生物活性
Temozolomide (TMZ)是一种DNA损伤诱导剂。Temozolomide是一种甲基化剂,可穿过血脑屏障,适用于恶性胶质瘤和转移性黑色素瘤。
化学数据
分子量 | 194.15 |
分子式 | C6H6N6O2 |
CAS号 | 85622-93-1 |
纯度 | 99.86% |
溶解性(25°C) | DMSO 18 mg/mL |
储存和运输条件 | -20°C, protect from light, sealed 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 | A2058, A375, M238 and M249 cell lines |
方法 | Colony formation assay Depending on the cell line (and plating efficiency), 200–1000 cells were seeded
into each well of a 6-well plate and treated as described in detail previously. In the case of primary melanoma cells, 1000 cells were seeded and let grow for 24 days in the presence or absence of drug treatment; because only small colonies formed, the stained colonies were counted under the microscope.Survival of melanoma cells after drug treatment. Five different melanoma cell lines (as indicated), as well as a culture of primary melanoma tissue cells (labeled ‘primary’) were exposed to increasing concentrations of TMZ (diamonds) or NEO212 (circles) for 48 hours, and long-term survival was determined via colony formation assay (CFA). |
浓度 | 0, 25, 50, 75, 100μM |
处理时间 | 48 h |
动物实验 |
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动物模型 | A375 cells subcutaneous tumor growth model |
配制 | 45% glycerol, 45% ethanol, 10% DMSO |
剂量 | 50 mg/kg |
给药处理 | subcutaneous injection |
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 | 5.1507 mL | 25.7533 mL | 51.5066 mL |
5 mM | 1.0301 mL | 5.1507 mL | 10.3013 mL |
10 mM | 0.5151 mL | 2.5753 mL | 5.1507 mL |