TAS-119 (TAS119) is a potent, selective, orally active inhibitor of Aurora A with IC50 of 1 nM.
TAS-119 displayed high target selectivity among 301 protein kinases, including Aurora B (IC50=95 nM) and Aurora C (IC50=35 nM).
TAS-119 dose dependently enhanced cell growth inhibition by paclitaxel, docetaxel, and cabazitaxel, also potentiated another microtubule stabilizer Epothilone B.
TAS-119 enhanced the antiproliferative effect of paclitaxel in different cell lines, including paclitaxel-resistant cells.
TAS-119 did neither induce mitosis and nor enhance the antiproliferative effect of paclitaxel in normal lung fibroblast cells.
TAS-119 enhanced the antitumor efficacy of paclitaxel and docetaxel in a nude mice NCI-H460 xenograft model, did not exaggerate paclitaxel-induced neutropenia and neurotoxicity.
