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Fig. 3 | Clinical Epigenetics

Fig. 3

From: Novel prodrugs of decitabine with greater metabolic stability and less toxicity

Fig. 3

Effects of OR-2003 and OR-2100 on in vitro tumor-suppressive activity. a Cell growth inhibition ratio. The IC50 values (μM) of the compounds were analyzed after the treatment using multiple types of cancer cell lines. Although the IC50 value varied among the cell lines, almost identical values were observed for DAC, OR-2003, and OR-2100. b Change in cell growth after treatment of compounds. The effect on growth of HCT116 cells was analyzed by monitoring their growth for 94 h using IncuCyte. OR-2003 and OR-2100 showed a decrease in the cell number similar to that of DAC. Results are shown as mean ± SD. c Reactivation of two tumor-suppressor genes. The re-expression of tumor-suppressor genes known to be methylated in HCT116 cells was analyzed. Both SFRP1 and UCHL1 showed re-expression in a dose-dependent manner. Each RT-qPCR analysis was performed thrice and the results are presented as mean ± SD. d Induction of gene expression by OR-2003 and OR-2100, along with DAC. Expression levels (log2 values) of 58,341 probes obtained by an expression microarray were compared for non-treated cells (x-axis) and drug (1 μM)-treated cells (y-axis). Probes with no change were plotted on the black dashed line, and the genes upregulated more than twofold and to − 1.0 log2 value by the drug treatment are surrounded by the trapezoid with red dashed lines. The numbers for DAC, OR-2003, and OR-2100 were 2011, 2060, and 2041, respectively

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