IC50 Values for FLT3 TKI sensitive and resistant cell lines
| . | CEP-5214, nM . | CEP-701, nM . | PKC412, nM . | AG1295, μM . |
|---|---|---|---|---|
| SEM-K2 | 29 | 23 | 96 | 10 |
| SEM(R)5214 | > 250 | 238 | > 250 | > 20 |
| SEM(R)701 | > 250 | 65 | > 250 | > 20 |
| MOLM14 | 3 | 12 | 27 | 1.6 |
| M14(R)5214 | > 250 | 170 | 165 | > 20 |
| M14(R)701 | > 250 | 51 | 158 | > 20 |
| Hb1119 | 104 | 14 | 125 | > 20 |
| Hb(R)5214 | > 250 | 85 | 226 | > 20 |
| Hb(R)701 | 147 | 88 | 199 | > 20 |
| . | CEP-5214, nM . | CEP-701, nM . | PKC412, nM . | AG1295, μM . |
|---|---|---|---|---|
| SEM-K2 | 29 | 23 | 96 | 10 |
| SEM(R)5214 | > 250 | 238 | > 250 | > 20 |
| SEM(R)701 | > 250 | 65 | > 250 | > 20 |
| MOLM14 | 3 | 12 | 27 | 1.6 |
| M14(R)5214 | > 250 | 170 | 165 | > 20 |
| M14(R)701 | > 250 | 51 | 158 | > 20 |
| Hb1119 | 104 | 14 | 125 | > 20 |
| Hb(R)5214 | > 250 | 85 | 226 | > 20 |
| Hb(R)701 | 147 | 88 | 199 | > 20 |
Prolonged exposure to CEP-5214 or CEP-701 selects for cell lines that are cross-resistant to CEP-5214, CEP-701, PKC412 and AG1295. Cellular activity/proliferation, as indicated by the IC50, was determined using the MTT assay in triplicates. Cells (300 000 cells/mL) were incubated with 0 to 250 nM CEP-5214, CEP-701, or PKC412, or 0 to 20 μM AG1295 for 48 hours at 37°C. IC50 values were calculated using CalcuSyn software (Cambridge, United Kingdom) and had correlation coefficients > 0.95. The results are representative of 3 independent studies.