生物活性
Pelitinib (EKB-569)是一种有效的，不可逆EGFR抑制剂，IC50为38.5 nM。
化学数据
| 分子量 | 467.92 |
| 分子式 | C24H23ClFN5O2 |
| CAS号 | 257933-82-7 |
| 纯度 | >98% |
| 溶解性（25°C） | DMSO 10 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 | A431, SKBR3 and SW620 cells line |
| 方法 | Cell Proliferation Assay.
Three human carcinoma cell lines, A431 (epidermoid carcinoma), SKBR3 (breast carcinoma), and SW620 (colon carcinoma), were used for the cell proliferation assays. All cell lines were obtained from the American Type Culture Collection. Cells were maintained in RPMI-1640 medium supplemented with 5% fetal bovine serum. Cells were plated in 96-well plates at the densities of 5.0 × 104/mL. On the next day, compounds were dosed at 0.5, 5, 50, 500, and 5000 ng/mL concentrations and the cells were cultured for 2 days. At the end of incubation, cell survival was determined by the sulforhodamine B assay as previously described.25 The IC50 values were obtained from the growth curves. |
| 浓度 | 0.5, 5, 50, 500 and 5000 ng/ml |
| 处理时间 | 2 days |
| 动物实验 |
|---|
| 动物模型 | human epidermoid carcinoma A431 tumour xenograft model in Athymic nu/nu female mice |
| 配制 | 0.2% Klucel or with 0.2% Klucel |
| 剂量 | 40 mg/kg for 28 consecutive days |
| 给药处理 | PO. |
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 | 2.1371 mL | 10.6856 mL | 21.3712 mL |
| 5 mM | 0.4274 mL | 2.1371 mL | 4.2742 mL |
| 10 mM | 0.2137 mL | 1.0686 mL | 2.1371 mL |
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