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Fulvestrant

Catalog No. T2146   CAS 129453-61-8
Synonyms: ZM 182780, ZD 9238, ICI 182780

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.

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Fulvestrant Chemical Structure
Fulvestrant, CAS 129453-61-8
Pack Size Availability Price/USD Quantity
10 mg In stock $ 42.00
25 mg In stock $ 67.00
50 mg In stock $ 118.00
100 mg In stock $ 198.00
200 mg In stock $ 297.00
500 mg In stock $ 565.00
1 g In stock $ 789.00
1 mL * 10 mM (in DMSO) In stock $ 52.00
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Purity: 100%
Purity: 99.87%
Purity: 99.77%
Purity: 99.09%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description 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.
Targets&IC50 Estrogen Receptor:9.4 nM (cell free)
In vitro METHODS: ER-positive MCF-7 and ER-negative MDA-MB-231 cells were treated with Fulvestrant (0.01-10000 nM) for 6 days, and the cell growth rate was measured by crystal violet staining.
RESULTS: Fulvestrant inhibited the growth of MCF-7 cells with an IC50 of 0.8 nM. Fulvestrant did not inhibit the growth of MDA-MB-231 cells with an IC50 greater than 1 µM. [1]
METHODS: Human breast cancer cells MCF-7 were treated with Fulvestrant (100 nM) for 0.25-6 h, and the expression levels of target proteins were detected by Western Blot.
RESULTS: ERα protein expression was reduced in a time-dependent manner when MCF-7 cells were exposed to Fulvestrant. [2]
In vivo METHODS: To assay anti-tumor activity in vivo, Fulvestrant (25-200 mg/kg, 5% DMSO/95% corn oil) was injected subcutaneously four times per week for four weeks into Nu/J mice bearing tamoxifen-resistant (TamR) tumors.
RESULTS: Significant inhibition of tumor growth was observed at all doses of Fulvestrant, and no significant differences were detected between doses. [3]
METHODS: To assay anti-tumor activity in vivo, Fulvestrant (5 mg/mouse) was injected subcutaneously into nude mice with in situ established ER+ mammary carcinomas twice weekly for twenty-four days.
RESULTS: Fulvestrant treatment resulted in a significant reduction in tumor growth. [4]
Cell Research 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].
Animal Research 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].
Synonyms ZM 182780, ZD 9238, ICI 182780
Molecular Weight 606.77
Formula C32H47F5O3S
CAS No. 129453-61-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 30.3 mg/mL (50 mM)

DMSO: 60.7 mg/mL (100 mM)

TargetMolReferences and Literature

1. Nukatsuka M, et al. Estrogen Down-regulator Fulvestrant Potentiates Antitumor Activity of Fluoropyrimidine in Estrogen-responsive MCF-7 Human Breast Cancer Cells. In Vivo. 2019 Sep-Oct;33(5):1439-1445. 2. Nukatsuka M, et al. Estrogen Down-regulator Fulvestrant Potentiates Antitumor Activity of Fluoropyrimidine in Estrogen-responsive MCF-7 Human Breast Cancer Cells. In Vivo. 2019 Sep-Oct;33(5):1439-1445. 3. Wardell SE, et al. 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 Res Treat. 2020 Jan;179(1):67-77. 4. Abrahamsson A, et al. Fulvestrant-Mediated Attenuation of the Innate Immune Response Decreases ER+ Breast Cancer Growth In Vivo More Effectively than Tamoxifen. Cancer Res. 2020 Oct 15;80(20):4487-4499. 5. Chen D, Tan Y, Li Z, et al. Organoid cultures derived from patients with papillary thyroid cancer[J]. The Journal of Clinical Endocrinology & Metabolism. 2021, 106(5): 1410-1426. 6. Chen D, Tan Y, Li Z, et al. Organoid cultures derived from patients with papillary thyroid cancer[J]. The Journal of Clinical Endocrinology & Metabolism. 2021 7. Zhao Z, Xue F, Gu Y, et al. Crosstalk between the muscular estrogen receptor α and BDNF/TrkB signaling alleviates metabolic syndrome via 7, 8-dihydroxyflavone in female mice[J]. Molecular Metabolism. 2020: 101149.

TargetMolCitations

1. Yang R, Wang X, Wang J, et al. Insights into the sex-dependent reproductive toxicity of 2-ethylhexyl diphenyl phosphate on zebrafish (Danio rerio). Environment International. 2022, 158: 106928. 2. Zhao Z, Xue F, Gu Y, et al. Crosstalk between the muscular estrogen receptor α and BDNF/TrkB signaling alleviates metabolic syndrome via 7, 8-dihydroxyflavone in female mice. Molecular Metabolism. 2020: 101149. 3. Chen D, Tan Y, Li Z, et al. Organoid cultures derived from patients with papillary thyroid cancer. The Journal of Clinical Endocrinology & Metabolism. 2021 Apr 23;106(5):1410-1426. doi: 10.1210/clinem/dgab020. 4. Wang, Zixiang, et al. EVI1 overexpression promotes ovarian cancer progression by regulating estrogen signaling. Molecular and Cellular Endocrinology. (2021): 111367. 5. Xiao Y, Chen D. ERα, but not ERβ and GPER, Mediates Estradiol‑Induced Secretion of TSH in Mouse Pituitary. Applied Biochemistry and Biotechnology. 2022: 1-11 6. Huang C S, Deng H F, Zhou L, et al.Undesirable ER stress induced by bavachin contributed to follicular atresia in zebrafish ovary.Biomedicine & Pharmacotherapy.2023, 166: 115322. 7. Cui S, Suo N, Yang Y, et al.The aminosteroid U73122 promotes oligodendrocytes generation and myelin formation.Acta Pharmacologica Sinica.2023: 1-12.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Anti-Cancer Approved Drug Library Anti-Cancer Compound Library Inhibitor Library Autophagy Compound Library Anti-Lung Cancer Compound Library Anti-Ovarian Cancer Compound Library NO PAINS Compound Library

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Keywords

Fulvestrant 129453-61-8 Apoptosis Autophagy Endocrinology/Hormones Estrogen Receptor/ERR Estrogen/progestogen Receptor Inhibitor ICI-182780 ZM 182780 inhibit ZM182780 ZD9238 ICI182780 ZM-182780 ZD-9238 ZD 9238 ICI 182780 inhibitor

 

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