Elacestrant 是一种具有口服活性的、选择性的雌激素受体 (ER) 降解剂 (SERD)，能够作用于 ERα (IC50:48 nM)和 ERβ (IC50:870 nM)。

Elacestrant with IC50s of 48 and 870 nM for ERα and ERβ, respectively.Elacestrant is an orally available selective estrogen receptor degrader .

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.RAD1901 selectively binds to and degrades the ER and is a potent antagonist of ER-positive breast cancer cell proliferation.?

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

722533-56-4

C30H38N2O2

458.63

依拉司群;RAD1901

DMSO:60 mg/ml (130.82 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years