Table 2.
Affinity and cytotoxicity of the different microtubule targeting agents
| MTAs | Ka (M−1) (K1K2 values (M−2)) | IC50 (nM) | IC50/K d |
|---|---|---|---|
| Paclitaxel | 1.07 × 107 | 1.4 ± 0.2a | 0.01498 |
| Docetaxel | 3.09 × 107 | 3.0 ± 0.3a | 0.0927 |
| Epothilone A | 3 × 107 | 7.5 ± 1.4a | 0.225 |
| Epothilone B | 60 × 107 | 0.8 ± 0.1a | 4.8 |
| Discodermolide | 526 × 107 | 6.6 ± 0.8a | 34.716 |
| Peloruside A | ND | 16 ± 2b | ND |
| Laulimalide | ND | 3.9 ± 0.4c | ND |
| Vinorelbine | 1.3 × 105 ± 0.2 (1.4 × 1011) | 28d | 0.00364 |
| Vinflunine | 8.8 × 104 ± 2.0 (2.6 × 1010) | 97d | 0.008536 |
| Vincristine | 1.4 × 105 ± 0.4 (2.4 × 1012) | 16d | 0.00224 |
| Vinblastine | 1.2 × 105 ± 0.2 (6.1 × 1011) | 16d | 0.00192 |
| Colchicine | 3.2 × 106 | 16.86 ± 0.63e | 0.053952 |
| Cyclostreptin | ND | 37 ± 8a | ND |