Table 1.
Inhibitors identified in the kinase inhibitor screen
| Inhibitor | Inhibitory Effect ± SD (%) | Target(s) | ||
|---|---|---|---|---|
| T47D | 182R-1 | 182R-2 | ||
| Barasertib | 28.2 ± 1.7 | 58.9 ± 2.2 | 59.9 ± 2.1 | Aurora B |
| PHA-680632 | 23.5 ± 7.4 | 62.8 ± 2.7 | 56.1 ± 5.0 | Aurora A/B/C |
| SNS-314 Mesylate | 19.4 ± 1.5 | 47.0 ± 2.6 | 52.8 ± 5.1 | Aurora A/B/C |
| ZM-447439 | 24.2 ± 6.1 | 57.7 ± 1.8 | 65.6 ± 1.5 | Aurora A/B/C |
| CCT129202 | 20.1 ± 13.2 | 44.5 ± 4.8 | 48.8 ± 4.3 | Aurora A/B/C |
| AMG 900 | 25.3 ± 3.0 | 55.8 ± 4.5 | 55.5 ± 0.6 | Aurora A/B/C |
| JNJ-7706621 | 1.7 ± 5.7 | 27.5 ± 4.9 | 33.4 ± 4.8 | Aurora A/B, cyclin A/CDK2, cyclin E/CDK2, cyclin B/CDK1 |
| AT9283 | 6.2 ± 3.6 | 46.4 ± 2.5 | 52.6 ± 2.1 | Aurora A/B, JAK2/3 and Abl |
| ENMD-2076 | 24.3 ± 16.5 | 61.8 ± 2.8 | 65.7 ± 1.5 | Aurora A/B, Flt3/4, SFKs and VEGFR2 |
| AZD7762 | 8.6 ± 10.3 | 30.3 ± 1.1 | 33.8 ± 2.8 | Chk1/2 |
| CX-4945 | 8.2 ± 2.1 | 27.9 ± 1.7 | 21.8 ± 1.7 | CK2 |
| PF-562271 | 1.4 ± 4.5 | 19.0 ± 3.5 | 14.8 ± 2.5 | FAK and Pyk2 |
| Nintedanib | 11.8 ± 3.0 | 42.2 ± 3.5 | 33.9 ± 6.2 | FGFR, VEGFR, PDGRF and SFKs |
| Dasatinib | 18.0 ± 3.5 | 47.1 ± 2.7 | 37.0 ± 3.4 | SFKs, Abl and c-Kit |
| TG100-115 | 5.0 ± 1.5 | 12.9 ± 2.3 | 13.2 ± 5.3 | PI3Kγ/δ |
The growth inhibitory effect of the kinase inhibitors compared with untreated cells ± standard deviation (SD). Abbreviations: Abelson (Abl), Casein kinase (CK), checkpoint kinase (Chk), cyclin-dependent kinases (CDK), fibroblast growth factor receptor (FGFR), Fms-like Tyrosine Kinase (Flt), focal adhesion kinase (FAK), janus kinase (JAK), platelet-derived growth factor receptor (PDGFR), proline-rich tyrosine kinase (Pyk), Src Family kinases (SFKs), vascular endothelial growth factor receptor (VEGFR), and phosphoinositide 3-kinase (PI3K).