Stemcell, 100-1649, Fulvestrant

Competitively inhibit estradiol (IC50 = 9.35 nM) with Fulvestrant, a potent estrogen receptor (ER) antagonist. Estradiol has been linked to the development and progression of ER-positive breast cancer (Johansson et al. J Endocr Soc, 2022; Rodriguez et al. Cancer Immunol Res, 2017). Fulvestrant has a high binding affinity for the estrogen receptor, 89% greater than that of estradiol (Wakeling & Bowler. J Endocrinol, 1987). By binding to the estrogen receptor, fulvestrant inhibits receptor dimerization, inactivates activating factor 1 (AF1) and activating factor 2 (AF2), and reduces translocation of the receptor to the nucleus (Nathan & Schmid. Oncol Ther, 2017). Competitive inhibition of estradiol by Fulvestrant also leads to accelerated degradation of the estrogen receptor (Nicholson et al. Ann N Y Acad Sci, 1995).

Fulvestrant has been used for:

CANCER RESEARCH

· Inhibit tumor growth and cause downregulation of the estrogen receptor in xenograft models of endocrine therapy-resistant breast cancer (Wardell et al. Breast Cancer Res Treat, 2020).

· Inhibit tumor growth and reduce tumor volume when used in combination with epidermal growth factor receptor (EGFR) inhibitors in a xenograft model of non–small-cell lung cancer (Garon et al. J Thorac Oncol, 2013).