Elacestrant 2HCl is an orally available, selective estrogen receptor degrader (SERD) and selective estrogen receptor modulator (SERM), with potential antineoplastic and estrogen-like activities.
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Elacestrant dihydrochloride (RAD1901), an orally administered selective degrader of estrogen receptors (SERD), shows IC50 values of 48 nM for ERα and 870 nM for ERβ. It has the capability to suppress the growth of ER+ breast cancer cells both in vitro and in vivo[1].[2].
体内研究
Administered orally at dosages ranging from 0.3 to 120 mg/kg once daily for 40 days, Elacestrant dihydrochloride counteracts estrogen (E2)-induced uterine growth in a dose-responsive manner in vivo[1].
With daily oral doses of 30 and 60 mg/kg for a duration of four weeks, Elacestrant dihydrochloride achieves complete inhibition of tumor growth in mouse models[2].
The effect of inhibiting tumor growth persists for four weeks following the cessation of Elacestrant dihydrochloride treatment[2].
体外研究
In a dose-dependent manner, Elacestrant dihydrochloride (RAD1901; concentration range: 0.5 nM-10 µM; duration: 48 hours) reduces ERα levels, achieving an EC50 of 0.6 nM in MCF-7 cells[1].
Elacestrant dihydrochloride, across a concentration range of 0-1 µM over 48 hours, diminishes the proliferation of Estradiol (E2)-stimulated MCF-7 cells, with the EC50 recorded at 4 pM[1].
Application of Elacestrant dihydrochloride (0-1 µM; for 24 or 48 hours) leads to a significant dose-dependent reduction in estrogen receptor protein levels in cell lines such as MCF7, T47D, and HCC1428[2].
At concentrations of 0.01, 0.1, and 1.0 µM, Elacestrant dihydrochloride lowers the expression of the progesterone receptor (PGR, PR), a target gene of the estrogen receptor, in both MCF7 and T47D cell lines[2].
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