Table 3.
Cellular inhibitory potencies of the Aurora inhibitor panel.
| Aurora kinase inhibitor | Cell line | Assay |
|||
|---|---|---|---|---|---|
| Substrate-phosphorylation | G2/M | Cytokinesis | |||
| pLATS2 (Ser83) | pHistone H3 (Ser28) | ||||
| IC50 (nM) | IC50 (nM) | IC50 (nM) | IC50 (nM) | ||
| VX-680 | HeLa | 150 | 45 | nd | nd |
| RPE1 | nd | nd | nd | nd | |
| U2OS | nd | nd | nd | nd | |
| MK-5108 | HeLa | 610 | NE@9 μM | 816 | nd |
| RPE1 | 1800 | 80% Inh @15 μM | 877 | nd | |
| U2OS | 1200 | 20% Inh @15 µM | 995 | nd | |
| MK-8745 | HeLa | 610 | NE@9 µM | 596 | nd |
| RPE1 | 2300 | NE@15 µM | 755 | nd | |
| U2OS | 1700 | NE@15 µM | 437 | nd | |
| MLN8054 | HeLa | 290 | 2900 | 736 | nd |
| RPE1 | 720 | 880 | 500 | nd | |
| U2OS | 800 | 3300 | 957 | nd | |
| MLN8237 | HeLa | 37 | 160 | 128 | nd |
| RPE1 | 130 | 130 | 115 | nd | |
| U2OS | 92 | 210 | 157 | nd | |
| Genentech Aurora Inhibitor 1 | HeLa | 490 | NE@9 μM | nd | nd |
| RPE1 | nd | nd | nd | nd | |
| U2OS | nd | nd | nd | nd | |
| ZM447439 | HeLa | NE@3 μM | 419 | nd | 615 |
| RPE1 | nd | nd | nd | 1315 | |
| U2OS | nd | nd | nd | 613 | |
| AZD1152-HQPA | HeLa | NE@100 nM | 5 | nd | 4 |
| RPE1 | NE@200 nM | 25 | nd | 23 | |
| U2OS | NE@200 nM | 12 | nd | 20 | |
| Hesperadin | HeLa | NE@100 nM | 14 | nd | 14 |
| RPE1 | nd | nd | nd | 47 | |
| U2OS | nd | nd | nd | 17 | |
| GSK1070916 | HeLa | NE@100 nM | 6 | nd | 6 |
| RPE1 | NE@200 nM | 15 | nd | 21 | |
| U2OS | NE@200 nM | 8 | nd | 6 | |
NE, no effect; nd, not determined.