Elacestrant

SKU: orb1308827

Description

Elacestrant is an orally bioavailable selective estrogen receptor degrader (SERD) with preferential activity against ERα (IC50 = 48 nM) over ERβ (IC50 = 870 nM). It is utilized in research for studying hormone receptor-positive breast cancer, demonstrating antitumor efficacy in both cellular assays and animal models.

Research Area

Metabolism Research

Key Properties

• CAS Number: 722533-56-4
• MW: 458.63
• Purity: 99.92% (May vary between batches)
• Formula: C₃₀H₃₈N₂O₂
• SMILES: CCNCCc1ccc(CN(CC)c2cc(OC)ccc2[C@@H]2CCc3cc(O)ccc3C2)cc1
• Target: Estrogen/progestogen Receptor,Estrogen Receptor/ERR
• Solubility: DMSO:60 mg/mL (130.82 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (8.72 mM)

Bioactivity

• Target IC50:
  ERα:48 nM |ERβ:870 nM
• In Vivo:
  Elacestrant produces a robust and profound inhibition of tumor growth in MCF-7 xenograft models.Elacestrant preserves ovariectomy-induced bone loss and preventes the uterotropic effects of E2.Elacestrant-treated animals survived longer than those treated with either control or fulvestrant.
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• In Vitro:
  Elacestrant treatment exhibits dose-dependent inhibition of ERα expression, 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 resultsin 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

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

Compound Identifiers

PubChem CID

23642301