tcsc6324 Elacestrant (dihydrochloride)

Elacestrant dihydrochloride (RAD1901 dihydrochloride) is a selective and orally available estrogen receptor (ERR) degrader with IC₅₀ values of 48 and 870 nM for ERα and ERβ, respectively.

IC50 & Target: IC50: 48 nM (ERα), 870 nM (ERβ)^[1]

In Vitro: RAD1901 selectively binds to and degrades the ER and is a potent antagonist of ER-positive breast cancer cell proliferation. RAD1901 treatment exhibits dose-dependent inhibition of ERα expression, with an EC₅₀ of 0.6 nM. Treatment of ER-positive MCF-7 cells with E2 results in a potent and dose-dependent increase in proliferation, with an EC₅₀ of 4 pM. Treatment of cells with RAD1901 in the presence of 10 pM E2 resultsin a dose-dependent decrease in proliferation, with an IC₅₀ value of 4.2 nM^[1].

In Vivo: RAD1901 produces a robust and profound inhibition of tumor growth in MCF-7 xenograft models. RAD1901-treated animals survived longer than those treated with either control or fulvestrant. RAD1901 preserves ovariectomy-induced bone loss and preventes the uterotropic effects of E2^[1].