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    地西他濱是一種脫氧胞苷類似物和細胞分化誘導劑。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形成不可逆共價鍵，通過獨立于DNA甲基化的轉(zhuǎn)錄后機制增加γ珠蛋白的表達。地西他濱在體外重新激活表觀遺傳學沉默的腫瘤抑制基因方面顯示出顯著的功效。在結(jié)腸癌細胞系中，地西他濱可以分別增加HCT116和RKO細胞中未甲基化hMLH1和MGMT啟動子的組蛋白H3-賴氨酸9乙?；?甲基化比率。在T24膀胱癌細胞中，地西他濱可以增加組蛋白H3-賴氨酸9乙?；徒M蛋白H3-賴氨酸4在未甲基化的p14啟動子的甲基化。

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

儲存條件：4°C, protect from light

注意事項:

為了您的安全和健康，請穿實驗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.