TABLE 1
Cross-resistance profile for novel P-gp substrates in P-gp- or ABCG2-expressing cells
All compounds were tested in triplicate. Results presented are mean GI50 values ± S.D.
| Compound | Structure | GI50 pcDNA | GI50 MDR-19 | RRa P-gp | GI50 R-5 | RRa ABCG2 |
|---|---|---|---|---|---|---|
| μM | μM | μM | ||||
| AT7519 |  | 0.61 ± 0.07 | 66.7 ± 28.2 | 110 | 2.3 ± 0.2 | 4 |
| AT9283 |  | 2.7 ± 0.1 | 34.8 ± 6.8 | 13 | 60.8 ± 1.9 | 22 |
| Ispinesib |  | 0.044 ± 0.037 | 2.8 ± 0.5 | 64 | 0.14 ± 0.09 | 3 |
| Gedatolisib |  | 0.028 ± 0.007 | 47.2 ± 12.8 | 1672 | 2.0 ± 0.3 | 70 |
| GSK-690693 |  | 0.19 ± 0.03 | 56.2 ± 18.8 | 290 | 11.6 ± 1.8 | 60 |
| KW-2478 |  | 0.48 ± 0.04 | 129.7 ± 27.5 | 270 | 4.5 ± 0.2 | 9 |
↵a Relative resistance (RR) value is the ratio of the GI50 (50% growth inhibitory concentration) values of P-gp- or ABCG2-expressing cells (MDR-19 or R-5) to the GI50 value of pcDNA cells.