TAS-119

TAS-119 is an orally available, highly selective small molecule inhibitor of Aurora kinase A (Aurora A), with additional inhibitory activity against tropomyosin receptor kinases TRKA, TRKB, and TRKC. It demonstrates potent inhibition of Aurora A (IC50 ~1 nM) and selectivity over Aurora B (IC50 ~95 nM). Preclinical studies show that TAS-119 induces mitotic arrest and apoptosis in cancer cells with MYC amplification or CTNNB1 mutation and inhibits tumor growth in xenograft models. It also degrades N-MYC protein in MYCN-amplified neuroblastoma cell lines and inhibits the activity of NTRK fusion proteins. In clinical trials for advanced solid tumors—including small-cell lung cancer, breast cancer, MYC-amplified/β-catenin-mutated tumors—TAS-119 showed a favorable safety profile distinct from other Aurora A inhibitors but limited single-agent anti-tumor activity. Combination studies with taxanes have shown enhanced antitumor efficacy without increased toxicity[1][3][7][10].

Other names

1453099-83-6UNII-6A57J83J27UNII6A57J83J27UNII 6A57J83J276A57J83J27