| Bioactivity | Epothilone A is a competitive inhibitor of the binding of [3H] paclitaxel to tubulin polymers, with a Ki of 0.6-1.4 μM. | |||||||||
| Invitro | Epothilone A is a competitive inhibitor of the binding of [3H] paclitaxel to tubulin polymers. The apparent Ki value for Epothilone A is 1.4 μM by Hanes analysis and 0.6 μM by Dixon analysis[1]. Epothilone A, is noted to be highly cytotoxic (IC50=0.05 μM) in vitro when applied to the human T-24 bladder carcinoma cell line. The binding affinity of Epothilone A to tubulin is of the same order of magnitude as the binding affinity of paclitaxel to tubulin based on competition assays. The IC50 for displacement of 100 nM of (3H) paclitaxel from the tubulin binding site is 3.6 μM for paclitaxel, 2.3 μM for Epothilone A, and 3.3 μM for patupilone[2]. | |||||||||
| Name | Epothilone A | |||||||||
| CAS | 152044-53-6 | |||||||||
| Formula | C26H39NO6S | |||||||||
| Molar Mass | 493.66 | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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