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Elacestrant dihydrochloride

Chemical Structure : Elacestrant dihydrochloride

CAS No.: 1349723-93-8

Elacestrant dihydrochloride (RAD1901 dihydrochloride)

Catalog No.: PC-45734Not For Human Use, Lab Use Only.

Elacestrant (RAD1901) dihydrochloride is a novel, orally bioavailable small-molecule selective estrogen receptor degrader (SERD).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Elacestrant (RAD1901) dihydrochloride is a novel, orally bioavailable small-molecule selective estrogen receptor degrader (SERD).
Elacestrant (RAD1901) inhibits ERα expression in MCF-7 cells (IC50=0.6 nM).
Elacestrant (RAD1901) 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 531.5568
Formula C30H40Cl2N2O2
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

DMSO: 17.6 mg/mL; H2O

Chemical Name/SMILES

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