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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 | Availability | Quantity |
---|---|---|---|
1 mg | $147 | In Stock | |
5 mg | $313 | In Stock | |
10 mg | $478 | In Stock | |
25 mg | $789 | In Stock | |
50 mg | $1,080 | In Stock | |
100 mg | $1,480 | In Stock | |
1 mL x 10 mM (in DMSO) | $383 | In Stock |
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]. |
Alias | SAR439859 |
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 | Powder: -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
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