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Decitabine (NSC127716, 5AZA-CdR)

现货
Catalog No.
A1906
脱氧胞苷类似物,细胞分化诱导剂。
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 550.00
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10mg
¥ 650.00
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50mg
¥ 2,200.00
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Background

Decitabine is a kind of deoxycytidine analog and an inducer of cellular differentiation. It is able to incorporate into DNA and form irreversible covalent bonds with DNA-methyltransferases at cytosine sites targeted for DNA methylation by increasing γ-globin expression through a posttranscriptional mechanism independent of DNA methylation. Decitabine has been shown substantial efficacy in reactivating epigenetically silenced tumor suppressor genes in vitro. In colon cancer cell lines, decitabine can increase the histone H3-lysine 9 acetylation: methylation ratio at the unmethylated hMLH1 and MGMT promoters in HCT116 and RKO cells, respectively. In T24 bladder cancer cells, decitabine can increase histone H3-lysine 9 acetylation and histone H3-lysine 4 methylation at the unmethylated p14 promoter.

Reference

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

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.

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,

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.

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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt228.08
Cas No.2353-33-5
FormulaC8H12N4O4
Synonyms5-Aza-2'-deoxycytidine;Decitabine
Solubility≥11.4 mg/mL in DMSO, ≥23.3 mg/mL in H2O with gentle warming, <1.18 mg/mL in EtOH
Chemical Name4-amino-1-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-1,3,5-triazin-2-one
SDFDownload SDF
Canonical SMILESC1C(C(OC1N2C=NC(=NC2=O)N)CO)O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验[1]:

细胞系

人类和小鼠黑色素瘤细胞(A375 and B16).

溶解方法

该化合物在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。

反应条件

在第1天和第4天加入0.5 μM的decitabine,在第8天获得图像。

实验结果

Decitabine减少黑素瘤细胞系的细胞增殖并诱导分化的形态学变化。

动物实验[2]:

动物模型

U2OS肿瘤异种移植小鼠

剂量

在第29、31和33天腹膜内给药2.5 mg/kg。在第37天,处死小鼠。

溶解方法

溶于生理盐水(0.9% w/v NaCl)

实验结果

Decitabine显著降低肿瘤异种移植物大小并降低有丝分裂活性,增加凋亡细胞数量和骨基质的生成量。Decitabine还增加促凋亡基因GADD45A、HSPA9B、PAWR、PDCD5、NFKBIA和TNFAIP3的表达(≥2倍)[2]。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

[1]. Alcazar O, Achberger S, Aldrich W, et al. Epigenetic regulation by decitabine of melanoma differentiation in vitro and in vivo. Int J Cancer, 2012, 131(1): 18-29.

[2]. Al-Romaih K, Somers GR, Bayani J, et al. Modulation by decitabine of gene expression and growth of osteosarcoma U2OS cells in vitro and in xenografts: identification of apoptotic genes as targets for demethylation. Cancer Cell Int, 2007, 7: 14.

质量控制

化学结构

Decitabine (NSC127716, 5AZA-CdR)