Home Endocrinology & Hormones Estrogen/progestogen Receptor antagonist Amcenestrant (SAR439859) For research use only.

Amcenestrant (SAR439859)

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.

Amcenestrant (SAR439859) Chemical Structure

Amcenestrant (SAR439859) Chemical Structure

CAS No. 2114339-57-8

Purity & Quality Control

Batch: S960901 DMSO]100 mg/mL]false]Ethanol]100 mg/mL]false]Water]Insoluble]false Purity: 99.92%
99.92

Amcenestrant (SAR439859) Related Products

Signaling Pathway

Estrogen/progestogen Receptor Signaling Pathways

Estrogen/progestogen Receptor Signaling Pathway

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
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]
Cell Research 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.
In Vivo
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.
Animal Research 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
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03816839 Active not recruiting
Breast Cancer
Sanofi
 March 25 2019 Phase 1

Chemical Information & Solubility

Molecular Weight 554.48 Formula

C31H30Cl2FNO3
CAS No. 2114339-57-8 SDF --
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
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (180.34 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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

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