Larotinib mesylate hydrate
规格
| Cas Number | 2097129-93-4 |
| 规格或纯度 | ≥98% |
| 纯度 | ≥98% |
| 包装 | 50mg 或 10mg 或 25mg |
产品信息
| 品牌 | 阿拉丁 |
| 过滤标签 | IRAK,Btk,Protein Tyrosine Kinase/RTK,Immunology/Inflammation |
| 储存温度 | 2-8°C储存,干燥 |
| 运输条件 | 冰袋运输 |
| 生化和生理学机理 | 甲磺酸拉罗替尼水合物是一种强效广谱口服活性酪氨酸激酶抑制剂（TKI），以表皮生长因子受体（EGFR）为主要靶点，IC 50 为 0.6 nM。 |
| 英文描述 |
Larotinib mesylate hydrate is a potent broad-spectrum and orally active tyrosine kinase inhibitor (TKI) with EGFR as the main target with an IC 50 of 0.6 nM In Vivo After daily administration of Larotinib mesylate hydrate, the no observed adverse effect level (NOAEL) is 10 mg/kg in Sprague-Dawley rats and the lowest observed adverse effect level (LOAEL) is 5 mg/kg in beagle dogs. The maximal tolerable doses (MTDs) are 20 and 25 mg/kg in Sprague-Dawley rats and beagle dogs, respectively . Larotinib mesylate hydrate shows dose-dependent antitumor results and a tumor-inhibiting rate exceeding 60% at 18 mg/kg in a tumor-bearing mice model (data not published) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:EGFR L861Q 0.423 nM (IC 50 ) EGFR L858R 0.563 nM (IC 50 ) EGFR (WT) 0.611 nM (IC 50 ) EGFR T790M 45.2 nM (IC 50 ) HER4 84 nM (IC 50 ) BLK 102 nM (IC 50 ) IRAK-1 167 nM (IC 50 ) BTK 196 nM (IC 50 ) HER2 253 nM (IC 50 ) |