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Dihydro-5-azacytidine acetate (DHAC), the nucleoside analog, is incorporated into DNA and inhibits DNA methylation. Dihydro-5-azacytidine acetate has an antitumor activity[1][2]. | [in vivo]
In tumor-bearing mice (injected with L1210/0 cells), after an LD10 dose of Dihydro-5-azacytidine (DHAC; 1500 mg/kg), the plasma peak concentration achieved is 317 μM and is eliminated biexponentially, with a t1/2 α of 1.03 h and a t1/2 β of 5 h[2]. | [References]
[1] Robert A Kratzke, et al. Response to the methylation inhibitor dihydro-5-azacytidine in mesothelioma is not associated with methylation of p16INK4a: results of cancer and leukemia group B 159904. J Thorac Oncol. 2008 Apr;3(4):417-21. DOI:10.1097/JTO.0b013e318168da0a
[2] W C Powell, et al. Biochemical pharmacology of 5,6-dihydro-5-azacytidine (DHAC) and DNA hypomethylation in tumor (L1210)-bearing mice. Cancer Chemother Pharmacol. 1988;21(2):117-21. DOI:10.1007/BF00257356 |
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