Table 2. Specificity of kinase inhibition of BPR1J-097.
| Kinase | Percentage of inhibition | IC50b, nM |
|---|---|---|
| FLT3 | 96 | 11 |
| FLT3-D835Y | 99 | 3c |
| FLT1 (VEGFR1) | 59 | 211 |
| KDR (VEGFR2) | 91 | 129 |
| PDGFRA (PDGFR-α) | 80 | ND |
| TEK (Tie2) | 61 | ND |
| KIT | 49 | ND |
| AURKA (Aurora A) | 80 | 340 |
| AURKB (Aurora B) | 79 | 876 |
| AURKC (Aurora C) | 26 | ND |
| AMPK A1/B1/G1 | 82 | ND |
| SRC | 81 | ND |
Abbreviations: FLT3=Fms-like tyrosine kinase 3; ND=not determined; PDGFR=platelet-derived growth factor receptor; VEGFR=vascular endothelial growth factor receptor.
a
Inhibition of kinase at 1 μM, carried out by Invitrogen SelectScreen kinase profiling service.
b
IC50 determination was performed by kinase-Glo assay.
c
IC50 determination was performed by Invitrogen SelectScreen kinase assay.