TABLE 1.
Directional flux of dabrafenib in MDCKII-WT– and MDCKII-Bcrp1–transfected cell lines
Data represent the mean ± S.D. (n = 3).
| Cell Line | Papp
|
ER | CFR | |
|---|---|---|---|---|
| A-to-B | B-to-A | |||
| cm/s ×10−6 | cm/s ×10−6 | |||
| MDCKII-WT | 11.5 ± 1.4 | 14.1 ± 1.4 | 1.2 | — |
| MDCKII-WT + 0.2 μM Ko143 | 16.4 ± 0.9 | 15.3 ± 2.6 | 0.9 | |
| MDCKII-Bcrp1 | 1.3 ± 0.3a | 27.3 ± 4.1a | 21.0 | 17.5 |
| MDCKII-Bcrp1 + 0.2 μM Ko143 | 13.2 ± 2.1b | 9.6 ± 0.33b | 0.7 | |
A, apical; B, basolateral; Bcrp1, breast cancer resistance protein 1; CFR, corrected efflux ratio; ER, efflux ratio; MDCKII, Madin-Darby canine kidney II; Papp, apparent permeability of dabrafenib; WT, wild type.
a
Significantly different compared with respective wild-type control cells.
b
Significantly different compared with untreated Bcrp1 control cells.