生物活性
Devimistat (CPI-613) 是Lipoate类似物,抑制线粒体酶pyruvate dehydrogenase (PDH)(丙酮酸脱氢酶)和α-ketoglutarate dehydrogenase(α-酮戊二酸脱氢酶),干扰肿瘤细胞线粒体代谢。
化学数据
| 分子量 | 388.59 |
| 分子式 | C22H28O2S2 |
| CAS号 | 95809-78-2 |
| 纯度 | 99.78% |
| 溶解性(25°C) | DMSO 48 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 | BxPC-3 human pancreatic tumor cells |
| 方法 | BxPC-3 human pancreatic tumor cells were treated with 50 μM CPI-613 or sham treated (i.e., vehicle), whereas the non-transformed NIH-3T3 mouse fibroblast cells were treated with 100 μM CPI-613 or sham treatment (i.e., vehicle), for 6 hours. The duration of treatment with CPI-613 was based on a time course experiment which measured the time taken to induce death in 10-15% of the cells. At the end of the 6-hour treatment period, live cells were selected based on Trypan blue exclusion and quantified using a hemocytometer. |
| 浓度 | 100 μM |
| 处理时间 | 6 h |
| 动物实验 |
|---|
| 动物模型 | CD1-Nu/Nu female mice |
| 配制 | PBS |
| 剂量 | 25 mg/kg |
| 给药处理 | i.p. |
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 | 2.5734 mL | 12.867 mL | 25.7341 mL |
| 5 mM | 0.5147 mL | 2.5734 mL | 5.1468 mL |
| 10 mM | 0.2573 mL | 1.2867 mL | 2.5734 mL |