Elacestrant dihydrochloride

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 AnalysisCell Line:MCF7, T47D, and HCC1428 cells Concentration:0-1 μM Incubation Time:24 or 48 h Result:Decreased the expression of estrogen receptor protein.

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RAD-1901 dihydrochloride

Endocrinology/Hormones

Estrogen Receptor/ERR

Estrogen Receptor/ERR

Cancer

Breast Cancer

1349723-93-8

531.5568

C30H40Cl2N2O2

>98% (HPLC)

DMSO: 17.6 mg/mL

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2-Naphthalenol, 6-[2-[ethyl[[4-[2-(ethylamino)ethyl]phenyl]methyl]amino]-4-methoxyphenyl]-5,6,7,8-tetrahydro-, hydrochloride (1:2), (6R)-

(-20℃)

With Ice Pack

≥ 2 years