Fulvestrant - CAS 129453-61-8
Catalog number: 129453-61-8
Category: Inhibitor
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Estrogen Receptor/ERR
Fulvestrant is an effective inhibitor of the growth of ER-positive MCF-7 (with IC50 of 0.29 nM) but with no effect on the growth of ER-negative BT-20 human breast cancer cells.
ICI-182780, ZD 9238
Canonical SMILES:
1.Binding of anterior gradient 2 and estrogen receptor-α: Dual critical roles in enhancing fulvestrant resistance and IGF-1-induced tumorigenesis of breast cancer.
Li Z1, Zhu Q2, Chen H2, Hu L2, Negi H2, Zheng Y2, Ahmed Y2, Wu Z3, Li D4. Cancer Lett. 2016 Apr 7;377(1):32-43. doi: 10.1016/j.canlet.2016.04.003. [Epub ahead of print]
Anterior gradient 2 (AGR2), an essential cancer biomarker, has been widely reported to be associated with estrogen receptor (ER) positive breast cancer development. Here, we uncovered the role of cytoplasmic and exogenous AGR2, through interaction with ER-α, in enhancing fulvestrant resistance and IGF-1-induced carcinogenesis respectively. Our present study revealed that the endogenous AGR2 level positively correlates with fulvestrant resistance in MCF-7 and T47D cells. AGR2-knockdown in MCF-7 cells strongly enhances the fulvestrant-induced G1 phase arrest and accelerates the fulvestrant-induced ER-α degradation. Furthermore, intracellular AGR2 exhibits a functional interaction with ER-α. On the other hand, extracellular AGR2 remarkably promotes the IGF-1-induced cell proliferation, migration, cell cycle progression and epithelial-mesenchymal transition. Extracellular AGR2 also enhances IGF-1 downstream signaling. We also showed that ER-α specifically interacts with both extracellular AGR2 and IGF-1 receptor as a potential intermediator.
2.Impact of Apparent Antagonism of Estrogen Receptor β by Fulvestrant on Anticancer Activity of 2-Methoxyestradiol.
Gorska M1, Wyszkowska RM2, Kuban-Jankowska A2, Wozniak M2. Anticancer Res. 2016 May;36(5):2217-26.
Osteosarcoma is one of the most malignant bone tumors of childhood and adolescence. Interestingly, the presence of estrogen receptors α and β has been reported in human bone cells, including osteosarcoma. Thus, inhibitors of estrogens such as fulvestrant, are considered candidates for novel endocrine therapy in treatment of osteosarcoma. Another anticancer agent that seems to be very effective in treatment of osteosarcoma is a derivative of 17β-estradiol, 2-methoxyestradiol. The aim of this study was to determine the anticancer activities of pure anti-estrogen, fulvestrant and combined treatment of fulvestrant and 2-methoxyestradiol towards highly metastatic osteosarcoma 143B cells. 3-(4,5-Dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide assay was used in order to determine the antiproliferative potential of the compounds, and western blotting for estrogen receptors α and β. Flow cytometry was used in order to determine induction of cell death, cell-cycle arrest, mitochondrial depolarization, and DNA damage.
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CAS 129453-61-8 Fulvestrant

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