Table 23.
Compd. | GI50 (µM) a | Entry | GI50 (µM) a | ||
---|---|---|---|---|---|
GIST-T1 | HMC1.2 | GIST-T1 | HMC1.2 | ||
imatinib | 0.02 ± 0.01 | 27.10 ± 3.36 | 142p | 0.66 ± 0.10 | 8.55 ± 2.40 |
sunitinib | 0.01 ± 0.00 | 2.53 ± 0.35 | 142q | 0.42 ± 0.07 | 15.53 ± 3.97 |
142a | >50 | Inactive b | 142r | 0.01 ± 0.00 | 1.15 ± 0.96 |
142b | 33.05 ± 7.09 | Inactive b | 142s | 0.02 ± 0.00 | 1.33 ± 0.43 |
142c | 33.69 ± 3.45 | Inactive b | 142t | 0.12 ± 0.03 | 6.62 ± 0.75 |
142d | 16.36 ± 2.73 | 25.18 ± 2.21 | 142u | 0.66 ± 0.08 | 11.31 ± 0.34 |
142e | 3.45 ± 0.41 | 11.53 ± 0.62 | 142v | 0.05 ± 0.01 | 6.81 ± 0.67 |
142f | 20.94 ± 2.00 | Inactive b | 142w | 0.02 ± 0.01 | 4.99 ± 0.43 |
142g | 10.84 ± 1.06 | 36.77 ± 10.9 | 143a | 0.08 ± 0.01 | 4.58 ± 0.32 |
142h | 0.96 ± 0.10 | 7.26 ± 4.13 | 143b | 0.10 ± 0.01 | 5.22 ± 0.59 |
142i | 7.16 ± 0.87 | 9.65 ± 1.06 | 143c | 0.01 ± 0.00 | 1.52 ± 0.43 |
142j | 3.31 ± 0.73 | 6.35 ± 0.32 | 143d | 8.13 ±1.81 | Inactive b |
142k | 0.18 ± 0.03 | 2.27 ± 0.84 | 143e | 0.23 ± 0.07 | 14.04 ± 10.2 |
142l | 0.08 ± 0.01 | 4.34 ± 1.31 | 143f | 0.30 ± 0.06 | 28.39 ± 13.3 |
142m | 0.27 ± 0.17 | 3.41 ± 1.49 | 143g | 0.07 ± 0.01 | 4.88 ± 1.18 |
142n | 0.55 ± 0.09 | 7.00 ± 2.68 | 143h | 0.02 ± 0.00 | 4.98 ± 0.32 |
142o | 0.28 ± 0.08 | 2.36 ± 0.58 |
a Radiometric biochemical kinase assay results. b less than 50% inhibition at a concentration of 10 µM.