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Pharmacological inhibitory kinase activity of regorafenib and its metabolites
| Gene symbol |
Kd, nmol/L |
||
|---|---|---|---|
| regorafenib* | M-2 | M-5 | |
| VEGFR-2 | 57/28 | 29 | 31 |
| PDGFRA | 21/19 | 7.3 | 11 |
| PDGFRB | 19/8.3 | 11 | 11 |
| KIT | 35/6.9 | 9.8 | 5.8 |
| RET | 7.7/5.2 | 7.6 | 5.8 |
| CSF1R | 43/10 | 21 | 13 |
| FLT3 | 9.6/4.8 | 6.7 | 2.6 |
| RAF1 | 87/59 | 130 | 66 |
| BRAF | 42/52 | 24 | 17 |
M-2, M-5: metabolites of regorafenib.
Duplicate Kd values are given.
