地西他滨是一种脱氧胞苷类似物和细胞分化诱导剂。它能够掺入DNA并与DNA甲基转移酶在靶向DNA甲基化的胞嘧啶位点形成不可逆共价键，通过独立于DNA甲基化的转录后机制增加γ珠蛋白的表达。地西他滨在体外重新激活表观遗传学沉默的肿瘤抑制基因方面显示出显著的功效。在结肠癌细胞系中，地西他滨可以分别增加HCT116和RKO细胞中未甲基化hMLH1和MGMT启动子的组蛋白H3-赖氨酸9乙酰化:甲基化比率。在T24膀胱癌细胞中，地西他滨可以增加组蛋白H3-赖氨酸9乙酰化和组蛋白H3-赖氨酸4在未甲基化的p14启动子的甲基化。

产品性质:

Cas No.：2353-33-5

别名：地西他滨; 5-Aza-2'-deoxycytidine; 5-AZA-CdR; NSC 127716

化学名：4-amino-1-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-1,3,5-triazin-2-one

Canonical SMILES：C1C(C(OC1N2C=NC(=NC2=O)N)CO)O

分子式：C8H12N4O4

分子量：228.08

溶解度：≥ 11.4 mg/mL in DMSO, ≥ 23.3 mg/mL in Water with gentle warming

储存条件：4°C, protect from light

注意事项:

为了您的安全和健康，请穿实验服并戴一次性手套操作。

References:

[1].Carlo Stresemann, Frank Lyko. Modes of action of the DNA methyltransferase inhibitors azacytidine and decitabine. International Journal of Cancer. 2008; 123(1): 8 – 13.

[2].Jean-Pierre J. Issa, Guillermo Garcia-Manero, Francis J. Giles, Rajan Mannari, Deborah Thomas, Stefan Faderl, Emel Bayar, John Lyons, Craig S. Rosenfeld, Jorge Cortes, and Hagop M. Kantarjian. Phase 1 study of low-dose prolonged exposure schedules of the hypomethylating agent 5-aza-2’-deoxycytidine (decitabine) in hematopoietic malignancies. Blood. 2004; 103 (5): 1635 – 40.

[3].Hagop Kantarjian, Yasuhiro Oki, Guillermo Garcia-Manero, Xuelin Huang, Susan O’Brien, Jorge Cortes, Stefan Faderl, Carlos Bueso-Ramos, Farhad Ravandi, Zeev Estrov, Alessandra Ferrajoli, William Wierda, Jianqin Shan, Jan Davis,

[4].Francis Giles, Hussain I. Saba, and Jean-Pierre J. Issa. Results of a randomized study of 3 schedules of low-dose decitabine in higher-risk myelodysplastic syndrome and chronic myelomonocytic leukemia. Blood. 2007; 109 (1): 52 – 57.

[5].Stuart A. Scotta, Wei-Feng Donga, Calley Hirscha, David Sheridana, Stephen E. Sanchea, C. Ronald Geyera, John F. DeCoteau. 5-Aza-2-deoxycytidine (decitabine) can relieve p21WAF1 repression in human acute myeloid leukemia by a mechanism involving release of histone deacetylase 1 (HDAC1) without requiring p21WAF1 promoter demethylation. Leukemia Research. 2006; 30(1): 69 – 76.