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CH-II-77 is a potent, small-molecule tubulin inhibitor that binds to the colchicine-binding site. Developed by researchers at the University of Tennessee Health Science Center, it is a pyridine analog derived from the lead compound ABI-274. CH-II-77 exhibits high antiproliferative activity with IC50 values in the low nanomolar range (1-3 nM) against various cancer cell lines, including those resistant to paclitaxel. Its mechanism involves inducing G2/M phase cell cycle arrest and apoptosis. In preclinical studies, CH-II-77 has demonstrated significant tumor growth inhibition in melanoma and triple-negative breast cancer (TNBC) xenograft models, suggesting potential for treating taxane-resistant cancers.
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