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Amcenestrant

🥰Excellent
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

Amcenestrant

🥰Excellent
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 SizePriceAvailabilityQuantity
1 mg$147In Stock
5 mg$313In Stock
10 mg$478In Stock
25 mg$789In Stock
50 mg$1,080In Stock
100 mg$1,480In Stock
1 mL x 10 mM (in DMSO)$383In Stock
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Purity:99%
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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].
AliasSAR439859
Chemical Properties
Molecular Weight554.48
FormulaC31H30Cl2FNO3
Cas No.2114339-57-8
SmilesOC(=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
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 125 mg/mL (225.44 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.8035 mL9.0175 mL18.0349 mL90.1746 mL
5 mM0.3607 mL1.8035 mL3.6070 mL18.0349 mL
10 mM0.1803 mL0.9017 mL1.8035 mL9.0175 mL
20 mM0.0902 mL0.4509 mL0.9017 mL4.5087 mL
50 mM0.0361 mL0.1803 mL0.3607 mL1.8035 mL
100 mM0.0180 mL0.0902 mL0.1803 mL0.9017 mL

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