Table 1.
IC50-shift analysis of the combination effects of ensartinib (10 µM) with the cytostatic substrates daunorubicin or mitoxantrone in MDCKII and HL60 cell lines.
| Cell Line | Drug(s) | IC50
1 (µM) |
95% CI (µM) | RR2 |
|---|---|---|---|---|
| MDCKII-parent | ||||
| daunorubicin | 0.947 | (0.814–1.07) | ||
| mitoxantrone | 1.59 | (1.39–1.64) | ||
| daunorubicin + ensartinib | 0.673 ns | (0.551–0.743) | 1.41 | |
| mitoxantrone + ensartinib | 0.955 ns | (0.746–1.13) | 1.66 | |
| MDCKII-ABCB1 | ||||
| daunorubicin | 11.9 | (10.7–12.9) | ||
| daunorubicin + ensartinib | 1.06 **** | (0.743–1.22) | 11.2 | |
| MDCKII-ABCG2 | ||||
| mitoxantrone | 9.98 | (8.91–11.5) | ||
| mitoxantrone + ensartinib | 1.62 *** | (1.22–1.98) | 6.16 | |
| HL60-parent | ||||
| daunorubicin | 0.0531 | (0.0473–0.0589) | ||
| mitoxantrone | 0.0305 | (0.230–0.0370) | ||
| daunorubicin + ensartinib | 0.0221 ns | (0.0169–0.0340) | 2.40 | |
| mitoxantrone + ensartinib | 0.0089 ns | (0.0059–0.0119) | 3.43 | |
| HL60-ABCB1 | ||||
| daunorubicin | 2.39 | (1.61–2.53) | ||
| daunorubicin + ensartinib | 0.108 **** | (0.0664–0.2248) | 22.1 | |
| HL60-ABCG2 | ||||
| mitoxantrone | 0.666 | (0.520–0.823) | ||
| mitoxantrone + ensartinib | 0.0359 **** | (0.0197–0.0603) | 18.6 | |
1 These values were calculated using the data shown in Figure 6. The IC50 values for the combinations were compared to those of daunorubicin or mitoxantrone alone in the appropriate cell lines using the two-tailed unpaired t-test (*** p < 0.001; **** p < 0.0001); 2 The reversal ratio (RR) is the ratio of the IC50 for single drug treatment to that for the combined drug treatment in the cell line of interest.