Cross-resistance profile of HEK-293 cells transfected with wild-type or mutant ABCG2 protein
IC50 values are in nanomolars. RR values were obtained by dividing the IC50 value of the ABCG2-transfected cells (482T-10, 482R-2, 482G-2) by the IC50 value of empty vector-transfected cells (pcDNA3-10). Values obtained were from at least six separate experiments. All ABCG2-transfected cell lines had IC50 values that were statistically different from empty vector control with p < 0.05.
Cell Line | SN-38 (IC50) | RR | CPT (IC50) | RR | hCPT (IC50) | RR | BN80915 (IC50) | RR |
|---|---|---|---|---|---|---|---|---|
| PcDNA3-10 | 0.7 ± 0.5 | 3.8 ± 2.2 | 1.2 ± 0.4 | 0.16 ± 0.13 | ||||
| 482T-10 | 90 ± 18 | 129 | 7.3 ± 2.0 | 1.9 | 36 ± 18 | 30 | 9.0 ± 1.1 | 56 |
| 482R-2 | 94 ± 48 | 134 | 7.0 ± 1.6 | 1.8 | 8 ± 4.2 | 6.7 | 1.3 ± 0.5 | 8.1 |
| 482G-2 | 123 ± 51 | 175 | 7.4 ± 2.2 | 1.9 | 57 ± 11 | 47.5 | 18 ± 3.9 | 112 |