Table 2.

Cell cytotoxicity of R547

A. Cell cytotoxicity in a 5-day MTT assay in human tumor cell lines treated with R547
Cell lineOriginp53 statusRetinoblastoma statusIC50* (μmol/L) ± SD
MDA-MB-468Breast carcinomaMutantMutant0.11 ± 0.01
MDA-MB-435Breast carcinomaMutantWild-type0.08 ± 0.01
MCF-7Breast carcinomaWild-typeWild-type0.06 ± 0.01
HCT116Colon carcinomaWild-typeWild-type0.08 ± 0.01
SW480Colon carcinomaMutantWild-type0.07
RKOColon carcinomaWild-typeWild-type0.05
HT-29Colon carcinomaMutantWild-type0.17
HCT15Colon carcinomaMutantWild-type0.61 ± 0.02
H460aLung carcinomaWild-typeWild-type0.06 ± 0.01
C33ACervical carcinomaMutantMutant0.32 ± 0.04
DU145Prostate carcinomaMutantMutant0.08 ± 0.04
OSA-CLOsteosarcomaMutantWild-type0.19
LOXMelanomaWild-typeWild-type0.05
JEKO-1Mantle cell lymphomaMutantWild-type0.08 ± 0.01
REC-1Mantle cell lymphomaWild-typeWild-type0.09 ± 0.03
B. Cytotoxicity in a MDR and non-MDR cell line treated with R547, paclitaxel, and 5-fluorouracil
Cell line
R547, IC50 (μmol/L) ± SD
Paclitaxel, IC50 (μmol/L) ± SD
5-Fluorouracil, IC50 (μmol/L) ± SD
(Non-MDR) KB-3-10.11 ± 0.01<0.0054.32 ± 0.11
(MDR) KB-A-10.39 ± 01.47 ± 05.51 ± 0.36
IC50 (MDR)/IC50 (non-MDR)3>2941
  • NOTE: Values are the concentrations of R547 necessary to inhibit proliferation by 50% and represent the average of at least two separate experiments done in duplicate. The activity of the compounds on the MDR cell line compared with the parental line was calculated by dividing the IC50 in the MDR cell line by the IC50 in the non-MDR cell line.

  • * IC50 is the concentration of drug necessary to inhibit cell proliferation by 50%.