生物活性
Monastrol是一种小的细胞渗透性分子,通过特异性抑制驱动蛋白-5家族成员Eg5来阻止有丝分裂细胞,IC50值为14 μM。在HeLa细胞中,Monastrol处理分裂细胞导致纺锤体塌陷和细胞周期停滞,引起凋亡。实时细胞生长动力学分析显示,Monastrol治疗可降低MCF-7肿瘤细胞的细胞活力,使细胞增殖减少。
化学数据
分子量 | 292.35 |
分子式 | C14H16N2O3S |
CAS号 | 329689-23-8 |
纯度 | 98.24% |
溶解性(25°C) | DMSO: 50 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 |
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细胞系 | BS-C-1 (monkey epithelial kidney) cells |
方法 | For the double thymidine arrest, exponentially growing BS-C-1 cells are cultured for 16 h in normal growth medium containing 2 mM thymidine. After this, the cells are released into normal growth medium supplemented with 24 μM deoxycytidine for 9 h. The second thymidine block is imposed for 16 h during which the cells were maintained in serum-free medium containing 2 mM thymidine. Finally, the cells are released into normal growth medium containing 24 μM deoxycytidine to which is added either 100 μM monastrol or 0.1% DMSO. To assess the reversibility of the effect of monastrol and nocodazole treatment, BS-C-1 cells plated on coverslips are treated for 4 h in normal growth medium containing either 2 μM nocodazole or 100 μM monastrol and then released into normal medium. At the different time points, coverslips are processed for immunofluorescence and the cells in interphase or mitosis are counted and categorized. |
浓度 | 100 μM |
处理时间 | 4 h |
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 |
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1 mM | 3.4206 mL | 17.1028 mL | 34.2056 mL |
5 mM | 0.6841 mL | 3.4206 mL | 6.8411 mL |
10 mM | 0.3421 mL | 1.7103 mL | 3.4206 mL |