Table 1.
Protein kinase profiling
| Protein kinase |
SPH3643 IC50 (nmol/L) |
LY2835219 IC50 (nmol/L) |
Palbociclib IC50 (nmol/L) |
|---|---|---|---|
| CDK4 | 2.2 | 2.6 | 3.7 |
| CDK6 | 8.3 | 23 | 12 |
| CDK9 | 171 | 52 | 1380 |
| CDK5 | 311.25 | 229 | >3333 |
| CDK2 | 350 | 74 | 8773 |
| CDK1 | 812 | 436 | >10 000 |
| CDK3 | 838.26 | 482.2 | >3333 |
| CDK7 | 862 | 1876 | >10 000 |
| PKCa | 73 | — | — |
| FLT3 | 75 | — | — |
| GSK3β | 88 | — | — |
| JNK3 | 378 | — | — |
| P70S6K | 614 | — | — |
| JNK2 | 832 | — | — |
| TRK‐A | 891 | — | — |
| CHK1 | 1707 | — | — |
| PDGFRb | 1948 | — | — |
| AMPKa1 | 2100 | — | — |
| FLT4 | 2776 | — | — |
| CHK2 | 5666 | — | — |
| AURA | 5754 | — | — |
| AURB | 6974 | — | — |
| FLT1 | 8265 | — | — |
| EGFR | 8315 | — | — |
| KDR | 9518 | — | — |
| PDGFRa | >10 000 | — | — |
| AKT1 | >10 000 | — | — |
| ERK1 | >10 000 | — | — |
| MAPKAPK2 | >10 000 | — | — |
| BRAF | >10 000 | — | — |
| CRAF | >10 000 | — | — |
| FGFR1 | >10 000 | — | — |
IC50 values were calculated by nonlinear regression analysis of dose‐response curves.
—, not present; AUR, Aurora; AMPK, Adenosine 5‘‐monophosphate‐activated protein kinase; CDK, cyclin‐dependent kinase; CHK, checkpoint kinase; EGFR, epidermal growth factor receptor; ERK, extracellular regulated protein kinases; FGFR, fibroblast growth factor receptor; FLT, fms‐related tyrosine kinase; GSK3β, glycogen synthase kinase 3β; JNK, c‐Jun N‐terminal kinase; KDR, kinase insert domain receptor; PDGFR, platelet‐derived growth factor receptor; MAPKAPK, mitogen‐activated protein kinase–activated protein kinase; p70S6K, p70 Ribosomal protein S6 kinase; PKC, protein kinase C; TRK‐A, tyrosine kinase receptor A.