Fulvestrant (ICI 182,780)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Fulvestran is a newer type of estrogen receptor (ER) antagonist with IC50 value of 9.4nM [1].
Fulvestrant treatment caused a significant decrease in MDM2 protein expression in human breast cancer cell lines MCF7 and T47D, and that the reduction of MDM2 correlated with the decrease in ER expression [1].
Fulvestrant enhances the sensitivity of human breast cancer cells to chemotherapeutic drugs. CompuSyn analyses showed that combined use of doxorubicin, paclitaxel or etoposide with fulvestrant resulted in different degrees of synergism in MCF7 and T47D cell lines tested. Besides, Combination of fulvestrant and chemotherapeutic drugs induces altered cell cycle distribution, apoptosis, and senescence [1].
References:
[1] Dolfi SC1, Jäger AV2, Medina DJ1, Haffty BG3, Yang JM4, Hirshfield KM5.Fulvestrant treatment alters MDM2 protein turnover and sensitivity of human breast carcinoma cells to chemotherapeutic drugs. Cancer Lett. 2014 Apr 18. pii: S0304-3835(14)00215-8.
- 1. Bai Y, Shen W, et al. "Combined detection of estrogen and tumor markers is an important reference factor in the diagnosis and prognosis of lung cancer." J Cell Biochem. 2018 Sep 14. PMID:30216488
- 2. McDermott MS, Chumanevich AA, et al. "Inhibition of CDK8 mediator kinase suppresses estrogen dependent transcription and the growth of estrogen receptor positive breast cancer." Oncotarget. 2017 Feb 21;8(8):12558-12575. PMID:28147342
- 3. Li, Han, et al. "Triptolide inhibits human breast cancer MCF-7 cell growth via downregulation of the ERα-mediated signaling pathway." Acta Pharmacologica Sinica (2015). PMID:25864647
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 606.77 |
| Cas No. | 129453-61-8 |
| Formula | C32H47F5O3S |
| Solubility | ≥30.35mg/mL in DMSO |
| Chemical Name | (7R,8R,9S,13S,14S,17S)-13-methyl-7-[9-(4,4,5,5,5-pentafluoropentylsulfinyl)nonyl]-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,17-diol |
| SDF | Download SDF |
| Canonical SMILES | CC12CCC3C(C1CCC2O)C(CC4=C3C=CC(=C4)O)CCCCCCCCCS(=O)CCCC(C(F)(F)F)(F)F |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. |
| Cell experiment [1]: | |
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Cell lines |
T47D and MCF7 breast cancer cell lines |
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Preparation method |
The solubility of this compound in DMSO is >30.3mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
|
Reacting condition |
1 μM, 10 μM, 66 h |
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Applications |
Treatment of ER+ human breast cancer cell lines, MCF7 and T47D cells with fulvestrant caused a significant decrease in MDM2 protein expression. Treatment with fulvestrant for 16 h or 66 h does not alter MDM2 mRNA level. Fulvestrant (1 μM, 16 h) facilitated degradation of MDM2 protein and shortened half-life of this protein (27 min vs. 42 min in T47D cells; 80 min vs. 180 min in MCF7 cells). Treatment with fulvestrant (5 μM, 72 h) increased the G1 population. |
| Animal experiment [2]: | |
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Animal models |
Nude mice bearing MCF-7 and Br10 human breast cancers |
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Dosage form |
s.c. injection; 5 mg; 4 weeks |
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Application |
Fulvestrant substantially reduced tumor growth. |
| Clinical Trials [3]: | |
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Clinical Trials |
Postmenopausal women with advanced breast cancer |
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Dosage form |
Intramuscular injection; 250 mg as a once-monthly (one × 5 mL), |
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Application |
Fulvestrant is an additional, effective, and well-tolerated treatment for advanced breast cancer in postmenopausal women whose disease progressed on prior endocrine therapy. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Dolfi SC1, Jger AV2, Medina DJ1, Haffty BG3, Yang JM4, Hirshfield KM5.Fulvestrant treatment alters MDM2 protein turnover and sensitivity of human breast carcinoma cells to chemotherapeutic drugs. Cancer Lett. 2014 Apr 18. pii: S0304-3835(14)00215-8. [2]. Wakeling A E, Dukes M, Bowler J. A potent specific pure antiestrogen with clinical potential[J]. Cancer research, 1991, 51(15): 3867-3873. [3]. Howell A, Robertson J F R, Quaresma Albano J, et al. Fulvestrant, formerly ICI 182,780, is as effective as anastrozole in postmenopausal women with advanced breast cancer progressing after prior endocrine treatment[J]. Journal of Clinical Oncology, 2002, 20(16): 3396-3403. |
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Quality Control & MSDS
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