Fulvestrant is a Estrogen receptor (ER) antagonist with IC50 of 0.094 nM. Fulvestrant effectively inhibited the growth of ER-positive McF-7 (IC50 = 0.29 nM), but had no effect on the growth of Er-negative BT-20 human breast cancer cells. Fulvestrant causes cells to accumulate in the G0/G1 phase and also reduces the proportion of cells capable of continuous DNA synthesis. Fulvestrant competitively inhibits estradiol binding to estrogen receptors. Fulvestrant can also induce autophagy and apoptosis, and has anti-tumor effect.
EMBO Mol Med. 2023 Dec.
MYSM1 acts as a novel co-activator of ERα to confer antiestrogen resistance in breast cancer
Fulvestrant purchased from AbMole
JCI Insight. 2022 Sep 8;7(17):e151851.
Targeting ESR1 mutation-induced transcriptional addiction in breast cancer with BET inhibition
Fulvestrant purchased from AbMole
NPJ Breast Cancer. 2022 Jan;8(1):1.
Effects of neoadjuvant trastuzumab, pertuzumab and palbociclib on Ki67 in HER2 and ER-positive breast cancer
Fulvestrant purchased from AbMole
Int J Biol Sci. 2018 Oct 3;14(12):1755-1768.
Inhibition of Estrogen Signaling Reduces the Incidence of BRCA1-associated Mammary Tumor Formation.
Fulvestrant purchased from AbMole
Oncotarget. 2016 Dec 20;7(51):83893-83906.
Arctigenin functions as a selective agonist of estrogen receptor β to restrict mTORC1 activation and consequent Th17 differentiation
Fulvestrant purchased from AbMole
Breast Cancer Res Treat. 2015 Jan;149(1):69-79.
The PI3K/mTOR dual inhibitor P7170 demonstrates potent activity against endocrine-sensitive and endocrine-resistant ER+ breast cancer.
Fulvestrant purchased from AbMole
Cell Experiment | |
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Cell lines | MCF-7 |
Preparation method | MCF-7 cells were plated at 10 000 cells/well in 96-well culture plates in MEM with 10% fetal bovine serum, and they were allowed to adhere for 48 h. Thereafter, the cultures were washed with serum-free MEM and incubated in 100 μl serum-free MEM. After 72 h, the medium was removed and replaced with 2% charcoal-stripped FBS–MEM containing 10 pmol/l E2 with either RAD1901 or additional E2 at concentrations ranging from 10−15 to 10−6 mol/l. The medium was removed after 48 h of incubation and the cells were lysed by adding 100 μl of CellTiter Glo (Promega, Madison, Wisconsin, USA), diluted 1 : 1 in water, per well. The plates were gently mixed on a plate shaker for 10 min before the luminescent signal was measured on a luminometer. The EC50 and IC50 of the test compound were defined as the concentrations that resulted in half-maximum shift. |
Concentrations | Ranging from 10−15 to 10−6 mol/l |
Incubation time | 48 h |
Animal Experiment | |
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Animal models | MCF-7 xenograft models: Female athymic nude mice [Crl:NU(NCr)-Foxn1nu] |
Formulation | Formulated for use as a homogenous suspension in 0.5% (w/v) methylcellulose in deionized water |
Dosages | 0.5 mg/animal daily |
Administration | subcutaneous injection |
Molecular Weight | 606.77 |
Formula | C32H47F5O3S |
CAS Number | 129453-61-8 |
Solubility (25°C) | DMSO 50 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[1] Johnston SJ, et al. Curr Med Chem. Fulvestrant - a novel endocrine therapy for breast cancer.
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