生物活性
TAS-102 is an orally administered combination of trifluridine and Tipiracil hydrochloride in a molar ratio of 1:0.5. Trifluridine is the active antitumor component of TAS-102; its monophosphate form inhibits thymidylate synthase, and its triphosphate form is incorporated into DNA in tumor cells.
In vivo, TAS-102 monotherapy has a significant antitumor activity against KM12C/5-FUFU-bearing nude mice. TAS-102 can overcome acquired resistance to 5-FU because the main mechanism of TAS-102 is not associated with main metabolic enzymes of 5-FU, such as TS and OPRT. TAS-102 has demonstrated efficacy in 5-FU-refractory cancers.
化学数据
| 分子量 | 575.32 |
| 分子式 | C19H23Cl2F3N6O7 |
| CAS号 | 733030-01-8 |
| 纯度 | >99% |
| 溶解性（25°C） | DMSO: ≥ 10 mg/mL warmed |
| 储存和运输条件 | 固体粉末： -20°C 冷藏长期储存
常温运输及临时存放 |
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 | 1.7382 mL | 8.6908 mL | 17.3816 mL |
| 5 mM | 0.3476 mL | 1.7382 mL | 3.4763 mL |
| 10 mM | 0.1738 mL | 0.8691 mL | 1.7382 mL |
