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Epothilone A

CAS No. : 152044-53-6

MCE 站：Epothilone A

产品活性：Epothilone A 是紫杉醇和管蛋白 (tubulin) 聚合物结合的竞争性抑制剂，其 K_i 值为 0.6-1.4 μM。

研究领域：Cell Cycle/DNA Damage  |  Cytoskeleton  |  Apoptosis

作用靶点：Microtubule/Tubulin  |  Apoptosis

In Vitro: Epothilone A is a competitive inhibitor of the binding of [³H] paclitaxel to tubulin polymers. The apparent K_i value for Epothilone A is 1.4 μM by Hanes analysis and 0.6 μM by Dixon analysis. 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.

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