生物活性
ZSTK474能够抑制I型PI3K亚型，IC50为37 nM，对PI3Kδ作用最显著。
化学数据
| 分子量 | 417.41 |
| 分子式 | C19H21F2N7O2 |
| CAS号 | 475110-96-4 |
| 纯度 | >98% |
| 溶解性（25°C） | DMSO 20 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 | panel of 39 human cancer cell lines |
| 方法 | Analysis of Cell Proliferation Inhibition
The inhibition of cell proliferation was assessed by measuring changes in total cellular protein in a culture of each cell line in the JFCR panel of cell lines after 48 hours of drug treatment by use of a sulforhodamine B assay. The 50% growth inhibition (GI 50 ) value of the drug was calculated as described previously. The graphic representation of a drug’s mean differential growth inhibition for the cell line panel was based on a calcula-tion that used a set of GI 50 values, as described previously. To analyze the correlation between the mean graphs of drug A and drug B, the COMPARE computer algorithm was developed as previously described by Paull et al. The Pearson correla-tion coeffi cient between the mean graphs of drug A and drug B was calculated (n = 39). |
| 浓度 | 0~10μM |
| 处理时间 | 48 h |
| 动物实验 |
|---|
| 动物模型 | Human A549 lung cancer cells, PC-3 prostate cancer cells, and WiDr colon cancer cells tumor xenografts |
| 配制 | 5% hydroxypropylcellulose in water |
| 剂量 | 100, 200, or 400 mg/kg daily from days 0 to 13 |
| 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 | 2.3957 mL | 11.9786 mL | 23.9573 mL |
| 5 mM | 0.4791 mL | 2.3957 mL | 4.7915 mL |
| 10 mM | 0.2396 mL | 1.1979 mL | 2.3957 mL |
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