Table 1.
Summary of biochemical IC50 values of CSF1R tyrosine kinase inhibitor in clinical development
|
Code
|
IC50
|
|||||
|
CSF1R, nM
|
KIT, nM
|
FLT3β, nM
|
PDGFRβ, nM
|
LCK
|
ABL
|
|
| ARRY382[24] | 9 | NA | NA | NA | NA | NA |
| BLZ945[25] | 1 | 3200 | 9100 | 4800 | > 10 μM | > 10 μM |
| DCC3014[28] | 3 | 1600 | NA | NA | 2800 nM | 2900 nM |
| JNJ40346527 (edicotinib)[29] | 3.2 | 20 | 190 | NA | NA | NA |
| PLX3397 (pexidartinib)[30] | 13 | 27 | 160 | NA | 860 nM | NA |
ABL: Abelson; CSF1R: colony-stimulating factor 1 receptor; FLT3: fms-like tyrosine kinase 3; IC50: half maximal inhibitory concentration; KIT: stem cell factor receptor; LCK: lymphocyte-specific protein tyrosine kinase; NA: not available; PDGFRβ: platelet-derived growth factor receptor β.