Powder: -20°C for 3 years | In solvent: -80°C for 1 year
LSZ-102 is an effective and selective degrader of estrogen receptor (IC50 = 0.2 nM) and can be used in studies about ERα positive breast cancer.
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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サンプルについてお問い合わせ | |||||
1 mg | 在庫あり | ¥ 22,500 | |||
2 mg | 在庫あり | ¥ 34,000 | |||
5 mg | 在庫あり | ¥ 57,000 | |||
10 mg | 在庫あり | ¥ 95,000 | |||
25 mg | 在庫あり | ¥ 159,000 | |||
50 mg | 在庫あり | ¥ 226,000 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 59,000 |
説明 | LSZ-102 is an effective and selective degrader of estrogen receptor (IC50 = 0.2 nM) and can be used in studies about ERα positive breast cancer. |
In vitro | LSZ-102 causes significant degradation of ERα after 24 h when given as a 10 μM solution to MCF-7 cells. LSZ-102 currently in Phase I/Ib trials for the treatment of ERα positive breast cancer. Robust inhibition of cell proliferation in MCF-7 cells is observed upon incubation with LSZ-102 with a half inhibitory concentration of 1.7 nM. Results show that LSZ-102 effectively inhibits the estrogen-induced activation of the ERE-luciferase reporter using charcoal-stripped serum treated with E2 (IC50: 0.3 nM)[1]. |
In vivo | In male Sprague-Dawley rats, LSZ-102 (3 mg/kg) causes 33% bioavailability and a dose-normalized exposure of 620 nM•h. In mice, LSZ-102 (20 mg/kg) causes significant tumor growth inhibition resulting in tumor stasis[1]. |
別名 | LSZ102 |
分子量 | 470.46 |
分子式 | C25H17F3O4S |
CAS No. | 2135600-76-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 90 mg/mL (191.3 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. 詳細
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LSZ-102 2135600-76-7 Endocrinology/Hormones Estrogen Receptor/ERR LSZ 102 LSZ102 Inhibitor inhibitor inhibit