Bioactivity | 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]. |
Invitro | 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]. 0 --> Dihydro-5-azacytidine acetate 相关抗体: |
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]. |
Name | Dihydro-5-azacytidine acetate |
CAS | 2470972-18-8 |
Formula | C10H18N4O7 |
Molar Mass | 306.27 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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. [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. |