生物活性
TAS-115 (Pamufetinib) mesylate inhibited the kinase activity of both VEGFR2 and MET and their signal-dependent cell growth as strongly as other known VEGFR or MET inhibitors, with IC50 values of 30 and 32 nM for rVEGFR2 and rMET, respectively.
In vivo, TAS-115 (Pamufetinib) completely suppressed the progression of MET-inactivated tumor by blocking angiogenesis without toxicity when given every day for 6 weeks, even at a serum-saturating dose of TAS-115. TAS-115 (Pamufetinib) induced marked tumor shrinkage and prolonged survival in MET-amplified human cancer-bearing mice. TAS-115 is a unique VEGFR/MET-targeted inhibitor with improved antitumor efficacy and decreased toxicity.
化学数据
| 分子量 | 614.66 |
| 分子式 | C28H27FN4O7S2 |
| CAS号 | 1688673-09-7 |
| 纯度 | >99% |
| 溶解性（25°C） | DMSO 65 mg/mL |
| 储存和运输条件 | 2-8°C, dry, sealed
常温运输及临时存放 |
实验操作 来自于公开的文献，仅供相同实验参考（如实验材料、目的不同，请参考其他文献）
| 细胞实验 |
|---|
| 细胞系 | PC-9 (del E746_A750) and HCC827 |
| 方法 | Tumor cells (8000 cells/800 mL) with or without TAS-115 (1.0 μM) or erlotinib (0.3 μM) in the lower Transwell collagen–coated chambers are cocultured with MRC-5 (1000 cells/300 μL) cells in the upper chamber for 72 hours. The upper chamber is then removed. Cell viability is measured using the MTT assay. |
| 浓度 | 1.0 μmol/liter |
| 处理时间 | 72 hours |
| 动物实验 |
|---|
| 动物模型 | SC-9 tumor-bearing nude mice |
| 配制 | - |
| 剂量 | 12.5, 50, and 200 mg/kg/d |
| 给药处理 | orally |
不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 |
| 重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| 体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km系数 | 3 | 6 | 12 | 8 | 5 | 20 |
| 动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
| 动物 A的Km系数 |
例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。
储备液配制
以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作。
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.6269 mL | 8.1346 mL | 16.2692 mL |
| 5 mM | 0.3254 mL | 1.6269 mL | 3.2538 mL |
| 10 mM | 0.1627 mL | 0.8135 mL | 1.6269 mL |
