RAD1901 dihydrochloride 是一种具有口服活性的的选择性雌激素受体 (ER) 降解剂 (SERD)，能够作用于 ERα (IC50:48 nM) 和 ERβ (IC50:870 nM)。

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

Elacestrant exhibits inhibition of ERα expression in a dose-dependent manner, 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 Elacestrant in the presence of 10 pM E2 results in a dose-dependent decrease in proliferation, with an IC50 value of 4.2 nM. Elacestrant selectively binds to and degrades the ER and is a potent antagonist of ER-positive breast cancer cell proliferation[1].?

In MCF-7 xenograft models, Elacestrant-treated animals survived longer than those treated with either control or ICI 182780. RAD1901 preserves ovariectomy-induced bone loss and prevents the uterotropic effects of E2. Elacestrant produces a robust and profound inhibition of tumor growth in MCF-7 xenograft models[1].?

1349723-93-8

C30H40Cl2N2O2

531.56

RAD1901 dihydrochloride

H2O:40 mg/mL (75.25 mM)
DMSO:80 mg/mL (150.50 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years