Quality Segment
assay
≥98% (HPLC)
form
powder
storage condition
desiccated
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
-10 to -25°C
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
存储类别
11 - Combustible Solids
闪点 (F)
Not applicable
闪点 (°C)
Not applicable