Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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 | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 147.00 | |
5 mg | In stock | $ 313.00 | |
10 mg | In stock | $ 478.00 | |
25 mg | In stock | $ 789.00 | |
50 mg | In stock | $ 1,080.00 | |
100 mg | In stock | $ 1,480.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 383.00 |
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 |
Molecular Weight | 554.48 |
Formula | C31H30Cl2FNO3 |
CAS No. | 2114339-57-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 125 mg/mL (225.44 mM), Sonification is recommended.
You can also refer to dose conversion for different animals. More
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Amcenestrant 2114339-57-8 Endocrinology/Hormones Estrogen Receptor/ERR Estrogen/progestogen Receptor breast SAR439859 Inhibitor degradation antitumor cancer SERD inhibit cross-resistance degrader SAR 439859 Orally SAR-439859 nonsteroidal inhibitor