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.
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
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Source | Int J Biol Sci (2018 Oct). Figure 6. Fulvestrant (Abmole Bioscience, Houston, USA) |
| Method | subcutaneously | |
| Cell Lines | Conditional Brca1-knockout and MMTV-Cre transgenic mice | |
| Concentrations | 250 mg/kg | |
| Incubation Time | - | |
| Results | The chemotherapeutic efficacy of fulvestrant was examined in 18 sets of allograft mice produced from tumors from 18 individuals. |
 |
Source | Int J Biol Sci (2018 Oct). Figure 5. Fulvestrant (Abmole Bioscience, Houston, USA) |
| Method | subcutaneously | |
| Cell Lines | Conditional Brca1-knockout and MMTV-Cre transgenic mice | |
| Concentrations | 250 mg/kg | |
| Incubation Time | - | |
| Results | In addition, histological analyses revealed that the number and size of lobular and ductal tubes were reduced in fulvestrant-treated mammary glands and their structure showed evidence of degeneration and shrinkage. |
 |
Source | Int J Biol Sci (2018 Oct). Figure 4. Fulvestrant (Abmole Bioscience, Houston, USA) |
| Method | subcutaneously | |
| Cell Lines | Conditional Brca1-knockout and MMTV-Cre transgenic mice | |
| Concentrations | 250 mg/kg | |
| Incubation Time | - | |
| Results | In addition, fulvestrant-treated tumors displayed large necrotic areas with a lower level of the proliferation marker, and higher levels of cleaved caspase-3 and positive TUNEL staining compared with untreated tumor tissues (Fig. 4C), suggesting that estrogen signaling contributes to altered aggressiveness of Brca1-mutant tumors. |
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Source | Oncotarget (2016). Figure 5. ICI-182780 (Abmole Bioscience Kowloon, Hong Kong). |
| Method | ||
| Cell Lines | CD4+CD62L+ T Cell | |
| Concentrations | 0.1 μM | |
| Incubation Time | 3 d | |
| Results | As shown in Figure 5A and 5B, neither MPP nor G15 showed noticeable effect on the decreased percentage of Th17 (IL-17A+CD4+ T) cells induced by arctigenin. Both ICI and PHTPP themselves did not affect the Th17 differentiation, but they markedly diminished the inhibitory effect of arctigenin. As expected, E2 could effectively decrease the percentage of Th17 cells. An addition of ICI also diminished the inhibitory effect of E2 on Th17 differentiation. Arctigenin markedly increased the expressions of ERβ target genes CAV1 and ENPP2, but showed no obvious effect on the expression of ERβ during Th17 differentiation (Figure 5C), which coincided well with the fact that arctigenin specifically promoted the expression of ERβ target genes in EL4 cells. |
-3.jpg) |
Source | Breast Cancer Res Treat (2015). Figure 4.Fulvestrant was obtained either in the clinical formulation (Astrazeneca) or in the powder form (Abmole), |
| Method | tumor volume, Ki67 staining, western bolt | |
| Cell Lines | T47D/FR | |
| Concentrations | 5 mg/week s.c. in 100 µL | |
| Incubation Time | 3 days(wb) or 8 weeks | |
| Results | "P7170 (in the context of a fulvestrant backbone) significantly decreased cell proliferation in T47D/FR tumors, but did not significantly increase apoptosis." |
-2.jpg) |
Source | Breast Cancer Res Treat (2015). Figure 3.Fulvestrant was obtained either in the clinical formulation (Astrazeneca) or in the powder form (Abmole), |
| Method | tumor volume, western blot, H&E staining, Ki67 staining, TUNEL test | |
| Cell Lines | MCF-7 | |
| Concentrations | 5 mg/week s.c. in 100 µL | |
| Incubation Time | 3 days(wb) or 4-6 weeks | |
| Results | The addition of 5 mg/kg/day P7170 to fulvestrant significantly decreased tumor volumes compared to fulvestrant alone after 3–4.5 weeks of treatment (p<0.05) |
-1.jpg) |
Source | Breast Cancer Res Treat (2015). Figure 2.Fulvestrant was obtained either in the clinical formulation (Astrazeneca) or in the powder form (Abmole), |
| Method | flow cytometry | |
| Cell Lines | MCF-7, MCF-7/FR, MCF-7/LTED, HCC-1428, T47D, T47D/FR | |
| Concentrations | 1 µM | |
| Incubation Time | 3-4 days | |
| Results | In MCF-7, MCF-7/LTED, T47D, and T47D/FR cells, the combination of P7170 and fulvestrant significantly increased apoptosis compared to either drug alone. |
| Cell Experiment | |
|---|---|
| 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 | |
|---|---|
| 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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