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).
パッケージサイズ | 在庫状況 | 単価(税別) | |||
---|---|---|---|---|---|
サンプルについてお問い合わせ | |||||
1 mg | 在庫あり | ¥ 34,000 | |||
5 mg | 在庫あり | ¥ 72,000 | |||
10 mg | 在庫あり | ¥ 110,000 | |||
25 mg | 在庫あり | ¥ 181,000 | |||
50 mg | 在庫あり | ¥ 248,000 | |||
100 mg | 在庫あり | ¥ 340,000 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 88,000 |
説明 | 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). |
ターゲット&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]. |
別名 | SAR439859 |
分子量 | 554.48 |
分子式 | 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), Sonication is recommended.
You can also refer to dose conversion for different animals. 詳細
bottom
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 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