生物活性
Clofarabine能抑制核苷酸还原酶(IC50=65 nM)和DNA聚合酶的酶活性。
化学数据
| 分子量 | 303.68 |
| 分子式 | C10H11ClFN5O3 |
| CAS号 | 123318-82-1 |
| 纯度 | >99% |
| 溶解性（25°C） | DMSO 33 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 | hela cells |
| 方法 | Radiosensitivity assay.
Cells were treated with indicated dose of clofarabine, and then media was changed 20 hours later. The cultures were incubated for 10-12 days, harvested, and stained with 0.5% crystal violet in methanol. The colony number was determined with a dissecting microscope. a population of >50 cells was counted as one colony, and the number of colonies was expressed as a percentage of the value for untreated controls and those treated with clofarabine. the survival curves were plotted by linear regression analyses, and the D0 value represents the radiation dose that lead to 37% survival. |
| 浓度 | 0, 10, 100, and 1000 n M |
| 处理时间 | 4h |
| 动物实验 |
|---|
| 动物模型 | male nude mice bearing DLD-1 human tumour xenografts model |
| 配制 | DMSO/H2O |
| 剂量 | 30mg/kg daily for 12 days |
| 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 | 3.2929 mL | 16.4647 mL | 32.9294 mL |
| 5 mM | 0.6586 mL | 3.2929 mL | 6.5859 mL |
| 10 mM | 0.3293 mL | 1.6465 mL | 3.2929 mL |
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