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Fulvestrant (ICI 182,780)
Estrogen receptor antagonist,high affinity

Fulvestrant (ICI 182,780)

Catalog No. A1428
Size Price Stock Qty
10mM (in 1mL DMSO) $55.00 In stock
25mg $50.00 In stock
100mg $100.00 In stock

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Sample solution is provided at 25 µL, 10mM.

Product Citations

1. 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

Quality Control

Chemical structure

Fulvestrant

Related Biological Data

Fulvestrant (ICI 182,780)

Protocol

Cell experiment [1]:

Cell lines

T47D and MCF7 breast cancer cell lines

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

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]:

Animal models

Nude mice bearing MCF-7 and Br10 human breast cancers

Dosage form

s.c. injection; 5 mg; 4 weeks

Application

Fulvestrant substantially reduced tumor growth.

Clinical Trials [3]:

Clinical Trials

Postmenopausal women with advanced breast cancer

Dosage form

Intramuscular injection; 250 mg as a once-monthly (one × 5 mL),

Application

Fulvestrant is an additional, effective, and well-tolerated treatment for advanced breast cancer in postmenopausal women whose disease progressed on prior endocrine therapy.

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.

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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Chemical Properties

Cas No. 129453-61-8 SDF Download 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 >30.3mg/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

Background

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.