Dihydro-5-azacytidine (DHAC), the nucleoside analog, is incorporated into DNA and inhibitsDNA methylation. Dihydro-5-azacytidine has an antitumor activity^[1][2].

Methylation studies show that an LD₁₀dose of [3H]DHAC results in a 25.06% hypomethylation of DNA in L1210/0 cells and a 46.32% hypomethylation in a deoxycytidine kinase mutant cell line L1210/dCK(-), compared with their respective controls^[2].
Dihydro-5-azacytidine (DHAC) competes with cytidine triphosphate for incorporation into RNA, leading to ribosomal degradation and defective protein synthesis^[1].

In tumor-bearing mice (injected with L1210/0 cells), after an LD₁₀dose of Dihydro-5-azacytidine (DHAC; 1500 mg/kg), the plasma peak concentration achieved is 317 μM and is eliminated biexponentially, with a t_1/2α of 1.03 h and a t_1/2β of 5 h^[2].

246.22

C₈H₁₄N₄O₅

62488-57-7

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