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

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

Dihydro-5-azacytidine (DHAC) 是一种核苷类似物,可掺入 DNA 并抑制 DNA 甲基化 (DNA methylation)。Dihydro-5-azacytidine 具有抗肿瘤活性。

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

Dihydro-5-azacytidine Chemical Structure

CAS No. : 62488-57-7

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生物活性

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

体外研究
(In Vitro)

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

246.22

Formula

C8H14N4O5

CAS 号

62488-57-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [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.

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