生物活性

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.

体外研究

体内研究

30% Propylene glycol, 5% Tween 80, 65% D5W(5%葡萄糖水溶液)

激酶实验

细胞实验

0 -100 ng/mL

动物实验

≤2.5 mg/kg 腹腔注射

不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

参考文献

[1] Shaker S, et al. Leuk Res, 2003, 27(5), 437-444.
[2] Zhu, W G., et al., 2001. DNA methyltransferase inhibition enhances apoptosis induced by histone deacetylase inhibitors. Cancer research. 61(4): 1327-33.
[3] Takebayashi, S., et al., 2001. 5-Aza-2'-deoxycytidine induces histone hyperacetylation of mouse centromeric heterochromatin by a mechanism independent of DNA demethylation. Biochemical and biophysical research communications. 288(4): 921-6.
[4] Jones, P A., et al., 1980. Cellular differentiation, cytidine analogs and DNA methylation. Cell. 20(1): 85-93.

体内溶解度

Clinical Trial Information ( data from http://clinicaltrials.gov )

注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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