| 產(chǎn)品編號(hào) | D51568 |
| 英文名稱 | GLL398 |
| 中文名稱 | |
| 別 名 | 雌激素受體下調(diào)劑 |
| 克 隆 號(hào) | |
| CAS | 2077980-83-5 |
| 理論分子量 | 398.26 kDa |
| 檢測(cè)分子量 | |
| 性 狀 | Lyophilized |
| 保存條件 | Store in dry, dark place for one year. |
| 注意事項(xiàng) | This product as supplied is intended for research use only, not for use in human, therapeutic or diagnostic applications. |
| 產(chǎn)品介紹 |
GLL398 is an Oral Selective Estrogen Receptor Downregulator. GLL398 strongly binds to ERα in a fluorescence resonance energy transfer binding assay (IC50 =1.14 nM) and potently degrades ERα in MCF-7 breast cancer cells (IC50 = 0.21 μM). Most importantly, the introduction of the boronic acid group confers superior oral bioavailability of GLL398 (AUC = 36.9 μg·h/mL) in rats as compared to GW7604 (AUC = 3.35 μg·h/mL). The strikingly favorable pharmacokinetic property of GLL398 makes it a promising oral SERD suitable for clinical evaluation. |
