Clofarabine(Synonyms: 氯法拉滨)

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Clofarabine (Synonyms: 氯法拉滨) 纯度: 99.92%

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)。

Clofarabine(Synonyms: 氯法拉滨)

Clofarabine Chemical Structure

CAS No. : 123318-82-1

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10 mM * 1 mL in DMSO ￥567 In-stock
10 mg ￥515 In-stock
50 mg ￥1989 In-stock
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生物活性

Clofarabine, a nucleoside analogue for research of cancer, is a potent inhibitor of ribonucleotide 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 (IC50 values=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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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 LD50 are found at various time points especially at 12:00 noon and 12:00 midnight[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Clinical Trial

分子量

303.68

Formula

C10H11ClFN5O3
CAS 号

123318-82-1
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
溶解性数据
In Vitro: 

DMSO : ≥ 50 mg/mL (164.65 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 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

*

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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 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 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Peter L Bonate, et al. Discovery and development of clofarabine: a nucleoside analogue for treating cancer. Nat Rev Drug Discov. 2006 Oct;5(10):855-63.

    [2]. Hai-Bo Liu, et al. [Effect of clofarabine on proliferation and Bcl-2 expression of NB4 cells]. Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2012 Jun;20(3):571-3.

    [3]. Jia-Jie Luan, et al. Dosing-time contributes to chronotoxicity of clofarabine in mice via means other than pharmacokinetics. Kaohsiung J Med Sci. 2016 May;32(5):227-34.

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