Elacestrant CAS# 722533-56-4 艾拉司群

Elacestrant, also known as RAD1901, is an orally available, selective estrogen receptor degrader (SERD) and selective estrogen receptor modulator (SERM). Elacestrant exhibits potent in vitro bioactivity as a selective estrogen receptor degrader (SERD), showing effective antagonism and degradation of estrogen receptor alpha (ERα) in ER-positive breast cancer cell lines. In MCF-7 and T47D cells, Elacestrant inhibits estrogen-driven proliferation with IC₅₀ values in the range of 1–3 nM. It induces dose-dependent degradation of ERα protein, with maximal degradation observed at concentrations as low as 10–30 nM. In ESR1-mutant models (e.g., Y537S and D538G), which are resistant to fulvestrant, Elacestrant retains potent antiproliferative effects, reducing cell viability with IC₅₀ values around 5–20 nM.