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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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Other Sizes |
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Purity: ≥98%
Fulvestrant (ICI-182780; ZD-9238; ZM-182780; Faslodex) is a synthetic and potent estrogen receptor (ER) antagonist approved as a medication for the treatment of hormone receptor (HR)-positive breast cancer in postmenopausal women. It ihibits ER with an IC50 of 0.94 nM in a cell-free assay. Unlike tamoxifen, which has partial agonist effects, and the aromatase inhibitors, which reduce the estrogen available to tumor cells, fulvestrant binds competitively to estrogen receptors in breast cancer cells, resulting in estrogen receptor deformation and decreased estrogen binding. In vitro studies indicate that fulvestrant reversibly inhibits the growth of tamoxifen-resistant, estrogen-sensitive, human breast cancer cell lines.
ln Vitro |
FuLvestrant (ICI 182780; ZD 9238; ZM 182780) is a very effective and selective oestrogen action inhibitor that shows superior growth suppression in animal models and human breast cancer cells. With an IC50 of 0.29 nM, fuLvestrant stops the development of MCF-7 human breast cancer cells. Fulvestrant has a relative binding affinity of 0.89. FuLvestrant maintains its pure estrogen antagonist activity while having a markedly increased antiestrogenic potency [1]. Fulvestrant, an ER antagonist that downregulates ER, is the first new class of endocrine control medication[3]. ERα expression in MCF-7 cells was not affected by 1 μM ICI 47699 treatment, while it was fully suppressed by 100 nM FuLvestrant [4].
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ln Vivo |
When given by itself, fulvestrant (ICI 182,780) exhibits no uterotropic activity parenterally (sc) in immature female rats. Fulvestrant completely opposes the effects of estrogen at a dose of 0.5 mg/kg/day sc. Oral fulvestrant (5 mg/kg/day) treatment and subcutaneous administration are qualitatively comparable [1]. in two human breast cancer models in naked mice. After a single injection, fulvestrant (5 mg) in one of the models totally stopped the growth of MCF-7 tumor xenografts for at least 4 weeks. Fulvestrant suppressed existing tumor growth for twice as long and delayed tumor growth more than treatment with ICI 47699 in additional experiments conducted in nude mice carrying MCF-7 xenografts. Large[3]. At day 40, fulvestrant showed 88% tumor growth inhibition (TGI) [4].
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Animal Protocol |
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References |
[1]. Wakeling AE, et al. A potent specific pure antiestrogen with clinical potential. Cancer Res. 1991 Aug 1;51(15):3867-73.
[2]. Yu X, et al.MiR-214 increases the sensitivity of breast cancer cells to tamoxifen and fulvestrant through inhibition of autophagy.Mol Cancer. 2015 Dec 15;14:208. [3]. Osborne CK, et al. Fulvestrant: an oestrogen receptor antagonist with a novel mechanism of action. Br J Cancer. 2004 Mar;90 Suppl 1:S2-6. [4]. Garner F, et al. RAD1901: a novel, orally bioavailable selective estrogen receptor degrader that demonstrates antitumor activity in breast cancer xenograft models. Anticancer Drugs. 2015 Oct;26(9):948-56 [5]. Julia Kuhn, et al. GPR30 estrogen receptor agonists induce mechanical hyperalgesia in the rat. Eur J Neurosci. 2008 Apr;27(7):1700-9 |
Molecular Formula |
C32H47F5O3S
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Molecular Weight |
606.77
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CAS # |
129453-61-8
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Related CAS # |
Fulvestrant (Standard);129453-61-8;Fulvestrant (S enantiomer);1316849-17-8;Fulvestrant (R enantiomer);1807900-80-6;Fulvestrant-d3
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
C[C@@]12[C@@H](O)CC[C@@]1([H])[C@]3([H])[C@H](CCCCCCCCCS(CCCC(F)(F)C(F)(F)F)=O)CC4=C(C=CC(O)=C4)[C@@]3([H])CC2
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: 2.75 mg/mL (4.53 mM) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.12 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 2.08 mg/mL (3.43 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Solubility in Formulation 4: ≥ 2.08 mg/mL (3.43 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL corn oil and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 5: 5% DMSO +95%Corn oil : 30mg/mL Solubility in Formulation 6: 2.5 mg/mL (4.12 mM) in 15% Solutol HS 15 10% Cremophor EL 35% PEG 400 40% water (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. |
Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.