Clofarabine|123318-82-1|(氯法拉滨)-陌孚医药/Medlife

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Clofarabine (Synonyms: 氯法拉滨)

目录号: PC10248 纯度: ≥98%

CAS No. :123318-82-1

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中文名称

Clofarabine

中文别名

2-氯-9-(2-去氧-2-氟-bata-D-阿拉伯呋喃)-9H-嘌呤-6-胺;氯法拉滨;克罗拉宾;克罗他滨;氯伐他滨;氯法拉宾;氯法拉滨(克罗拉滨);克罗拉滨;Clofarabine 克罗拉滨;安妥明;咳必清-枸橼酸喷托维林;克罗拉滨（氯法拉滨）;氯法拉滨(又叫克罗拉滨);氯法拉滨clofarabine;奈必洛尔;2-氯-9-(2-脱氧-2-氟-β-D-呋喃阿拉伯糖基)腺嘌呤;氯法拉滨,2-氯-9-(2-去氧-2-氟-bata-D-阿拉伯呋喃)-9H-嘌呤-6-胺;硝酸镉,四水

英文名称

Clofarabine

英文别名

clofarabine;5-(6-amino-2-chloro-purin-9-yl)-4-fluoro-2-(hydroxymethyl)oxolan-3-ol;2-CHLORO-2'-ARABINOFLUORO-2'-DEOXYADENOSINE;CAFDA;2-chloro-9-(2-deoxy-2-fluoroarabinofuranosyl)adenine;2-chloro-9-(2-deoxy-2-fluoro-beta-d-arabinofuranosyl)-9h-purin-6-amin;2-chloro-9-(2-deoxy-2-fluoro-beta-d-arabinofuranosyl)adenine;Clolar;Clofarabine & its intermediates（R&D）;(2R,3R,4S,5R)-5-(6-amino-2-chloropurin-9-yl)-4-fluoro-2-(hydroxymethyl)oxolan-3-ol;2-chloro-2'-arabino-fluoro-2'-deoxyadenosine;2-Chloro-9-(2-deoxy-2-fluoro-β-D-arabinofuranosyl)adenine;CadMiuM nitrate tetrahydrate;(2R,3R,4S,5R)-5-(6-amino-2-chloropurin-9-yl)-4-fluoro-2-(hydroxymethyl)oxolan-3-ol, 2-chloro-2′-arabino-fluoro-2′-deoxyadenosine;Evoltra;Clofarex;clofarabinum;clofarabina;C1-F-Ara-A;2-Chloro-9-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl)-9H-purin-6-amine;762RDY0Y2H;(2R,3R,4S,5R)-5-(6-amino-2-chloro-9H-purin-9-yl)-4-fluoro-2-(hydroxymethyl)tetrahydrofuran-3-ol;2-Chloro-9-(2-deoxy-2-fluoro-b-D-arabinofurano

Cas No.

123318-82-1

分子式

C₁₀H₁₁ClFN₅O₃

分子量

303.68

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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.

性状

Solid

体外研究(In Vitro)

Clofarabine potently inhibits DNA synthesis. Clofarabine demonstrates strong 体外研究 growth inhibition and cytotoxic activity (IC₅₀ values=0.028-0.29 μM) in a wide variety of leukaemia and solid tumour cell lines.
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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

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

Cell Line:	NB4 cells
Concentration:	0.01-0.1 μM
Incubation Time:	24 hours
Result:	Apoptosis rate increased obviously.

Western Blot Analysis

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.

Medlife 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)
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.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

ClinicalTrial

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. [Information]

[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. [Information]

[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. [Information]

溶解度数据

体外研究:

DMSO : ≥ 50 mg/mL (164.65 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液

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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： 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 ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 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.

建议依照次序添加每种溶剂： 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。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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