生物活性

RG 108(RG-108) is an inhibitor of DNA methyltransferase with IC50 of 115 nM, does not cause trapping of covalent enzymes. RG 108 inhibits DNA methylation in human cancer cell lines without detectable toxicity in vitro. The compound demethylates and reactivates epigenetically silences tumor suppressor genes.

体外研究

体内研究

激酶实验

细胞实验

1-100 μM

动物实验

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] Brueckner B, et al, Cancer Res, 2005, 65(14), 6305-6311.
[2] Functional diversity of DNA methyltransferase inhibitors in human cancer cell lines. Cancer Res. 66 2794. Schirrmacher et al (2006)
[3] Epigenetic reactivation of tumor suppressor genes by a novel small-molecule inhibitor of DNA methyltransferase. Cancer Res. 65 6305. Stresemann et al (2006)
[4] Stresemann et al (2006) Functional diversity of DNA methyltransferase inhibitors in human cancer cell lines. Cancer Res. 66 2794.
[5] Schirrmacher et al (2006) Synthesis and in vitro evaluation of biotinylated RG108: a high affinity compound for studying binding interactions with human DNA methyltransferases. Bioconjug.Chem. 17 261.

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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