Amcenestrant (SAR439859)

Catalog No.S9609 Batch:S960901

Technical Data

Formula

C₃₁H₃₀Cl₂FNO₃

Molecular Weight

554.48

CAS No.

2114339-57-8

Solubility (25°C)*

In vitro

DMSO

100 mg/mL (180.34 mM)

Ethanol

100 mg/mL (180.34 mM)

Water

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution	5% DMSO 1 95% Corn oil	0.83mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 16.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	5.0mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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.

Protocol (from reference)

Cell Assay:^{^[2]}	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.
Animal Study:^{^[1]}	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

Cell Assay:^{^[2]}

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.

Animal Study:^{^[1]}

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

References

RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.