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Indibulin is a microtubule destabilizer that blocks tubulin polymerization (IC50 = 0.3 μM). It acts by blocking cell cycle progression at metaphase and displays antitumor activity against a variety of malignancies in vitro (IC50 values ranging from 0.036-0.285 μM). Has been shown to induce complete tumor remission in the Yoshida AH13 rat sarcoma model in vivo. It is not neurotoxic due to an ability to discriminate between posttranslationally modified tubulin in mature neuronal microtubules and less-modified tubulin present in immature neuronal or nonneuronal microtubules. Also, Indibulin displays oral availability and efficacy towards MDR tumor cells.
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