Clofarabine是一种用于癌症研究的核苷类似物，是一种有效的核糖核苷酸还原酶 (ribonucleotide reductase) 抑制剂 (IC50=65 nM)。
| 生物活性 | Clofarabine, a nucleoside analogue for research ofcancer, is a potent inhibitor ofribonucleotide reductase(IC50=65 nM) by binding to the allosteric site on the regulatory subunit[1]. |
体外研究
(In Vitro) | Clofarabine potently inhibits DNA synthesis. Clofarabine demonstrates strong in vitro growth inhibition and cytotoxic activity (IC50values=0.028-0.29 μM) in a wide variety of leukaemia and solid tumour cell lines[1].
Clofarabine (0.01-0.1 μM) inhibits proliferation of NB4 cells, which may be related with the down-regulation of Bcl-2 and induction of apoptosis[2].
Cell Viability Assay[2] | Cell Line: | NB4 cells | | Concentration: | 0.01-0.1 μM | | Incubation Time: | 48 hours | | Result: | Inhibited proliferation of NB4 cells in a concentration-depended manner. |
Apoptosis Analysis[2] | Cell Line: | NB4 cells | | Concentration: | 0.01-0.1 μM | | Incubation Time: | 24 hours | | Result: | Apoptosis rate increased obviously. |
Western Blot Analysis[2] | Cell Line: | NB4 cells | | Concentration: | 0.01-0.1 μM | | Incubation Time: | 24 hours | | Result: | Bcl-2 expression decreased obviously. |
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体内研究
(In Vivo) | Clofarabine (330 mg/kg, after a 7-day treatment) causes the death of mice. Higher mortality rates were observed in daytime treatment groups, while more animals survived in night treatment groups. Significant differences of LD50are found at various time points especially at 12:00 noon and 12:00 midnight[3].
| Animal Model: | Kunming mice (18-22 g, with equal numbers of male and female mice)[3] | | Dosage: | 600, 480, 384, 307, 246 mg/kg | | Administration: | Injected intraperitoneally at 8:00 am, 12:00 noon, 8:00 pm and 12:00 midnight; 7 days continuous administration | | Result: | LD50s of 8:00 am, 12:00 noon, 8:00 pm, 12:00 midnight were 333.59, 319.73, 362.58 and 366.92 mg/kg, respectively. |
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| 中文名称 | 克罗拉滨；氯法拉滨；克罗他滨；氯伐他滨；氯法拉宾；氯伐拉滨 |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : ≥ 50 mg/mL(164.65 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 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 |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (6.85 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (6.85 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (6.85 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (6.85 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (6.85 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (6.85 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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