生物活性
TSR-011 is an orally available ALK inhibitor being developed for the treatment of solid tumors including NSCLC. ALK is known to be involved in certain types of cancers, including subsets of non-small cell lung cancer, neuroblastoma and lymphoma. TSR-011 is a potent inhibitor of both anaplastic lymphoma kinase (ALK) and tropomyosin-related kinases (TRK). Preliminary results after eight weeks of treatment with TSR-011 demonstrated disease control (partial responses plus stable disease) in 11 of 17 (65%) evaluable patients treated with TSR-011.
化学数据
| 分子量 | 577.73 |
| 分子式 | C33H44FN5O3 |
| CAS号 | 1357920-84-3 |
| 纯度 | >98% |
| 溶解性（25°C） | 100 mg/mL in DMSO |
| 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 | 1.7309 mL | 8.6546 mL | 17.3091 mL |
| 5 mM | 0.3462 mL | 1.7309 mL | 3.4618 mL |
| 10 mM | 0.1731 mL | 0.8655 mL | 1.7309 mL |
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