2',3',5'-triacetyl-5-Azacytidine

2',3',5'-triacetyl-5-Azacytidine

Catalog Number:
L002372949APE
Mfr. No.:
APE-C4119
Price:
$209
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      • Overview
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          Background

          2',3',5'-triacetyl-5-Azacytidine (TAC) is the lead prodrug form of 5-azacytidine which may be rapidly absorbed after oral administration [1]. 5-Azacytidine is an inhibitor of DNA methyltransferase [2].
          The DNA methyltransferase belongs to a family of enzymes involved in catalyzing the transfer of a methyl group to DNA. DNA methylation has been implicated in regulating gene expression in normal and malignant cells [2].
          In vivo: In CD-1 mice, oral administration of TAC for five days per week for 2 weeks didn’t result in animal deaths and weight loss, but induced changes in hematological parameters, lymph nodes, bone marrow, and duodenal epithelium. TAC inhibited global DNA methylation in the spleen and gut. In an in vivo L1210 leukemia model, TAC exhibited antineoplastic activity [1].

          [1] Ziemba A, Ramirez M C, Freeman B, et al. Abstract# 3369: Development of oral demethylating agents for the treatment of myelodysplastic syndrome[J]. 2009.
          [2] Brueckner B, Boy R G, Siedlecki P, et al. Epigenetic reactivation of tumor suppressor genes by a novel small-molecule inhibitor of human DNA methyltransferases[J]. Cancer research, 2005, 65(14): 6305-6311.

      • Properties
        • Alternative Name
          4-amino-1-(2,3,5-tri-O-acetyl-β-D-ribofuranosyl)-1,3,5-triazin-2(1H)-one
          CAS Number
          10302-78-0
          Molecular Formula
          C14H18N4O8
          Molecular Weight
          370.3
          Appearance
          A crystalline solid
          Purity
          Purity ≥95.00%
          Solubility
          ≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide
          Storage
          Store at -20°C

          * For Research Use Only

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