Decitabine(NSC127716, 5AZA-CdR) (Synonyms: DAC, 5aza2’Deoxycytidine, NSC 127716) |
| カタログ番号GC15255 |
5-アザシチジンの2'デオキシアナログ
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Cas No.: 2353-33-5
Sample solution is provided at 25 µL, 10mM.
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Decitabine(DAC) is a deoxycytidine analogue antimetabolite with oral bioactivity and functions as an inhibitor of DNA methyltransferase. By substituting for cytosine within DNA, Decitabine covalently captures DNA methyltransferases within the DNA structure, thereby inducing irreversible inhibition of this enzyme. Decitabine has been shown to be effective against multiple cancers, including chronic myelomonocytic leukaemia (CMML), acute myeloid leukaemia (AML) [1-3].
Decitabine (10 µM; 0-120hs) treatment significantly inhibited cell growth[4]. Decitabine-pretreated(low-dose:10 nM decitabine; 24h) CD8+ T cells have increased cytotoxicity against tumors following anti-PD-1 treatment[5]. Low-dose decitabine promoted the generation of Myeloid-derived suppressor cells (MDSCs) and enhanced their aerobic metabolism and immunosuppressive functions[6]. Decitabine treatment resulted in an increased CD4:CD8 T-cell ratio and an elevation in the central memory (Tcm, CD45RO + CD62L+) and CD25-positive populations among cultured CAR T cells when compared to CAR T cells[7].
Decitabine (1.0 mg/kg; i.p.; 5days) treatment inhibits tumorigenesis and leads to regression of established tumors in mice[8]. Decitabine (1.0 mg/kg, p.o) in combination with Tetrahydrouridine (THU) causes severe toxicity in female CD-1 mice, along with an elevated sensitivity to Decitabine toxicity correlated with Decitabine plasma levels [9].
References:
[1]. Dhillon S. Decitabine/Cedazuridine: First Approval. Drugs. 2020 Sep;80(13):1373-1378. doi: 10.1007/s40265-020-01389-7. Erratum in: Drugs. 2021 Jan;81(1):179. PMID: 32860582; PMCID: PMC7708383.
[2]. Nakamura M, Nishikawa J, et,al ecitabine inhibits tumor cell proliferation and up-regulates e-cadherin expression in Epstein-Barr virus-associated gastric cancer. J Med Virol. 2017 Mar;89(3):508-517. doi: 10.1002/jmv.24634. Epub 2016 Nov 17. PMID: 27430892.
[3]. Parker WB. Enzymology of purine and pyrimidine antimetabolites used in the treatment of cancer. Chem Rev. 2009 Jul;109(7):2880-93. doi: 10.1021/cr900028p. PMID: 19476376; PMCID: PMC2827868.
[4]. Nakamura M, Nishikawa J, et,al Decitabine inhibits tumor cell proliferation and up-regulates e-cadherin expression in Epstein-Barr virus-associated gastric cancer. J Med Virol. 2017 Mar;89(3):508-517. doi: 10.1002/jmv.24634. Epub 2016 Nov 17. PMID: 27430892.
[5]. Han P, Hou Y, et,al. Low-dose decitabine modulates T-cell homeostasis and restores immune tolerance in immune thrombocytopenia. Blood. 2021 Aug 26;138(8):674-688. doi: 10.1182/blood.2020008477. PMID: 33876188; PMCID: PMC8394906.
[6]. Ni X, Wang L, et,al. Low-dose decitabine modulates myeloid-derived suppressor cell fitness via LKB1 in immune thrombocytopenia. Blood. 2022 Dec 29;140(26):2818-2834. doi: 10.1182/blood.2022016029. PMID: 36037415.
[7]. Wang Y, Tong C, et,al. Low-dose decitabine priming endows CAR T cells with enhanced and persistent antitumour potential via epigenetic reprogramming. Nat Commun. 2021 Jan 18;12(1):409. doi: 10.1038/s41467-020-20696-x. PMID: 33462245; PMCID: PMC7814040.
[8]. Wang LX, Mei ZY, et,al. Low dose decitabine treatment induces CD80 expression in cancer cells and stimulates tumor specific cytotoxic T lymphocyte responses. PLoS One. 2013 May 9;8(5):e62924. doi: 10.1371/journal.pone.0062924. PMID: 23671644; PMCID: PMC3650049.
[9]. Terse P, Engelke K, et,al. Subchronic oral toxicity study of decitabine in combination with tetrahydrouridine in CD-1 mice. Int J Toxicol. 2014 Mar-Apr;33(2):75-85. doi: 10.1177/1091581814524994. Epub 2014 Mar 17. PMID: 24639139; PMCID: PMC4001115.
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