生物活性

Clofarabine is a potent HIV-1 inhibitor in both activated CD4+ T cells and macrophages. Clofarabine inhibits the enzymatic activities of ribonucleotide reductase (IC50 = 65 nM) and DNA polymerase. Due to its minimal toxicity in macrophages, clofarabine displays a selectivity index over 300 in this nondividing cell type. The anti-HIV-1 activity of clofarabine correlated with a significant decrease in both cellular dNTP levels and viral DNA synthesis. Clofarabine triphosphate was directly incorporated into DNA by HIV-1 reverse transcriptase and blocked processive DNA synthesis, particularly at the low dNTP levels found in macrophages.

体外研究

体内研究

激酶实验

细胞实验

动物实验

不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

参考文献

[1] Michele B. Daly,et al. Dual anti-HIV mechanism of clofarabine. Retrovirology. 2016; 13: 20. Published online 2016 Mar 24. doi: 10.1186/s12977-016-0254-0.
[2] Benigno C. Valdez,et al. Mechanistic studies on the synergistic cytotoxicity of the nucleoside analogs gemcitabine and clofarabine in multiple myeloma: Relevance of p53 and its clinical implications. Exp Hematol. Author manuscript; available in PMC 2014 Aug 1. Published in final edited form as: Exp Hematol. 2013 Aug; 41(8): 719–730. Published online 2013 May 3. doi: 10.1016/j.exphem.2013.04.009.

体内溶解度

Clinical Trial Information ( data from http://clinicaltrials.gov )

注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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