Compound | Inhibitor | A-B Papp | B-A Papp | %Cella | ERb | NERb | Calcein-AM Inhibitionc |
---|---|---|---|---|---|---|---|
nm/s | % | ||||||
Abemaciclib | − | 12 | 49 | 68 | 4.1 | 5.1 | 30, 64 |
+ | 19 | 16 | 56 | 0.8 | |||
Palbociclib | − | 60 | 720 | 46 | 12 | 8.6 | 1, 3 |
+ | 150 | 210 | 32 | 1.4 |
A-B, apical to basal; B-A, basal to apical; ER, efflux ratio; NER, net efflux ratio.
↵a Estimated buffer/cell distribution coefficient defined as the fraction of mass that was added to the donor and recovered in the methanol rinse.
↵b ER is B-A Papp/A-B Papp. NER is ER without inhibitor/ER with inhibitor.
↵c Inhibition of Calcein-AM uptake into MDCK–P-gp cells at 5 and 25 μM relative to inhibition using 5 μM LSN335984.