Fulvestrant
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.
5 Customer Reviews
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PTPH1 confers breast cancer cell sensitivity to fulvestrant. E and F, PTPH1 overexpression increases the growth inhibition by fulvestrant. PTPH1 was overexpressed by a Tet-on system or a stable transfection, and resultant cells were incubated with fulvestrant as indicated for about 2 weeks. Colony formed was stained and counted. Results shown are normalized to its own solvent control of Vector and PTPH1-overexpressed cells, respectively (means ± SD; n = 3–5) with insets showing PTPH1 overexpression. *, versus vector or no Tet cells for E and F.
Mol Cancer Ther 2014 13(1), 230-8. Fulvestrant purchased from Selleck.
Fulvestrant resistance induced by 6 different ZF-TFs. (A) Drug sensitivity of fulvestrant-selected MCF7 ZF-TF-transduced cells. MCF7 cells transduced with one of six different ZF-TF-expressing retroviruses selected first in puromycin (the transduction selection marker) and then in fulvestrant for 1 month were grown in the absence of fulvestrant for 7 days and then challenged with 100 nM fulvestrant or vehicle (0.1% ethanol) for 21 days followed by crystal violet staining and visualization. Data are representative of triplicate experiments.PLoS One 2011 6, e21112. Fulvestrant purchased from Selleck.
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Fulvestrant resistance induced by 6 different ZF-TFs. (B and C) Growth curves of MCF7 and T47D cells in the presence and absence of fulvestrant. Comparison of cell growth rates (cell number, mean +/2 SEM, n = 8; time in days as indicated) of MCF7 and T47D cells stably transduced with control retrovirus or one of six different ZF-TF-expressing retroviruses (7, 19, 64, 70, 83 and 115) in the presence (blue line) or absence (pink line) of fulvestrant.
PLoS One 2011 6, e21112. Fulvestrant purchased from Selleck.
CDK4/6 inhibitor resistance promotes diminished ER expression and activity. (a and b) Proliferation of MCF-7 and MR cells in the presence of different concentrations of ICI (a) or 4-hydroxytamoxifen (4-OHT) (b) was measured by the alamarBlue assay and plotted as % inhibition of proliferation against log concentration of inhibitor. Each data point represents the average value±s.d. of six replicates obtained in three independent experiments. (c) MCF-7 and MR cells were treated with different concentrations of ICI, collected after 24 h and then immunoblotted with the indicated antibodies.
Oncogene, 2017, 36(16):2255-2264. Fulvestrant purchased from Selleck.
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A: Time dependent loss of MGMT activity in ERα-positive MCF7 and T47D tumor cells but not in ERα-negative MDAMB-468 cells after 1 μmol/L Fulvestrant treatment (upper panel). Concentration dependent inhibition of MGMT activity in MCF7 and T47D cells but not in MDA-MB-468 cells after a 72 hours exposure to fulvestrant (lower panel). The data represents the mean of two independent experiments in duplicate and the last time point (72 hours) as assessed by student's t-test was significant at P < 0.05. B: Decreased MGMT and ER-α protein levels in MCF7 cells after 48 hours and 72 hours fulvestrant exposure. ICI is fulvestrant, also called ICI-182,780. C: Decreased MGMT and ER-α protein levels in T47D cells after 48 hours and 72 hours fulvestrant exposure.
J Biomed Res, 2016, 30(5):393-410. Fulvestrant purchased from Selleck.
