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Elacestrant

Chemical Structure : Elacestrant

CAS No.: 722533-56-4

Elacestrant (RAD-1901, RAD1901)

Catalog No.: PC-45733Not For Human Use, Lab Use Only.

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

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Biological Activity

Elacestrant (RAD-1901) is a novel, orally bioavailable small-molecule selective estrogen receptor degrader (SERD).
Elacestrant (RAD-1901) inhibits ERα expression in MCF-7 cells (IC50=0.6 nM).
Elacestrant (RAD-1901) 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.

Physicochemical Properties

M.Wt 458.6349
Formula C30H38N2O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

References

1. Wardell SE, et al. Endocr Relat Cancer. 2015 Oct;22(5):713-24.

2. Garner F, et al. Anticancer Drugs. 2015 Oct;26(9):948-56.

3. Bihani T, et al. Clin Cancer Res. 2017 May 4. pii: clincanres.2561.2016.

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