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Postion:Product Catalog >API>Antineoplastic agents>Hormonal antineoplastic drugs>Fulvestrant
Fulvestrant
  • Fulvestrant

Fulvestrant NEW

Price $42 $67 $118
Package 10mg 25mg 50mg
Min. Order:
Supply Ability: 10g
Update Time: 2024-11-19

Product Details

Product Name: Fulvestrant CAS No.: 129453-61-8
Purity: 99.87% Supply Ability: 10g
Release date: 2024/11/19

Product Introduction

Bioactivity

NameFulvestrant
DescriptionFulvestrant (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.
Cell ResearchIn 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 ResearchMCF-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].
In vitroMETHODS: 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 vivoMETHODS: 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]
Storagekeep away from direct sunlight,keep away from moisture,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility InformationEthanol : 30.3 mg/mL (50 mM)
DMSO : 45 mg/mL (74.16 mM)
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 6.07 mg/mL (10 mM), Suspension. Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
KeywordsEstrogen Receptor/ERR | Inhibitor | Autophagy | ICI-182780 | inhibit | ZM182780 | Fulvestrant | ZD9238 | Apoptosis | ICI182780 | ZM-182780 | ZD-9238
Inhibitors RelatedStavudine | 5-Fluorouracil | Sodium 4-phenylbutyrate | L-Ascorbic acid | Hydroxychloroquine | Guanidine hydrochloride | Taurine | Tributyrin | Curcumin | Paeonol | Naringin | Gefitinib
Related Compound LibrariesBioactive Compound Library | EMA Approved Drug Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Anti-Cancer Approved Drug Library | FDA-Approved Drug Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library

Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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  • Since: 2011-01-07
  • Address: 36?Washington?Street, Wellesley?Hills
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