別品名 |
2'-Deoxy-5-azacytidine,
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別包装 |
あり
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純度 |
>=98%
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分子量 |
228.21
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CAS RN® |
2353-33-5
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化合物の概要 |
Nucleoside (deoxycytidine) analog; DNMT inhibitor, protein synthesis inhibitor.
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構造 |
C8H12N4O4
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溶媒 |
acetic acid: water (1:1): 50 mg/mL
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使用目的 |
Decitabine is a deoxycytidine analog that is incorporated into DNA, inhibiting DNA methyltransferase (DNMT1/3A/3B) activity. This demethylating agent is clinically used to treat myelodysplastic syndromes. Decitabine’s inhibition of DNA methyltransferase may be modulated by PKC. Decitabine exhibits anticancer chemotherapeutic, immunomodulatory, and neurotoxic activities. In cellular models of acute myelogenous leukemia (ALL), decitabine demethylation prevents cancer cell inactivation of TRAIL signaling, increasing apoptosis and cell death. In vivo, decitabine stimulates increases in cancer testis antigen-specific cytotoxic (CD8+) T cell activity. In dopaminergic neurons, this compound induces apoptosis and upregulation of tyrosine hydroxylase and α-synuclein, suggesting complications for use in subjects with Parkinson’s disease. Decitabine also inhibits replication of HIV in cellular models without displaying cytotoxicity. Additionally, this compound shows benefit in the treatment of sickle-cell anemia through its stimulation of fetal hemoglobin production.
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参考文献 |
Zhou JH, Yao YS, Wang LX, et al. Demethylating agent decitabine induces autologous cancer testis antigen specific cytotoxic T lymphocytes in vivo. Chin Med J (Engl). 2013 Dec;126(23):4552-6. PMID: 24286424.Wang Y, Wang X, Li R, et al. A DNA methyltransferase inhibitor, 5-aza-2'-deoxycytidine, exacerbates neurotoxicity and upregulates Parkinson's disease-related genes in dopaminergic neurons. CNS Neurosci Ther. 2013 Mar;19(3):183-90. PMID: 23441691.Soncini M, Santoro F, Gutierrez A, et al. The DNA demethylating agent decitabine activates the TRAIL pathway and induces apoptosis in acute myeloid leukemia. Biochim Biophys Acta. 2013 Jan;1832(1):114-20. PMID: 23046813.Datta J, Ghoshal K, Motiwala T, et al. Novel Insights into the Molecular Mechanism of Action of DNA Hypomethylating Agents: Role of Protein Kinase C δ in Decitabine-Induced Degradation of DNA Methyltransferase 1. Genes Cancer. 2012 Jan;3(1):71-81. PMID: 22893792.Saba HI. Decitabine in the treatment of myelodysplastic syndromes. Ther Clin Risk Manag. 2007 Oct;3(5):807-17. PMID: 18473005.Momparler RL. Pharmacology of 5-Aza-2'-deoxycytidine (decitabine). Semin Hematol. 2005 Jul;42(3 Suppl 2):S9-16. PMID: 16015507.Bouchard J, Walker MC, Leclerc JM, et al. 5-azacytidine and 5-azadeoxycytidine inhibit human immunodeficiency virus type 1 replication in vitro. Antimicrob Agents Chemother. 1990 Feb;34(2):206-9. PMID: 1691617.
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メーカー |
品番 |
包装 |
LKT
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A9603
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50 MG
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※表示価格について
当社在庫 |
なし
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納期目安 |
1週間程度
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保存温度 |
常温
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