Elacestrant dihydrochloride

SKU: orb1308826

Description

Elacestrant dihydrochloride is an orally bioavailable selective estrogen receptor degrader (SERD) that demonstrates potent and selective activity against ERα (IC50 = 48 nM) over ERβ. It is utilized in research for studying hormone receptor-positive breast cancer, with applications in both in vitro cellular assays and in vivo xenograft models.

Research Area

Metabolism Research

Key Properties

• CAS Number: 1349723-93-8
• MW: 531.56
• Purity: 99.99%
• Formula: C₃₀H₄₀Cl₂N₂O₂
• SMILES: Cl.Cl.CCNCCc1ccc(CN(CC)c2cc(OC)ccc2[C@@H]2CCc3cc(O)ccc3C2)cc1
• Target: Estrogen Receptor/ERR,Estrogen/progestogen Receptor
• Solubility: H2O:40 mg/mL (75.25 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.76 mM);DMSO:55 mg/mL (103.47 mM)

Bioactivity

• Target IC50:
  ERα:48 nM |ERβ:870 nM
• In Vivo:
  In MCF-7 xenograft models, Elacestrant-treated animals survived longer than those treated with either control or ICI 182780. RAD1901 preserves ovariectomy-induced bone loss and prevents the uterotropic effects of E2. Elacestrant produces a robust and profound inhibition of tumor growth in MCF-7 xenograft models.
• In Vitro:
  Elacestrant exhibits inhibition of ERα expression in a dose-dependent manner, with an EC50 of 0.6 nM. Treatment of ER-positive MCF-7 cells with E2 results in a potent and dose-dependent increase in proliferation, with an EC50 of 4 pM. Treatment of cells with Elacestrant in the presence of 10 pM E2 results in a dose-dependent decrease in proliferation, with an IC50 value of 4.2 nM. Elacestrant selectively binds to and degrades the ER and is a potent antagonist of ER-positive breast cancer cell proliferation.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, Elacestrant, Elacestrant Dihydrochloride, Elacestrant dihydrochloride, ERβ, ERα, Estrogen Receptor, EstrogenReceptor, Estrogen Receptor/ERR, inhibit, RAD1901, RAD-1901, RAD1901 Dihydrochloride, RAD1901 dihydrochloride, RAD-1901 Dihydrochloride, RAD 1901 Dihydrochloride, RAD 1901, progestogenReceptor, progestogen Receptor

Compound Identifiers

PubChem CID

67479909