 µM Tamoxifen. 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, Tamoxifen (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.

    References
    Molecular Weight

    606.77

    Formula

    C₃₂H₄₇F₅O₃S

    CAS No.

    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

    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 99.99%

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    Product Name:
    Fulvestrant
    Cat. No.:
    HY-13636
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    Cat. No.: HY-13636