CAS NO: | 10302-78-0 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 370.3 |
Cas No. | 10302-78-0 |
Formula | C14H18N4O8 |
Solubility | ≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide |
Chemical Name | 4-amino-1-(2,3,5-tri-O-acetyl-β-D-ribofuranosyl)-1,3,5-triazin-2(1H)-one |
Canonical SMILES | O=C1N([C@@H]2O[C@H](COC(C)=O)[C@@H](OC(C)=O)[C@H]2OC(C)=O)C=NC(N)=N1 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
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].
References:
[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.