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. 2021 Jul 29;10:e70429. doi: 10.7554/eLife.70429

Figure 6. CB002-analog #4 has potent anti-tumor effects in vitro and in vivo.

Figure 6.

HCT116 isogenic panel treated with CB002 or analog #4 for 48 hr and their respective IC50 values shown in the table (A). CB002-analog #4 increases apoptotic cells as indicated by the sub-G1 content in cancer cells but not in normal WI38 cells (48 hr). Two-way ANOVA, p<0.0001 (B). 72 hr treatment with CB002-analog #4 is most potent (C) and increases dead cells as indicated by the ethidium homodimer staining (red) compared to calcein stained live cells (green) (A), and cleaved caspase-3 (green) immunofluorescence (D) in colorectal cancer patient-derived organoid cells. CB002-analog #4 decreases ki67 staining (green) in a dose-dependent manner (72 hr) in colorectal cancer patient-derived organoid cells (E). CB002-analog #4 is non-toxic in vivo (F) and significantly reduces tumor volume in NSG mouse xenografts with SW480 wild-type cells (G) but not in SW480 cells with shNoxa (H). 50 mg/kg by oral gavage three times per week, final tumor volume at 5 weeks. Unpaired t-test, p<0.05.