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Biological Activity
| Description | Fulvestrant is an estrogen receptor (ER) antagonist with IC50 of 0.94 nM in a cell-free assay. | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| In vitro |
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. [1] 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. [2] Fulvestrant (10 nM) not only decreases IGF-IR mRNA levels but also decreases the half-life. [3] Treatment with 100 μM Fulvestrant leads to a time dependent increase of TNFR1 and TRADD steady-state mRNA levels in MCF-7 cells. [4] 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%. [5] Fulvestrant is able to modulate mitosis and cell death in immature cerebellar neurons via rapid activation of MAPK. [6] |
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| Cell Data |
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| 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. [1] Fulvestrant (10 mg/rat, s.c.) reduces the androgen receptor expression, ERK1/2 phosphorylation and cell proliferation in the rat ventral prostate. [7] Fulvestrant also displays anti-angiogenesis in the chick egg chorioallantoic membrane. [8] |
Protocol
| Cell Research:[1] |
+ Expand
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| Animal Research:[6] |
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References
- [1] Wakeling AE, et al. Cancer Res, 1991, 51(15), 3867-3873.
- [2] Osborne CK. Br J Cancer, 2004, 90 Suppl 1, S2-6.
- [3] Huynh H, et al. Clin Cancer Res, 1996, 2(12), 2037-2042.
- [4] Smolnikar K, et al. Breast Cancer Res Treat, 2000, 63(3), 249-259.
- [5] Bhattacharyya RS, et al. Mol Cancer Ther, 2006, 5(6), 1539-1549.
- [6] Wong JK, et al. J Neurosci, 2003, 23(12), 4984-4995.
- [7] Fernandes SA, et al. Int J Androl, 2011, 34(5 Pt 1), 486-500.
- [8] Gagliardi A, et al. Cancer Res, 1993, 53(3):533-535.
Solubility (25°C)
| In vitro | DMSO | 100 mg/mL (164.8 mM) |
|---|---|---|
| Ethanol | 100 mg/mL warmed (164.8 mM) | |
| Water | Insoluble | |
| In vivo | Add solvents to the product individually and in order: 5% DMSO+95% Corn oil For best results, use promptly after mixing. |
30mg/mL |
* 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.
Chemical Information
| Molecular Weight | 606.77 |
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| Formula | C32H47F5O3S |
| CAS No. | 129453-61-8 |
| Storage | powder |
| in solvent | |
| Synonyms | ICI-182780, ZD 9238 |
Bio Calculators
Molarity Calculator
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Dilution Calculator
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
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Molarity Calculator
Clinical Trial Information
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT01797120 | Active, not recruiting | Metastatic Breast Cancer | PrECOG, LLC.|Novartis | May 31, 2013 | Phase 2 |
| NCT01633060 | Active, not recruiting | Metastatic Breast Cancer | Novartis Pharmaceuticals|Novartis | October 3, 2012 | Phase 3 |
| NCT03007979 | Not yet recruiting | Breast Cancer|Breast Carcinoma|Cancer of Breast|Malignant Tumor of Breast | Washington University School of Medicine | February 28, 2017 | Phase 2 |
| NCT03024580 | Not yet recruiting | Breast Neoplasm | Instituto Nacional de Cancer, Brazil|Cancer Research UK Cambridge Institute | March 2017 | Phase 2 |
| NCT02947685 | Not yet recruiting | HER-2 Positive Breast Cancer|Estrogen Receptor Positive Breast Cancer | Alliance Foundation Trials, LLC.|Pfizer|German Breast Group (GBG)|Fondazione Michelangelo|PrECOG, LLC.|The Australia and New Zealand Breast Cancer Trials Group (ANZBCTG)|Alliance Foundation Trials Biorepository - Washington State University|Alliance Foundation Trials Central Imaging Core Lab - Ohio State University|Mastering Breast Cancer Initiative, LLC|Mayo Clinic Statistics and Data Center|INC Research|SOLTI Breast Cancer Research Group | February 2017 | Phase 3 |
| NCT02983604 | Recruiting | Advanced Estrogen Receptor Positive HER2- Breast Cancer | Gilead Sciences | January 2017 | Phase 1|Phase 2 |
Tech Support
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.
Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.
Frequently Asked Questions
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Question 1:
Is there any information for the half-life of fulvestrant (Cat No.S1191)?
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Answer:
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.
