Tubulin Polymerization Inhibitor is a low molecular weight, cell-permeable, benzylidene-anthracenone antimicrotubule agent that exhibits potent antitumor activity (IC50 = 20 and 50 nM in inhibiting Tumor cell growth in K562 and SKOV3 cells, respectively) comparable to other commonly used antitumor agents. Unlike Paclitaxel , Vinblastine , or Vincristine , it does not function as a substrate for Pgp-170 and exhibits cytotoxic effects towards tumor cell lines with various MDR resistance phenotypes. It is shown to interact with Tubulin at the Colchicine, but not the Vinblastine, binding site.
1. Prinz, H., et al. 2003. J. Med. Chem. 46: 3382-3394. PMID: 19220018
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