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Biological Activity:

Napabucasin (BBI608) is a potent and selective STAT3 inhibitor. It can inhibit gene transcription driven by Stat3 and cancer stemness properties, can inhibit stemness gene expression and block spherogenesis of or kill stemness-high cancer cells isolated from a variety of cancer types (IC50 ~0.14-1.25 µM), but not hematopoietic stem cells. Napabucasin inhibits PaCa-2 xenograft tumor growth in mice, even after cessation of treatment, and decreases population of CSCs in PaCa-2 tumors from treated mice.

How to Use:

In vitro: Napabucasin (BBI608) was used at 0.5-2 µM final concentration in various assays.
In vivo: Napabucasin (BBI608) can be dosed to mice at 50 mg/Kg by IP injection once per day in xenograft models.

Reference:

• 1. Li Y, et al. Suppression of cancer relapse and metastasis by inhibiting cancer stemness. （2015）Proc Natl Acad Sci USA. 112(6):1839-44.