Clofarabine 

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].

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].

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

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].

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

303.68

Solid

C₁₀H₁₁ClFN₅O₃

123318-82-1

O[[email protected]]1[[email protected]](F)[[email protected]](N(C=N2)C3=C2C(N)=NC(Cl)=N3)O[[email protected]@H]1CO

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• [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]