5-Azacytidine

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Chemical Structure| 320-67-2 同义名 : 5-氮杂胞苷;阿托胞苷;阿扎胞苷（5-氮杂胞嘧啶核苷） ;Azacitidine; 5-AzaC; WR 183027; U 18496; NSC 103-627; NSC 102816; Mylosar; Ladakamycin
CAS号 : 320-67-2
货号 : A386837
分子式 : C8H12N4O5
纯度 : 95%
分子量 : 244.2
MDL号 : MFCD00006539
存储条件：

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(122.85 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 25 mg/mL(102.37 mM)，配合低频超声，并水浴加热至45℃助溶
生物活性
靶点

  • DNA Methyltransferase
描述 DNA methyltransferase enzymes (DNMTs) are responsible for the DNA methylation process which could catalyze the transfer of a methyl group from S-adenosyl methionine to the cytosine target nucleotide producing methylcytosine[5].
作用机制 The 5-AZ could inhibit the DNA methylation through covalently binding to DNA methyltransferases, forming nucleoprotein adducts. Therefore, the number of active DNA methyltransferase enzymes in the cells are depletes[9].
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
92.1 0.5/1/2 μM Growth Inhibition Assay 7 d inhibits cell growth in a dose dependent manner 25146981
92.1 0.5/1 μM Function Assay 48 h decreases clonogenicity dose-dependently 25146981
92.1 0.5/1 μM Cell Viability Assay 5 d decreases radiation-induced cell viability inhibition 25146981
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.09mL

0.82mL

0.41mL

20.47mL

4.09mL

2.05mL

40.95mL

8.19mL

4.09mL
参考文献

[1]Christman JK. 5-Azacytidine and 5-aza-2'-deoxycytidine as inhibitors of DNA methylation: mechanistic studies and their implications for cancer therapy. Oncogene. 2002 Aug 12;21(35):5483-95.

[2]Creusot F, Acs G, et al. Inhibition of DNA methyltransferase and induction of Friend erythroleukemia cell differentiation by 5-azacytidine and 5-aza-2'-deoxycytidine. J Biol Chem. 1982 Feb 25;257(4):2041-8.

[3]Mahesh S, Saxena A, et al. Intratracheally administered 5-azacytidine is effective against orthotopic human lung cancer xenograft models and devoid of important systemic toxicity. Clin Lung Cancer. 2010;11(6):405-11.

[4]Heby O, Russell DH. Depression of polyamine synthesis in L1210 leukemic mice during treatment with a potent antileukemic agent, 5-azacytidine. Cancer Res. 1973;33(1):159-65.

[5]Holliday R, Pugh JE. DNA modification mechanisms and gene activity during development. Science. 1975 Jan 24;187(4173):226-32.

[6]Kiziltepe T, Hideshima T, Catley L, Raje N, Yasui H, Shiraishi N, Okawa Y, Ikeda H, Vallet S, Pozzi S, Ishitsuka K, Ocio EM, Chauhan D, Anderson KC. 5-Azacytidine, a DNA methyltransferase inhibitor, induces ATR-mediated DNA double-strand break responses, apoptosis, and synergistic cytotoxicity with doxorubicin and bortezomib against multiple myeloma cells. Mol Cancer Ther. 2007 Jun;6(6):1718-27.

[7]Harman RM, Curtis TM, Argyle DJ, Coonrod SA, Van de Walle GR. A Comparative Study on the In Vitro Effects of the DNA Methyltransferase Inhibitor 5-Azacytidine (5-AzaC) in Breast/Mammary Cancer of Different Mammalian Species. J Mammary Gland Biol Neoplasia. 2016 Jun;21(1-2):51-66.

[8]Cao D, Li D, Huang Y, Ma Y, Zhang B, Zhao C, Deng S, Luo M, Yin T, Wei YQ, Wang W. 5-Azacytidine promotes invadopodia formation and tumor metastasis through the upregulation of PI3K in ovarian cancer cells. Oncotarget. 2017 Jun 20;8(36):60173-60187.

[9]Griffin PT, Niederhuth CE, Schmitz RJ. A Comparative Analysis of 5-Azacytidine- and Zebularine-Induced DNA Demethylation. G3 (Bethesda). 2016 Sep 8;6(9):2773-80.