TABLE 1 

EC50 values of anticancer drugs that are substrates of BCRP in MDCKII-MOCK and MDCKII-BCRP cells

For each drug and cell type, the table displays the median EC50 value, range of EC50 (micromolars), number of experimental determinations of EC50 performed (N), and resistance ratio (RR). RR was calculated by dividing the median EC50 for a given drug in the absence of FTC (EC50, −FTC) by the median EC50 of that drug in the presence of FTC (EC50, +FTC) for each cell type.

DrugMDCKII-MOCKMDCKII-BCRP
EC50, −FTC (range)EC50, +FTC (range)NRREC50, −FTC (range)EC50, +FTC (range)NRR
µMµMµMµM
Cytotoxic
 Antimetabolites
  Capecitabine>200 (–)>200 (–)1NC>200 (–)>200 (–)1NC
  Methotrexate0.035 (–)0.028 (–)11.30.047 (–)0.026 (–)11.8
 Topoisomerase I inhibitor
  SN-380.16 (0.14–0.17)0.051 (0.044–0.057)23.16.5 (6.4–6.6)0.070 (0.069–0.070)294
  Topotecan0.39 (0.31–0.46)0.26 (0.19–0.33)21.514 (12–16)0.44 (0.36–0.52)232
 Topoisomerase II inhibitor
  Mitoxantrone0.29 (0.29–0.29)0.26 (0.26–0.26)21.11.2 (1.1–1.3)0.29 (0.28–0.30)34.0
  Etoposide2.8 (–)1.8 (–)11.65.2 (–)2.1 (–)12.5
  Teniposide0.57 (–)0.42 (–)11.41.4 (–)0.47 (–)13.0
Molecular targeted
 Cyclin-dependent kinase inhibitor
  Dinaciclib0.065 (–)0.030 (–)12.20.18 (–)0.027 (–)16.7
  Flavopiridol0.12 (0.12–0.12)0.12 (0.11–0.12)21.00.54 (0.46–0.61)0.097 (0.084–0.11)25.5
  • NC, not calculated.