Dihydro-5-azacytidine  (Synonyms: DHAC; NSC 264880)

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

Methylation studies show that an LD₁₀ dose 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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 t_1/2 α of 1.03 h and a t_1/2 β of 5 h^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

246.22

C₈H₁₄N₄O₅

62488-57-7

NC(NC1)=NC(N1[C@H]2[C@H](O)[C@H](O)[C@@H](CO)O2)=O

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• [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.  [Content Brief]

  [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.  [Content Brief]