Clofarabine inhibits the enzymatic activities of ribonucleotide reductase (IC50 = 65 nM) and DNA polymerase.
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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.
Clofarabine 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
DU145 cells
Function assay
5 days
Cytostatic activity against human DU145 cells after 5 days by SRB assay, GI50=0.125 μM
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