Clofarabine抑制核苷酸还原酶的酶活性（IC50 = 65 nM）和 DNA 聚合酶的酶活性。
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Limited Quantity
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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/克罗拉滨 细胞实验
Cell Line
Concentration
Treated Time
Description
References
A375
30 nM
24 hours
Induced G2/M phase cell cycle arrest
J Immunother Cancer. 2025 Feb 6;13(2):e010252.
A549
1 µM
24 hours
Induced G2/M phase cell cycle arrest
J Immunother Cancer. 2025 Feb 6;13(2):e010252.
TC-71
10 µM
48 hours
To evaluate the cytotoxicity of Clofarabine on TC-71 cells, results showed that Clofarabine significantly inhibited cell proliferation.
Oncogene. 2018 Apr;37(16):2181-2196.
RDES
10 µM
48 hours
To evaluate the cytotoxicity of Clofarabine on RDES cells, results showed that Clofarabine significantly inhibited cell proliferation.
Oncogene. 2018 Apr;37(16):2181-2196.
B16F10
1.5 µM
48 hours
Induced apoptosis
J Immunother Cancer. 2025 Feb 6;13(2):e010252.
A4573
3 µM
6 hours
To evaluate the cytotoxicity of Clofarabine on A4573 cells, results showed that Clofarabine significantly inhibited cell proliferation.
Oncogene. 2018 Apr;37(16):2181-2196.
K562 cells
8 nM
72 hours
To evaluate the therapeutic effects of Clofarabine in combination with RSV or ATRA on CML cells, the results showed significant inhibition of cell growth and induction of caspase-3-dependent apoptosis.
Mol Med Rep. 2019 Oct;20(4):3597-3608.
Clofarabine/克罗拉滨 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
SCID/beige mice
TC-71 xenograft model
Oral
30 mg/kg
Once daily for 14 days
To evaluate the antitumor activity of Clofarabine in the TC-71 xenograft model, results showed that Clofarabine significantly inhibited tumor growth and prolonged event-free survival.
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