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Amcenestrant

Name: Amcenestrant
Brand: TargetMol
SKU: T12832
Price: 84 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T12832Cas No. 2114339-57-8

Alias SAR439859

Amcenestrant (SAR439859) is an orally active, nonsteroidal and selective degrader of estrogen receptor (SERD). SAR439859 is a potent antagonist of ER (with an EC50 of 0.2 nM for ERα degradation).

Amcenestrant

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Purity: 99%

Catalog No. T12832Alias SAR439859Cas No. 2114339-57-8

Amcenestrant (SAR439859) is an orally active, nonsteroidal and selective degrader of estrogen receptor (SERD). SAR439859 is a potent antagonist of ER (with an EC50 of 0.2 nM for ERα degradation).

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$84	In Stock	In Stock
5 mg	$198	In Stock	In Stock
10 mg	$328	In Stock	In Stock
25 mg	$579	In Stock	In Stock
50 mg	$868	In Stock	In Stock
100 mg	$1,290	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$248	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99%

Color:White

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	Amcenestrant (SAR439859) is an orally active, nonsteroidal and selective degrader of estrogen receptor (SERD). SAR439859 is a potent antagonist of ER (with an EC50 of 0.2 nM for ERα degradation).
Targets&IC50	ERα:0.2 nM （EC50）
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[1].
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[1]. 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)[1].
Synonyms	SAR439859

Chemical Properties

Molecular Weight	554.48
Formula	C₃₁H₃₀Cl₂FNO₃
Cas No.	2114339-57-8
Smiles	OC(=O)c1ccc2c(CCCC(c3ccc(Cl)cc3Cl)=C2c2ccc(O[C@H]3CCN(CCCF)C3)cc2)c1
Relative Density.	1.297 g/cm3 (Predicted)

Storage & Solubility Information

Storage

In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 125 mg/mL (225.44 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 8 mg/mL (14.43 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.8035 mL	9.0175 mL	18.0349 mL	90.1746 mL
5 mM	0.3607 mL	1.8035 mL	3.6070 mL	18.0349 mL
10 mM	0.1803 mL	0.9017 mL	1.8035 mL	9.0175 mL
20 mM	0.0902 mL	0.4509 mL	0.9017 mL	4.5087 mL
50 mM	0.0361 mL	0.1803 mL	0.3607 mL	1.8035 mL
100 mM	0.0180 mL	0.0902 mL	0.1803 mL	0.9017 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Amcenestrant

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