ElacestrantElacestrant
MedChemExpress (MCE)
HY-19822
722533-56-4
RAD1901
99.80%
4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months
-20°C, 1 month (sealed storage, away from moisture and light)
Room temperature in continental US
may vary elsewhere.
Elacestrant (RAD1901) is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant also can inhibit growth of ER+ breast cancer cell lines in vitro and in vivo.
Elacestrant (RAD1901
0.5 nM-10 µM
48 h) exhibits dose-dependent inhibition of ERα expression, with a EC50 of 0.6 nM in MCF-7 cells[1]. Elacestrant (0-1 µM
48 h) inhibits proliferation of Estradiol (E2)-stimulated MCF-7 cells in a dose-dependent manner, with an EC50 of 4 pM[1]. Elacestrant (0-1 µM
24 or 48 h) results in a dose-dependent and marked decrease in estrogen receptor protein expression in MCF7, T47D, and HCC1428 cells[2]. Elacestrant (0.01, 0.1, 1.0 µM) decreases expression of progesterone receptor (PGR, PR
an ER target gene), in both MCF7 and T47D cell lines[2].
Elacestrant (0.3-120 mg/kg
p.o.
single daily for 40 days) antagonizes E2-mediated uterine stimulation in a dose-dependent manner in vivo[1]. Elacestrant (30, 60 mg/kg
p.o.
single daily for 4 weeks) induces complete tumor growth inhibition in mice[2]. Tumor growth inhibition is maintained for 4 weeks after Elacestrant withdrawal[2].
IC50: 48 nM (ERα), 870 nM (ERβ)[1] Cellular Effect Cell Line Type Value Description References
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[1]. Garner F, et al. RAD1901: a novel, orally bioavailable selective estrogen receptor degrader that demonstrates antitumor activity in breast cancer xenograft models. Anticancer Drugs. 2015 Oct
26(9):948-56. [Content Brief]
[2]. Bihani T, et al. Elacestrant (RAD1901), a Selective Estrogen Receptor Degrader (SERD), Has Antitumor Activity in Multiple ER+ Breast Cancer Patient-derived Xenograft Models. Clin Cancer Res. 2017 Aug 15
23(16):4793-4804. [Content Brief]