生物活性
Torkinib (PP242)是一种选择性的mTOR抑制剂，IC50为8 nM；靶向作用于mTOR复合体，作用于mTOR比作用于PI3Kδ或PI3Kα/β/γ选择性分别高10倍多和100倍。
化学数据
| 分子量 | 308.34 |
| 分子式 | C16H16N6O |
| CAS号 | 1092351-67-1 |
| 纯度 | >99% |
| 溶解性（25°C） | DMSO 50 mg/mL |
| 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 |
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-3, SKOV3, 786-O, and U87 cells |
| 方法 | In vitro proliferation and drug combination experiments.
Cells were seeded in triplicate wells of 96-well flat bottom culture plates for 48 hr in the presence of increasing concentrations of indicated inhibitors. Cell viability and median-effect dose affecting growth (GIC50) was determined using the MTS assay (Cell Titer 96 Aqueous One solution cell proliferation assay kit; Promega). Absorbance values (490 nm) were normalized to controls and expressed as %MTS conversion. Wells lacking cells but with MTS added were used as the zero value when normalizing. For drug combination experiments, a range of fixed ratios of inhibitors was used to assess synergy using the combination index (CI) with CalcuSyn software (Biosoft) according to the median-effect method as previously described 2. For proliferation experiments with PC-3, SKOV3, 786-O, and U87 cells, the CellTiter-Glo Luminesecent reagent (Promega) was used following the manufacturer’s instructions. Quantitation was performed as mentioned above. |
| 浓度 | 0~10 μM |
| 处理时间 | 48 h |
| 动物实验 |
|---|
| 动物模型 | xenograft experiments with human Ph+ leukemia |
| 配制 | PEG400 or 5% NMP, 15% PVP, 80% water |
| 剂量 | 60mg/kg once daily |
| 给药处理 | oral |
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 | 3.2432 mL | 16.2159 mL | 32.4317 mL |
| 5 mM | 0.6486 mL | 3.2432 mL | 6.4863 mL |
| 10 mM | 0.3243 mL | 1.6216 mL | 3.2432 mL |
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