Elacestrant

Research use only, not for human use.

Elacestrant (RAD-1901) is a novel, orally bioavailable small-molecule selective estrogen receptor degrader (SERD).

Elacestrant (RAD-1901) is a novel, orally bioavailable small-molecule selective estrogen receptor degrader (SERD); inhibits ERα expression in MCF-7 cells (IC50=0.6 nM); induces the degradation of ER, inhibits ER-mediated signaling and growth of ER+ breast cancer cell lines in vitro and in vivo, and significantly inhibits tumor growth of multiple PDX models.Breast Cancer Phase 2 Clinical.

Cell Proliferation Assay Cell Line:ER-positive MCF-7 cells (Estradiol (E2)-stimulated)Concentration:0-1 μM Incubation Time:48 h Result:Showed antiproliferative activity on cells.Western Blot Analysis Cell Line:MCF-7 cells Concentration:0.5 nM-10 μM Incubation Time:48 h Result:Inhibited ERα expression (EC50 of 0.6 nM) in a dose-dependent manner.Western Blot Analysis Cell Line:MCF7, T47D, and HCC1428 cells Concentration:0-1 μM Incubation Time:24 or 48 h Result:Decreased the expression of estrogen receptor protein.

Animal Model:MCF7 cell line xenograft model of mice.Dosage:30, 60 mg/kg Administration:Oral administration; single daily for 4 weeks.Result:Inhibited growth of tumor.

RAD-1901

Endocrinology/Hormones

Estrogen Receptor/ERR

Estrogen Receptor/ERR

Cancer

Breast Cancer

722533-56-4

458.6349

C30H38N2O2

>98% (HPLC)

DMSO

CCNCCC1=CC=C(C=C1)CN(CC)C2=C(C=CC(=C2)OC)C3CCC4=C(C3)C=CC(=C4)O

2-Naphthalenol, 6-[2-[ethyl[[4-[2-(ethylamino)ethyl]phenyl]methyl]amino]-4-methoxyphenyl]-5,6,7,8-tetrahydro-, (6R)-

(-20℃)

With Ice Pack

≥ 2 years