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Fulvestrant

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Fulvestrant is a selective estrogen receptor down-regulator (SERD) used as a laboratory reagent. It functions by competitively binding to the estrogen receptor, leading to its degradation and depletion. This action inhibits the transcriptional activity of the estrogen receptor.

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Lab products found in correlation

Azd9496, by MedChemExpress (3 mentions) Tamoxifen treatment pellets, by Innovative Research (2 mentions) Gdc0810, by MedChemExpress (2 mentions) Er hc 20 or h184, by Santa Cruz Biotechnology (2 mentions) Actin a5441, by Merck Group (2 mentions) Vinculin 13901, by Cell Signaling Technology (2 mentions) Estradiol, by Merck Group (2 mentions) Bazedoxifene, by MedChemExpress (2 mentions) Tamoxifen, by MedChemExpress (2 mentions) Tamoxifen, by Merck Group (2 mentions) Palbociclib, by MedChemExpress (2 mentions) Pelp1 antibody a300 180a, by Fortis Life Sciences (2 mentions) Zr 75, by American Type Culture Collection (2 mentions) β estradiol, by MedChemExpress (1 mentions) Azd7762, by Merck Group (1 mentions) Nu7441, by Selleck Chemicals (1 mentions) Bazedoxifene, by Selleck Chemicals (1 mentions) Lasofoxifene, by Merck Group (1 mentions) Estradiol e2, by Merck Group (1 mentions) Azd9496, by Selleck Chemicals (1 mentions)

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Fulvestrant from (2 citations)

14 protocols using fulvestrant

1

Evaluating Endocrine Therapies in Breast Cancer

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Tamoxifen treatment pellets were purchased from Innovative Research of America. Fulvestrant, AZD9496, GDC0810, and bazedoxifene were purchased from MedChemExpress. Estradiol was purchased from Sigma-Aldrich, Inc. Antibodies used for immunoblot detection included the following: estrogen receptor (ER) - HC-20 or H184, Santa Cruz Biotechnology; actin - A5441, Sigma-Aldrich, Inc.; vinculin – 13901S, Cell signaling.
Wardell S.E., Yllanes A.P., Chao C.A., Bae Y., Andreano K.J., Desautels T.K., Heetderks K.A., Blitzer J.T., Norris J.D, & McDonnell D.P. (2019). Pharmacokinetic and pharmacodynamic analysis of fulvestrant in preclinical models of breast cancer to assess the importance of its estrogen receptor-α degrader activity in antitumor efficacy. Breast Cancer Research and Treatment, 179(1), 67-77.
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2

Endogenous Steroid-Free Cell Culture

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To remove the confounding effects of endogenous steroids, ADS_Eu_ESC, ADS_Ec_ESC and IshikawaER+ cells were cultured in phenol red-free DMEM/f12 medium for 48 h before drug treatment. Subsequently, cells were incubated in fresh medium (as control), β-E2 (10nM, Sigma, USA), Fulvestrant (10 nM, ICI 182780, a selective ER antagonist, MedChem Express, USA) or β-E2 plus Fulvestrant for 24 h.
Wang Y.Y., Duan H., Wang S., Quan Y.J., Huang J.H, & Guo Z.C. (2021). Upregulated Talin1 synergistically boosts β-estradiol-induced proliferation and pro-angiogenesis of eutopic and ectopic endometrial stromal cells in adenomyosis. Reproductive Biology and Endocrinology : RB&E, 19, 70.
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3

Estrogen Receptor Modulation Assay

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Tamoxifen treatment pellets were purchased from Innovative Research of America. Fulvestrant, AZD9496, GDC0810, and bazedoxifene were purchased from MedChemExpress. Estradiol was purchased from Sigma-Aldrich, Inc. Antibodies used for immunoblot detection included the following: estrogen receptor (ER)—HC-20 or H184, Santa Cruz Biotechnology; actin—A5441, Sigma-Aldrich, Inc.; vinculin—13901S, Cell Signaling.
Wardell S.E., Yllanes A.P., Chao C.A., Bae Y., Andreano K.J., Desautels T.K., Heetderks K.A., Blitzer J.T., Norris J.D, & McDonnell D.P. (2019). Pharmacokinetic and pharmacodynamic analysis of fulvestrant in preclinical models of breast cancer to assess the importance of its estrogen receptor-α degrader activity in antitumor efficacy. Breast Cancer Research and Treatment, 179(1), 67-77.
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4

