Name: Amcenestrant (SAR439859)
Brand: Selleck Chemicals
SKU: S9609
Rating: 5 (1 reviews)

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

CAS: 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

Related Targets	Estrogen receptor Progesterone receptor ERR	Click to Expand
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Signaling Pathway

Estrogen/progestogen Receptor Signaling Pathway

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
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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT03816839	Active not recruiting	Breast Cancer	Sanofi	March 25 2019	Phase 1

References

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	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years -20°C powder		1 month-20°Cin solvent

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

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

Preparing Stock Solutions

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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

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Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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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