生物活性
TAK-901是一种新型Aurora A/B抑制剂,IC50为21 nM/15 nM,不是有效的细胞JAK2, c-Src和Abl抑制剂。
化学数据
| 分子量 | 504.64 |
| 分子式 | C28H32N4O3S |
| CAS号 | 934541-31-8 |
| 纯度 | 99.89% |
| 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 | A2780, A375, A549, COLO-205, HCT116, PC-3 cells line |
| 方法 | Cell proliferation and viability assays. Cells were plated in 96-well microtiter plates and incubated with serial dilutions of TAK-901 for 72 hours. Cell proliferation was determined by ELISA analysis of bromodeoxyuridine (BrdUrd) incorporation into DNA (Roche Diagnostics). IMR-90 immortalized lung fibroblasts were seeded in 96-well microtiter plates and cultured for 3 to 4 days until confluent. Cells were then incubated with serial dilutions of TAK-901 for 72 hours. The MTS assay was conducted as per the manufacturer's instructions (Promega). The concentration of TAK-901 required to inhibit half of the maximal effective concentration (EC50) was determined from the dose–response curves. |
| 浓度 | 0~8 μM |
| 处理时间 | 72 h |
| 动物实验 |
|---|
| 动物模型 | Nude mice or rats Xenograft models |
| 配制 | 12% Captisol, 25 mmol/L citrate, pH 3.0 |
| 剂量 | 5 μL/mg twice daily |
| 给药处理 | intravenously |
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 | 1.9816 mL | 9.9081 mL | 19.8161 mL |
| 5 mM | 0.3963 mL | 1.9816 mL | 3.9632 mL |
| 10 mM | 0.1982 mL | 0.9908 mL | 1.9816 mL |