地西他濱是一種脫氧胞苷類(lèi)似物和細(xì)胞分化誘導(dǎo)劑。它能夠摻入DNA并與DNA甲基轉(zhuǎn)移酶在靶向DNA甲基化的胞嘧啶位點(diǎn)形成不可逆共價(jià)鍵，通過(guò)獨(dú)立于DNA甲基化的轉(zhuǎn)錄后機(jī)制增加γ珠蛋白的表達(dá)。地西他濱在體外重新激活表觀遺傳學(xué)沉默的腫瘤抑制基因方面顯示出顯著的功效。在結(jié)腸癌細(xì)胞系中，地西他濱可以分別增加HCT116和RKO細(xì)胞中未甲基化hMLH1和MGMT啟動(dòng)子的組蛋白H3-賴氨酸9乙?；?甲基化比率。在T24膀胱癌細(xì)胞中，地西他濱可以增加組蛋白H3-賴氨酸9乙酰化和組蛋白H3-賴氨酸4在未甲基化的p14啟動(dòng)子的甲基化。

產(chǎn)品性質(zhì):

Cas No.：2353-33-5

別名：地西他濱; 5-Aza-2'-deoxycytidine; 5-AZA-CdR; NSC 127716

化學(xué)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

儲(chǔ)存條件：4°C, protect from light

注意事項(xiàng):

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References:

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[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.