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. 2014 Dec 16;6(4):632–650. doi: 10.3390/pharmaceutics6040632

Table 1.

IC50 and f2 (concentration needed to increase baseline fluorescence two-fold) values for transporter inhibition assays for dovitinib and the corresponding control compound.

Protein Inhibited Cell Model Used Dovitinib f2 [µM] Control Compound f2 [µM]
P-gp L-MDR1 48.4 ± 15.6 Verapamil 3.9 ± 1.9 [28]
IC50 [µM] IC50 [µM]
BCRP MDCKII-BCRP 10.3 ± 4.5 Fumitremorgin C 0.7 ± 0.3 [37]
OATP1B1 HEK-OATP1B1 76.5 ± 28.9 Rifampicin 2.4 ± 0.9 [13]
OATP1B3 HEK-OATP1B3 105.2 ± 23.0 Rifampicin 2.1 ± 1.0 [13]