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Clofarabine

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Chemical Structure| 123318-82-1 同义名 : 氯法拉滨 ;Clolar;Evoltra;Clolar. Abbreviation: CAFdA.;Clofarabine, US brand names: Clofarex;C1-F-Ara-A
CAS号 : 123318-82-1
货号 : A195550
分子式 : C10H11ClFN5O3
纯度 : 97%
分子量 : 303.677
MDL号 : MFCD00871077
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(164.65 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

2% DMSO+30% PEG 300 +1% Tween 80+water 8 mg/mL

生物活性
靶点

  • ribonucleotide reductase

    Ribonucleotide reductase, IC50:65 nM
描述 Clofarabine (CAFdA or CL-F-Ara-a) is a deoxyadenosine analogue compound that has been used in treatment for relapsed or refractory acute lymphoblastic leukemia (see https://www.fda.gov/). Clofarabine can inhibit DNA synthesis through both inhibition of ribonucleotide reductase activity and DNA polymeraseαactivity. The first, clofarabine is phosphorylated by deoxycytidine kinase to clofarabine triphosphate. Clofarabine triphosphate can compete with dATP for incorporation into A sites of the extending DNA strand catalyzed by both human DNA polymeraseα. The second, clofarabine triphosphate is a potent inhibitor of ribonucleotide reductase and thus depletes the dNTP pool primarily of dCTP and dATP. And this further facilitates clofarabine triphosphate incorporated into the DNA[1]. Though inhibition of DNA synthesis is mainly contributed to the anti-tumor effect, the cytotoxicity of clofarabine can be implemented through induction of DNA damage and mitochondrial damage on CLL cells, thus triggering the apoptosis[2].
作用机制 Clofarabine can inhibit DNA synthesis and DNA strands extension through both inhibition of ribonucleotide reductase and DNA polymeraseα.
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
A549 cells Function assay 5 days Cytostatic activity against human A549 cells after 5 days by SRB assay, GI50=0.086 μM 21711054
BT549 cells Cytotoxicity assay 5 days Cytotoxicity against human BT549 cells after 5 days by SRB assay, GI50=0.065 μM 19929004
CCRF-CEM cell lines Cytotoxicity assay Compound was tested for cytotoxicity against CCRF-CEM cell lines, IC50=0.05 μM 1732556
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.29mL

0.66mL

0.33mL

16.46mL

3.29mL

1.65mL

32.93mL

6.59mL

3.29mL
参考文献

[1]Xie KC, Plunkett W, et al. Deoxynucleotide pool depletion and sustained inhibition of ribonucleotide reductase and DNA synthesis after treatment of human lymphoblastoid cells with 2-chloro-9-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl) adenine. Cancer Res. 1996 Jul 1;56(13):3030-7.

[2]Genini D, Adachi S, et al. Deoxyadenosine analogs induce programmed cell death in chronic lymphocytic leukemia cells by damaging the DNA and by directly affecting the mitochondria. Blood. 2000 Nov 15;96(10):3537-43.

[3]Luan JJ, Zhang YS, 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.