Table 1

In vitro cytotoxicity of BMS-275183 against sensitive- and paclitaxel-resistant tumor cell lines and the effect of exposure time

CompoundHCT-116 IC50aHCT-116/MDR R:S ratiobA2780 IC50aA2780/txl R:S ratioc
72 h6 h2 h
Paclitaxel0.0017>690.002816.3
0.00280.0890 (32)d0.1877 (67)Not done
BMS-2751830.00183.90.00463.5
0.00310.1497 (48)d0.2593 (84)Not done
  • a Drug concentration (μm) that inhibited cell growth by 50% was determined after 72 h of exposure unless indicated otherwise within the A2780 column.

  • b HCT-116/MDR R:S ratio, IC50 versus HCT-116/MDR cells divided by IC50 versus HCT-116 cells.

  • c A2780/txl R:S ratio, IC50 versus A2780/txl cells divided by IC50 versus A2780 cells.

  • d Values in parentheses are the fold loss in potency for 6- or 2-h exposures relative to 72-h exposure. The results are the average of three separate experiments.