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Napabucasin (BBI608) is a first-in-class, orally active inhibitor of Stat3 and cancer cell pluripotency that increases ROS levels through the biological activation of NAD(P) H-quinone dehydrogen1 (NQO1). Napabucasin inhibits the expressions of stemness markers and kill stemness-high cancer cells isolated from several kinds of tumors except PCa. Napabucasin also effectively blocks sphere formation of PrCSCs and kill them as well as inhibits stemness gene expression. Napabucasin inhibits cell proliferation in PC-3 cells and 22RV1 cells at 48, 72, 96, and 120 h (P<0.05).
In vivo, Napabucasin (40 mg/kg) or Docetaxel significantly reduces xenograft tumor growth and tumor volume (TV) compared with PBS (P<0.05). Notably, while no differences are observed between the Napabucasin and the docetaxel groups in PC-3 mouse xenograft models, the TV in Napabucasin group is even lower than docetaxel group in 22RV1 mouse xenograft models (P<0.05).
| Molecular Weight | 240.21 |
| Formula | C14H8O4 |
| CAS Number | 83280-65-3 |
| Solubility (25°C) | DMSO 4 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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