Amcenestrant

SKU: orb1309128

Description

Amcenestrant (SAR439859) is an orally bioavailable, nonsteroidal selective estrogen receptor degrader (SERD) that potently antagonizes and degrades ERα (EC50 = 0.2 nM). It is a research tool for investigating hormone receptor-positive breast cancer in both cellular and animal models, as evidenced by preclinical studies.

Research Area

Metabolism Research

Key Properties

• CAS Number: 2114339-57-8
• MW: 554.48
• Purity: 99.00%
• Formula: C₃₁H₃₀Cl₂FNO₃
• SMILES: OC(=O)c1ccc2c(CCCC(c3ccc(Cl)cc3Cl)=C2c2ccc(O[C@H]3CCN(CCCF)C3)cc2)c1
• Target: Estrogen/progestogen Receptor,Estrogen Receptor/ERR
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:8 mg/mL (14.43 mM);DMSO:125 mg/mL (225.44 mM)

Bioactivity

• Target IC50:
  ERα:0.2 nM （EC50）
• In Vivo:
  SAR439859(orally; 2.5-25 mg/kg; twice daily for 30 days) exhibits substantial tumor-growth inhibition and displays tumor regression at the dose of 25 mg/kg/BID. It is noticed that T1/2 was variable across species (1.98 h in mouse, 4.13 h in rat and 9.80 h in dog).
• In Vitro:
  in vivo SAR439859 induces strong antitumor activity against a variety of BC cell lines and patient-derived xenografts, including models that harbor ERα mutations.

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

cancer, Amcenestrant, antitumor, breast, degrader, degradation, cross-resistance, nonsteroidal, Inhibitor, inhibit, Orally, Estrogen Receptor/ERR, EstrogenReceptor, Estrogen Receptor, ERR, ERα, progestogen Receptor, progestogenReceptor, SAR439859, SAR-439859, SAR 439859, SERD

Compound Identifiers

PubChem CID

130232326