Table 1. Chemosensitivity towards drugs, including MDR-associated compounds, as determined by high throughput screening in HCT116, HAB-68mut and HAB-92wt cells.
Drug
|
Cell line, IC50 (M)
|
|||
---|---|---|---|---|
Name | Class (target) | HCT116 | HAB-68mut | HAB-92wt |
Adriamycina | Standard cytotoxic agent | 5,90E-08 | 7,90E-08 | 1,06E-07 |
Paclitaxela | Standard cytotoxic agent | 3,45E-09 | 4,25E-09 | 7,10E-09 |
Vincristinea | Standard cytotoxic agent | 1,20E-08 | 5,80E-09 | 7,10E-09 |
Etoposide (VP-16)a | Standard cytotoxic agent | 3,60E-06 | 3,70E-06 | 4,70E-06 |
Mitoxanthronea | Standard cytotoxic agent | 2,15E-08 | 5,80E-08 | 6,85E-08 |
Topotecana | Standard cytotoxic agent | 1,05E-08 | 2,00E-08 | 4,85E-08 |
Melphalena | Standard cytotoxic agent | 7,60E-06 | 7,10E-06 | 9,60E-06 |
5-Fluorouracila | Standard cytotoxic agent | 4,40E-06 | 4,10E-06 | 4,50E-06 |
Gemcitabine | Standard cytotoxic agent | 9,70E-10 | 8,30E-10 | 1,70E-09 |
5-Azacytidine | Epigenetic modulator | 1,60E-06 | 3,70E-07 | 1,10E-06 |
PXD101 | Epigenetic modulator | 4,60E-07 | 3,30E-07 | 4,20E-07 |
Cyclopamine | Hedgehog pathway | 8,60E-06 | 9,80E-06 | 1,10E-05 |
Bortezomid (Velcade) | Proteasome | 4,50E-09 | 4,10E-09 | 6,20E-09 |
17-DMAG | Heat shock protein | 7,20E-08 | 6,30E-08 | 1,50E-07 |
RHPS4 | Telomerase | 1,80E-05 | 1,80E-05 | 3,40E-05 |
Dasatinib | Kinases | 3,10E-08 | 1,80E-08 | 1,30E-08 |
Erlotinib | Kinases | 1,30E-04 | 1,30E-04 | 1,30E-04 |
Gefitinib (Iressa) | Kinases | 1,60E-05 | 1,60E-05 | 1,70E-05 |
Imatinib (Gleevec) | Kinases | 2,00E-05 | 2,00E-05 | 2,50E-05 |
Lapatinib | Kinases | 1,50E-05 | 1,50E-05 | 2,00E-05 |
PV 1019 | Kinases | 1,70E-05 | 1,60E-05 | 1,70E-05 |
Sunitinib | Kinases | 7,10E-06 | 5,90E-06 | 9,40E-06 |
Sorafenib | Kinases | 5,10E-06 | 4,20E-06 | 5,50E-06 |
SU11274 (Sigma S9820) | Kinases | 5,80E-06 | 3,70E-06 | 8,20E-06 |
By high throughput screening, 24 chemotherapeutic drugs were applied in 18 different concentrations to HCT116, HAB-68mut and HAB-92wt cells. Chemosensitivities of HCT116, HAB-68mut and HAB-92wt cells, expressed as IC50 values and given as averages of triplicates, did not differ significantly despite their differences in β-catenin genotype and ABCB1 expression levels, when comparing HAB-92wt with HCT116 cells, or HAB-92wt with HAB-68mut cells.
Concentration-dependent growth of HCT116, HAB-68mut and HAB-92wt cells, treated with the marked drugs, is illustrated in Figure 7.