Napabucasin (BBI608) is an orally available Stat3 and Y cell stemness inhibitor.

Napabucasin 通过 Stat3 降调干细胞性基因表达及癌干细胞特性，并高效抑制高干细胞性癌细胞的自我更新，IC50 范围为 0.291~1.19 μM，对正常干细胞的抑制作用。[1]

在携带PaCa-2异种移植瘤的小鼠中，Napabucasin（20 mg/kg，i.p.）显著抑制了肿瘤生长、复发和转移。[1]

For cancer stem cells, spheres are dissociated and plated under cancer stem cell culture conditions on coated 96-well plates. After 72 h of culture, wells are dosed with the indicated compounds. Seventy-two hours or 24 h after dosing, CellTiter-Glo 2.0 is added to each well, and the luminescence is measured as described by the manufacturer. IC50 values are calculated by fitting a four parameter dose–response curve to normalized data using GraphPad Prism software. For bulk cells, cells are plated at 5,000 cells per well on 96-well plates. Twenty-four hours after plating, cells are treated with the indicated compounds. Viability is determined at 72 h as described above.(Only for Reference)