Evaluating Estrogen Receptor Modulators

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Tamoxifen was obtained from MedChemExpress (HY-13757A). Fulvestrant was obtained from MedChemExpress (HY-13636). AZD9496 was obtained from MedChemExpress (HY-12870). NU7441, an inhibitor of DNA protein kinase catalytic subunit (DNAPKcs), was obtained from Selleckchem (Ku-57788). AZD7762, an inhibitor of Chk1/2, was purchased from Sigma (SML0350). β-estradiol was obtained from MedChemExpress (HY-B0141). All compounds were solubilized in DMSO.
Michmerhuizen A.R., Lerner L.M., Pesch A.M., Ward C., Schwartz R., Wilder-Romans K., Liu M., Nino C., Jungles K., Azaria R., Jelley A., Zambrana Garcia N., Harold A., Zhang A., Wharram B., Hayes D.F., Rae J.M., Pierce L.J, & Speers C.W. (2022). Estrogen receptor inhibition mediates radiosensitization of ER-positive breast cancer models. NPJ Breast Cancer, 8, 31.
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5

Comparative Evaluation of Selective ER Modulators

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Fulvestrant (CAS No: 129453–61-8, > 99% purity) was purchased from MedChem Express. Estradiol (E2) (E8875), lasofoxifene (SML1026), 4-hydroxytamoxifen (H7904), and tamoxifen (T5648) were purchased from Sigma. Raloxifene (2280) was purchased from Tocris. GDC-0810 (S7855), bazedoxifene (S2128), and AZD9496 (S8372) were purchased from Selleckchem. GW5638 (5638), GW7604 (7604), and RU 58,668 (RU) were provided by Donald McDonnell (Duke University). G1T48 was provided by G1 Therapeutics, Inc., as analytical grade compound.
Andreano K.J., Wardell S.E., Baker J.G., Desautels T.K., Baldi R., Chao C.A., Heetderks K.A., Bae Y., Xiong R., Tonetti D.A., Gutgesell L.M., Zhao J., Sorrentino J.A., Thompson D.A., Bisi J.E., Strum J.C., Thatcher G.R, & Norris J.D. (2020). G1T48, an oral selective estrogen receptor degrader, and the CDK4/6 inhibitor lerociclib inhibit tumor growth in animal models of endocrine-resistant breast cancer. Breast Cancer Research and Treatment, 180(3), 635-646.
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6

Evaluating Dose-Dependent Responses to Pharmacological Agents

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The dose and conditions of multiple agents were as follows: ART (Sigma, United States) was dissolved in PBS with a final working concentration of 0–30 μg/mL for 0–6 days; Fulvestrant (MedChemExpress, United States) was dissolved in DMSO and treated cells at the dose of 250 nM; 10 nM of estrogen (Sigma, United States) was diluted using PBS. Pim1/AKK1-IN-1 (380 nM in DMSO, MedChemExpress, United States) was performed to treat cells. After 4 days, the cells were collected for further study.
Yin X., Liu Y., Qin J., Wu Y., Huang J., Zhao Q., Dang T., Tian Y., Yu P, & Huang X. (2021). Artesunate Suppresses the Proliferation and Development of Estrogen Receptor-α-Positive Endometrial Cancer in HAND2-Dependent Pathway. Frontiers in Cell and Developmental Biology, 8, 606969.
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7

Drug Sensitivity Assay for Patient-Derived Samples

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Spheroids derived from the human patient’s core-needle biopsy sample or CTCs were cultured for drug tests. Anti-cancer drugs, including epirubicin, 5-fluorouracil (5-FU), fulvestrant, gemcitabine, paclitaxel, palbociclib, vinorelbine, carboplatin, eribulin, and doxorubicin, were purchased from MedChemExpress, and treated at a dose of 0.1, 0.3, 1 or 3 Cmax. All drugs were dissolved in DMSO, which were further diluted in media containing 10% FBS (final [DMSO] ≤ 0.25% (v/v)). Cell viability was measured using RealTime-Glo TM Cell Viability Assay, following the manufacturer’s protocol (Promega). Relative cell viability was calculated by comparing the absolute luminescence intensity before (at time 0) and after (24, 48, and 72 h) drug treatment and was used to determine the effectiveness of the chemotherapeutic drug.
Chen J.Y., Chou H.H., Lim S.C., Huang Y.J., Lai K.C., Guo C.L., Tung C.Y., Su C.T., Wang J., Liu E., Han H.F., Yeh P.Y., Hu C.M., Dunn A.R., Frank C.W., Wu Y.C., Yang M.H, & Chang Y.C. (2022). Multiomic characterization and drug testing establish circulating tumor cells as an ex vivo tool for personalized medicine. iScience, 25(10), 105081.
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8

