Fulvestrant (ICI 182,780) |
| Catalog No.: GC18000 |
Fulvestrant (ICI 182,780) (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant (ICI 182,780) is also a GPR30 agonist. Fulvestrant (ICI 182,780) effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant (ICI 182,780) also induces autophagy and has antitumor efficacy.
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
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Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| 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. |
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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. | |
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.
| Cas No. | 129453-61-8 | SDF | |
| 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 | ||
| Canonical SMILES | CC12CCC3C(C1CCC2O)C(CC4=C3C=CC(=C4)O)CCCCCCCCCS(=O)CCCC(C(F)(F)F)(F)F | ||
| Formula | C32H47F5O3S | M.Wt | 606.77 |
| Solubility | ≥ 30.35mg/mL in DMSO | Storage | Store at -20°C |
| 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. | ||
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
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Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
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