Amcenestrant (SAR439859)

For research use only.

Catalog No.S9609

Amcenestrant (SAR439859) Chemical Structure

CAS No. 2114339-57-8

Amcenestrant (SAR439859, compound 43d) is an orally available and nonsteroidal selective estrogen receptor degrader (SERD) with potential antineoplastic activity. SAR439859 is a potent estrogen receptor (ER) antagonist with EC50 of 0.2 nM for ERα degradation.

Purity & Quality Control

Choose Selective Estrogen/progestogen Receptor Inhibitors

Biological Activity

Description Amcenestrant (SAR439859, compound 43d) is an orally available and nonsteroidal selective estrogen receptor degrader (SERD) with potential antineoplastic activity. SAR439859 is a potent estrogen receptor (ER) antagonist with EC50 of 0.2 nM for ERα degradation.
Targets
ERα [1]
(Cell-free assay)
0.2 nM(EC50)
In vitro

SAR439859 is a novel, orally bioavailable SERD with potent antagonist and degradation activities against both wild-type and mutant Y537S ER. Driven by its fluoropropyl pyrrolidinyl side chain, SAR439859 has demonstrated broader and superior ER antagonist and degrader activities across a large panel of ER+ cells, including inhibition of ER signaling and tumor cell growth.[2]

In vivo

SAR439859 shows promising antitumor activity in breast cancer mice xenograft models.[1] In vivo treatment with SAR439859 demonstrates significant tumor regression in ER+ breast cancer models, including MCF7-ESR1 wild-type and mutant-Y537S mouse tumors, and HCI013, a patient-derived tamoxifen-resistant xenograft tumor.[2]

Protocol

Cell Research:

[2]

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  • Cell lines: LCC2 cells, MCF7 cells
  • Concentrations: 0.01-1000 nM
  • Incubation Time: 7 days, 4 hours
  • Method:

    Trypsinized cells are dispensed into 384-well plates in IMEM (supplemented with 5% FBS) and after overnight incubation cells are treated with SAR439859 for the times indicated. Cell viability is assessed using CellTiter-Glo according to the manufacturer’s protocol and relative luminescence units (RLU) are measured using an Envision Multilabel Reader. The RLUs of the treated samples are normalized to that of the untreated samples and cell viability is expressed as a percentage of the value of the untreated cells.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: rat, mouse, dog
  • Dosages: 3 mg/kg, 10 mg/kg; 2.5 mg/kg, 5 mg/kg, 12.5 mg/kg, 25 mg/kg
  • Administration: IV, Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (180.34 mM)
Water Insoluble
Ethanol ''''100 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 554.48
Formula

C31H30Cl2FNO3

CAS No. 2114339-57-8
Storage powder
in solvent
Synonyms N/A
Smiles C1CC2=C(C=CC(=C2)C(=O)O)C(=C(C1)C3=C(C=C(C=C3)Cl)Cl)C4=CC=C(C=C4)OC5CCN(C5)CCCF

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03816839 Active not recruiting Drug: Amcenestrant (SAR439859) Breast Cancer Sanofi March 25 2019 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Estrogen/progestogen Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID