Summary of mean Papp values and efflux ratios for compounds tested in Transwell assays
Data for all compounds were from three to four individual experiments, except the data for flavopiridol in inducible Bcrp cells are presented as the average of two individual experiments.
Flavopiridol | Imatinib | PF-407288 | Prazosin | |||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| A>B | B>A | ER | A>B | B>A | ER | A>B | B>A | ER | A>B | B>A | ER | |||||||||||||||||||||||||
| Mean | SD | Mean | SD | Mean | SD | Mean | SD | Mean | SD | Mean | SD | Mean | SD | Mean | SD | |||||||||||||||||||||
| × 10-6 cm/s | × 10-6 cm/s | × 10-6 cm/s | × 10-6 cm/s | |||||||||||||||||||||||||||||||||
| MDCKa | 16.6 | 3.1 | 14.1 | 2.0 | 0.9 | 3.9 | 0.4 | 15.5 | 2.0 | 4.0 | 13.6 | 2.9 | 9.8 | 3.1 | 0.7 | 11.0 | 2.0 | 21.3 | 3.9 | 1.9 | ||||||||||||||||
| MDR1a | 10.6 | 2.8 | 29.3 | 3.9 | 2.8 | 1.3 | 0.2 | 23.9 | 3.7 | 18.9 | 9.8 | 2.7 | 7.8 | 2.1 | 0.8 | 6.8 | 1.9 | 27.3 | 4.8 | 4.0 | ||||||||||||||||
| Mdr1aa | 13.5 | 1.4 | 36.7 | 4.7 | 2.7 | 1.9 | 0.5 | 30.9 | 5.0 | 16.1 | 10.7 | 1.1 | 8.4 | 1.7 | 0.8 | 8.6 | 1.0 | 37.7 | 11.3 | 4.4 | ||||||||||||||||
| BCRPa | 9.4 | 1.1 | 51.0 | 8.0 | 5.4 | 3.7 | 1.7 | 34.6 | 2.5 | 9.4 | 4.4 | 0.5 | 21.0 | 5.9 | 4.8 | 4.9 | 1.0 | 39.5 | 2.0 | 8.1 | ||||||||||||||||
| Bcrp Ub | 18.2 | 2.1 | 23.7 | 9.7 | 1.3 | 15.7 | 4.1 | 24.4 | 2.2 | 1.6 | 11.2 | 0.4 | 20.2 | 3.9 | 1.8 | 22.7 | 8.5 | 32.4 | 10.9 | 1.4 | ||||||||||||||||
| Bcrp Ib | 4.0 | 4.4 | 42.9 | 1.3 | 10.7 | 10.1 | 2.0 | 36.6 | 3.9 | 3.6 | 3.4 | 0.7 | 22.8 | 0.8 | 6.7 | 6.5 | 0.8 | 77.8 | 3.1 | 11.9 | ||||||||||||||||
ER, efflux ratio, which was equal to B>A Papp divided by A>B Papp in different cell lines; U, uninduce Bcrp; I, induced Bcrp.
↵ a Human MDR1, mouse Mdr1a, and human BCRP substrate properties were examined in the MDCK cell line stably transfected with MDR1, Mdr1a, or BCRP genes, respectively.
↵ b Mouse Bcrp substrate properties were examined in the MDCK cell line transfected with inducible Bcrp genes.