TABLE 3

Bidirectional flux studies using MDCK cell monolayers that overexpress mouse bcrp

Inhibition with 20 μM chrysin. Average values from duplicate test runs where variability is < 18%.

CompoundInhibitorA-B PappB-A Papp%CellaERbNERbBODIPY-Prazosin Inhibitionc
nm/s%
Abemaciclib384105811929, 47
+94110521.2
Palbociclib7211804.4161121, 39
+310480241.5
  • 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 BODIPY-prazosin uptake into MDCK-bcrp cells at 5 and 25 μM relative to inhibition using 20 μM chrysin.