Table 1.
Biochemical inhibition constants of the Aurora inhibitor panel.
| Aurora A | Aurora A-TPX21–43 | Aurora B-INCENP783–918 | |
|---|---|---|---|
|
Ki Mean ± SD (nM) |
Ki Mean ± SD (nM) |
Ki Mean ± SD (nM) |
|
| VX-680 | 1.03 ± 0.18 (n=11) | 4.55 ± 0.57 (n=9) | 1.11 ± 0.20 (n = 9) |
| MK-5108 | <0.01a (n = 4) | 0.04 ± 0.008 (n = 3) | 1.49 ± 0.21 (n = 3) |
| MK-8745 | 0.06 ± 0.004 (n =4) | 0.41 ± 0.06 (n =3) | 66.8 ± 19.6 (n =3) |
| MLN8054 | 0.15 ± 0.01 (n =4) | 0.80 ± 0.09 (n = 3) | 1.65 ± 0.36 (n = 3) |
| MLN8237 | 0.04 ± 0.007 (n =3) | 0.23 ± 0.02 (n = 3) | 1.10 ± 0.23 (n = 3) |
| Genentech Aurora Inhibitor 1 | 0.57 ± 0.06 (n = 3) | 0.24 ± 0.02 (n = 3) | 156.2 ± 33.7 (n = 3) |
| ZM447439 | 55.5 ± 8.2 (n = 4) | 336.8 ± 50.5 (n = 3) | 1.83 ± 0.28 (n = 3) |
| AZD1152-HQPA | 83.8 ± 14.2 (n = 4) | 351.9 ± 64.1 (n=3) | 0.02 ± 0.009 (n = 3) |
| Hesperadin | 1.21 ± 0.14 (n = 3) | 1.37 ± 0.12 (n = 3) | 0.03 ± 0.014 (n = 3) |
| GSK1070916 | 16.1 ± 1.3 (n =3) | 130.2 ± 33.2 (n =3); 490b | 0.38b |
aUpper bound.
bValues from Ref. (61).