Table 12.
SAR of the literature PDGFR inhibitors in KIT-mutant Ba/F3 cell lines and their effect on KDR.
| Compd. | Structure | Ba/F3 GI50 (μM) | ||||
|---|---|---|---|---|---|---|
| Parental | Exon 11 Del + V654A | Exon 11 Del + D816H | Exon 11 Del + T670I | KDR | ||
| AZD2932 |
|
>10 | 0.012 | 0.070 | 0.004 | 0.093 |
| I-a |
|
4.289 | 0.685 | 0.786 | 1.918 | 2.674 |
| I-b |
|
>10 | 0.337 | 2.592 | 0.078 | 3.595 |
| I-c |
|
>10 | 0.008 | 0.026 | 0.012 | 0.442 |
| I-d |
|
>10 | 0.021 | 0.176 | 0.060 | 8.030 |
| I-e |
|
>10 | 0.013 | 0.027 | 0.061 | 3.924 |
| I-f |
|
>10 | 0.006 | 0.008 | 0.007 | 0.077 |
| II |
|
>10 | 0.044 | 0.488 | 0.007 | 0.680 |
| II-a |
|
>10 | 0.021 | 0.250 | 0.141 | 1.615 |
| II-b |
|
>10 | 0.078 | 0.251 | 0.086 | 2.551 |
| III |
|
>10 | 0.026 | 0.047 | 0.007 | 0.082 |
| III-a |
|
>10 | 0.150 | 0.518 | 0.008 | 0.761 |
| IV |
|
>10 | 0.003 | 0.019 | 0.017 | 0.612 |
| V |
|
>10 | 0.007 | 0.050 | 0.055 | 1.222 |
| V-a |
|
>10 | 0.003 | 0.048 | 0.107 | 5.408 |
| V-b |
|
>10 | 0.002 | 0.025 | 0.068 | >10 |
| 75 |
|
>10 | 0.003 | 0.009 | 0.016 | 1.378 |