Table 1. Nonlinear Regression Analysis of Transport Activity of Fluorescent Substrates after 48 h Exposure to Cetuximab in ciPTEC-OAT1a.
| +EGF |
–EGF |
+EGF+CTX |
–EGF+CTX |
|||||
|---|---|---|---|---|---|---|---|---|
| Km (μM) | Vmax (a.u.) | Km (μM) | Vmax (a.u.) | Km (a.u.) | Vmax (a.u.) | Km (μM) | Vmax (a.u.) | |
| Fluorescein | 4.3 ± 0.5 | 14.7 ± 0.5 | 5.6 ± 0.5 | 9.6 ± 0.3 | 5.1 ± 0.6 | 9.4 ± 0.4 | 5.4 ± 0.8 | 8.2 ± 0.5 |
| Hoechst 33342 | 21.3 ± 4.3 | 108.7 ± 8.1 | 23.8 ± 4.6 | 81.0 ± 6.0 | 19.15 ± 4.3 | 82.7 ± 6.6 | 22.4 ± 4.3 | 76.2 ± 5.5 |
| Calcein-AM | 36.8 ± 6.3 | 378.7 ± 43.6 | 38.4 ± 6.7 | 272.8 ± 32.4 | 22.4 ± 3.3 | 209 ± 18.0 | 22.7 ± 3.8 | 178.3 ± 17.5 |
| CMFDA | 20.2 ± 1.5 | 436.5 ± 18.1 | 17.5 ± 1.6 | 296.6 ± 14.8 | 13.0 ± 1.6 | 267.2 ± 15.8 | 13.5 ± 1.4 | 250.4 ± 13.1 |
a
Data are expressed as mean values ± SEM of a minimum of two independent assays performed in triplicate. Transport activity is depicted in fluorescent intensity, expressed in arbitrary units (a.u).