SML4454

Elacestrant dihydrochloride

≥98% (HPLC)

• Synonym(e): (6R)-6-[2-[Ethyl[[4-[2-(ethylamino)ethyl]phenyl]methyl]amino]-4-methoxyphenyl]-5,6,7,8-tetrahydro-2-naphthalenol hydrochloride, RAD 901 dihydrochloride
• Empirische Formel (Hill-System): C₃₀H₃₈N₂O₂·2HCl
• CAS-Nummer: 1349723-93-8
• Molekulargewicht: 531.56
• UNSPSC Code: 12352200
• Assay: ≥98% (HPLC)
• Form: powder
• Storage condition: desiccated

Eigenschaften

• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: powder
• storage condition: desiccated
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: -10 to -25°C

Beschreibung

Biochem/physiol Actions

Elacestrant (RAD1901) is an orally bioavailable, non-steroidal selective estrogen receptor degrader (SERD) and ER antagonist that potently inhibits ERα-mediated proliferation (e.g., 4 pM EC50 in MCF-7 cells, 48 nM ERα IC50) while showing minimal activity against ERβ (870 nM IC50). Elacestrant induces dose-dependent ERα degradation via the proteasome, a dual mechanism distinct from PI3K/AKT/mTOR pathways, conferring efficacy in preclinical models resistant to fulvestrant and CDK4/6 inhibitors, including those with ESR1 mutations. Elacestrant also penetrates the blood-brain barrier and shows synergistic potential with palbociclib or everolimus, positioning it as a key agent for advanced ER+ breast cancer.

Disclaimer

Hygroscopic, store with desiccant

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable