For research use only.
Catalog No.S1191 Synonyms: ICI-182780, ZD 9238
Molecular Weight(MW): 606.77
Fulvestrant is an estrogen receptor (ER) antagonist with IC50 of 0.94 nM in a cell-free assay. Fulvestrant also induces autophagy and apoptosis and has antitumor activity.
Selleck's Fulvestrant has been cited by 75 publications
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Choose Selective Estrogen/progestogen Receptor Inhibitors
|Description||Fulvestrant is an estrogen receptor (ER) antagonist with IC50 of 0.94 nM in a cell-free assay. Fulvestrant also induces autophagy and apoptosis and has antitumor activity.|
Fulvestrant is an effective inhibitor of the growth of ER-positive MCF-7 (with IC50 of 0.29 nM) but with no effect on the growth of ER-negative BT-20 human breast cancer cells. Fulvestrant causes accumulation of cells in G0/G1 and also reduces the proportion of cells capable of continued DNA synthesis.  Fulvestrant competitively inhibits binding of oestradiol to the estrogen receptor. Fulvestrant blocks nuclear localization of the ER through impairing receptor dimerisation, and energy-dependent nucleo-cytoplasmic shuttling. Because of the instability of fulvestrant-ER complex, the binding of Fulvestrant with ER finally results in accelerated degradation of the ER protein.  Fulvestrant (10 nM) not only decreases IGF-IR mRNA levels but also decreases the half-life.  Treatment with 100 μM Fulvestrant leads to a time dependent increase of TNFR1 and TRADD steady-state mRNA levels in MCF-7 cells.  Fulvestrant is capable of down-regulating androgen receptor expression and diminishes androgenic responses in LNCaP human prostate cancer cells. Fulvestrant also significantly attenuates R1881-stimulated growth by 70%.  Fulvestrant is able to modulate mitosis and cell death in immature cerebellar neurons via rapid activation of MAPK. 
|In vivo||Fulvestrant is devoid of uterotropic activity, and when co-administered with estradiol, it effectively blocks the uterotropic action of estradiol with ED50 of 0.06 mg/kg/day s.c. in immature female rats. A single s.c. injection of 5 mg of Fulvestrant suspension blocks completely the growth of MCF-7 xenografts. The growth of transplants of the BrlO human breast tumor is also suppressed effectively by 10 μM Fulvestrant.  Fulvestrant (10 mg/rat, s.c.) reduces the androgen receptor expression, ERK1/2 phosphorylation and cell proliferation in the rat ventral prostate.  Fulvestrant also displays anti-angiogenesis in the chick egg chorioallantoic membrane. |
-  Wakeling AE, et al. Cancer Res, 1991, 51(15), 3867-3873.
-  Osborne CK. Br J Cancer, 2004, 90 Suppl 1, S2-6.
-  Huynh H, et al. Clin Cancer Res, 1996, 2(12), 2037-2042.
-  Smolnikar K, et al. Breast Cancer Res Treat, 2000, 63(3), 249-259.
-  Bhattacharyya RS, et al. Mol Cancer Ther, 2006, 5(6), 1539-1549.
-  Wong JK, et al. J Neurosci, 2003, 23(12), 4984-4995.
-  Fernandes SA, et al. Int J Androl, 2011, 34(5 Pt 1), 486-500.
-  Gagliardi A, et al. Cancer Res, 1993, 53(3):533-535.
|In vitro||DMSO||100 mg/mL (164.8 mM)|
|Ethanol||'100 mg/mL warmed|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|Synonyms||ICI-182780, ZD 9238|
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Molecular Weight Calculator
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04300790||Not yet recruiting||Drug: Alpelisib|Drug: Metformin|Drug: Fulvestrant||Breast Cancer||MedSIR|Novartis||June 30 2020||Phase 2|
|NCT04024436||Recruiting||Drug: TAS-120|Drug: Fulvestrant||Metastatic Breast Cancer|FGFR2 Amplification||Taiho Oncology Inc.||December 15 2019||Phase 2|
|NCT04318223||Recruiting||Drug: Palbociclib||Metastatic Breast Cancer|Locally Advanced Breast Cancer||Consorzio Oncotech||July 16 2019||Phase 2|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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Frequently Asked Questions
Is there any information for the half-life of fulvestrant (Cat No.S1191)?
S1191, is about 13.5 to 18.5 hours in vivo: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2750771/. The half life of these compounds in cell culture might be different and we generally recommend replenishing with fresh drug every 24-48 hours.