Cell Viability Assay for Combination Therapy

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In cell viability assay, 4000 cells per well were planted in 96-well plates and cells were exposed to different concentrations of agents in the following day. After 48-hour treatment, cell survival was assessed with the Cell Counting kit-8 in according to the recommended guideline (KeyGEN Biotech, Nanjing, China). Combination index (CI) values were calculated using CompuSyn software (ComboSyn, Inc., NJ, USA).
Palbociclib, Ribociclib, Abemaciclib, enzalutamide, Fulvestrant and Dihydrotestosterone (DHT) were obtained from MedChem Express, and Palbociclib was diluted in sterile water, DHT was dissolved in ethanol and others above were diluted in DMSO.
Ji W., Shi Y., Wang X., He W., Tang L., Tian S., Jiang H., Shu Y, & Guan X. (2019). Combined Androgen receptor blockade overcomes the resistance of breast cancer cells to palbociclib. International Journal of Biological Sciences, 15(3), 522-532.
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9

Estrogen-Modulated Liver Cell Culture

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L02 cells (normal human liver cells) were purchased from the American Type Culture Collection (ATCC). L02 cells were cultured in high-glucose DMEM, phenol red free DMEM (PRF DMEM) medium (HyClone) containing 10% fetal bovine serum (FBS) or estrogen charcoal-stripped FBS (CS FBS), and 1% penicillin/streptomycin (100 μg ml−1) at a constant temperature (37 °C) in a humidified incubator (5% CO2). To ensure that the experimental results were not influenced by exogenous estrogen levels, PRF DMEM medium and CS FBS were used in our experiments that were conducted in preparation of CS FBS and was followed based on a prior work (de Faria et al. 2016 (link); Simoncini et al. 2005 (link)). Fulvestrant (ICI 182780, MedChemExpress, 100 nM) was used for estrogen receptor inhibition. L02 cells were exposed to lentivirus (LV)-HNF1b (Genechem Co., Ltd., Shanghai) or LV-shPPARγ (TianYuCheng Co., Ltd., Xi’an) for 12 h and then selected with puromycin (BioFroxx, Germany) for 12 h to establish a cell line with stable overexpression of HNF1b. L02 cells were treated with 1 or 10 μM BPA for 48 h.
Long Z., Fan J., Wu G., Liu X., Wu H., Liu J., Chen Y., Su S., Cheng X., Xu Z., Su H., Cao M., Zhang C., Hai C, & Wang X. (2020). Gestational bisphenol A exposure induces fatty liver development in male offspring mice through the inhibition of HNF1b and upregulation of PPARγ. Cell Biology and Toxicology, 37(1), 65-84.
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10

Stem Cell Culture and Characterization

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α-Minimum Essential Medium, high-sugar Dulbecco Modified Eagle Medium (H-DMEM), and fetal bovine serum (FBS) were purchased from Gibco (Grand Island, NY). ASA VI was purchased from PuYi (Nanjing, Jiangsu, China) and fulvestrant (estrogen receptor antagonist) was purchased from MedChemExpress (Monmouth Junction, NJ). Anti-CD44-PE, anti-CD31-PE, anti-CD73-PE, and anti-CD45-PE were purchased from SinoBiological (Beijing, China), and the reverse transcription kit was purchased from Axygen (San Francisco, CA). The alkaline phosphatase (ALP) assay kit was purchased from Jiancheng (Nanjing, Jiangsu, China).
Niu J., Wang Y., Meng Y., Qi W, & Wen J. (2022). Asperosaponin VI induces osteogenic differentiation of human umbilical cord mesenchymal stem cells via the estrogen signaling pathway. Medicine, 101(50), e32344.
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