Cayman Ispinesib, 25 mg

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Ispinesib is a cell-permeable, allosteric inhibitor of Eg5 (K_i app = 2.3 nM) with >10,000-fold selectivity for Eg5 over a range of other mitotic kinesins.^1,2 It induces a monopolar spindle phenotype, leading to the activation of a spindle assembly checkpoint, mitotic arrest, and subsequent cell death (GI₅₀s = 22-82 nM in colon, pancreas, prostrate, and lung cancer cells in vitro).³ At 10 mg/kg, ispinesib produces tumor regression of breast cancer cell xenografts in mice.⁴ It has also been used to halt the growth of treatment-resistant glioblastoma tumor-initiating cells, to prevent tumor initiation and self-renewal of a cancer stem cell population (EC₅₀ = 1.15 nM), and to reduce glioma cell invasion.⁵

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