Table 1.

Effect of IRC-083927 on the cell proliferation of cell lines resistant to tubulin-binding agents

Cell lines/compoundsIC50 (μmol/L)
MIA PaCa-2MDA-MB-231DU-145NCI-H69NCI-H69/AR (MRP+)NCI-H69/Lx4 (PgP+)A549A549.EpoB40A549.EpoB480
IRC-0839277 ± 015 ± 0.311 ± 0.28 ± 313 ± 242 ± 1110 ± 0.19 ± 0.823 ± 3
Colchicine13 ± 32526 ± 1NDNDNDNDNDND
Navelbine3 ± 163 ± 16 ± 416 ± 2>325NDNDND
Paclitaxel13138 ± 35 ± 0.514 ± 2>1252 ± 1.598 ± 0.32,080 ± 514
AdriamycinNDNDND85 ± 46>3,000>3,000NDNDND
Epothilone BNDNDNDNDNDND0.4 ± 0.268 ± 91,710 ± 163
ABT-751443426469NDNDND1,721 ± 1,0543,711 ± 2,0979,089 ± 372
  • NOTE: The growth inhibition was assayed on human cell lines (MIA PaCa-2, MDA-MB-231, DU-145, NCI-H69, and A549) on human drug-resistant cell lines due to drug efflux pumps [MRP1+ (NCI-H69/AR) and PgP+ (NCI-H69/Lx4)] and on human cell lines resistant to tubulin-binding agents due to the expression of mutated tubulins (A549.EpoB40 and A549.EpoB480) using the WST1 cell proliferation assay. The IC50 values are calculated from at least two independent experiments with four determinations per tested concentration.