生物活性
IMB5046 is a microtubule inhibitor that has antitumor activity, overcoming multidrug-resistance. IMB5046 was cytotoxic with an IC50range of 37 to 426 nM against multiple tumor cell lines, including some that were resistant to colchicine, vincristine and paclitaxel. IMB5046 was also active against human lung tumor xenografts. IMB5046 was found to bind to tubulin at the colchicine site, but with a different binding mode. IMB5046 inhibited tubulin polymerization, and induced G2/M arrest.
化学数据
| 分子量 | 388.44 |
| 分子式 | C19H20N2O5S |
| CAS号 | 1001571-08-9 |
| 纯度 | >98% |
| 溶解性（25°C） | DMSO: 20 mg/mL
clear |
| 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 |
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 | 2.5744 mL | 12.872 mL | 25.744 mL |
| 5 mM | 0.5149 mL | 2.5744 mL | 5.1488 mL |
| 10 mM | 0.2574 mL | 1.2872 mL | 2.5744 mL |
