Napabucasin (83280-65-3) inhibits gene transcription driven by STAT3. Inhibits cancer cell stemness gene expression and blocks spherogenesis of stemness-high cancer cells isolated from a variety of cancer types.¹ Effective antitumor agent as a monotherapy or in combination with other agents such as taxol in mouse models.² Clinical trials have demonstrated encouraging anti-tumor activity with the potential to suppress metastasis and prevent relapse in patients with various types of cancer.^2,3 Overcomes cisplatin resistance in non-small cell lung cancer.⁴

References/Citations

1) Li et al. (2015), Suppression of cancer relapse and metastasis by inhibiting cancer stemness; Proc. Natl. Acad. Sci. USA, 112 1839
2) Hubbard and Grothey (2017), Napabucasin: an Update on the First-in-Class Cancer Stemness Inhibitor; Drugs, 77 1091
3) Zhang et al. (2016), Suppression of prostate cancer progression by cancer cell stemness inhibitor napabucasin; Cancer Med., 5 1251
4) MacDonagh et al. (2018), BBI608 inhibits cancer stemness and reverses cisplatin resistance in NSCLC; Cancer Lett., 428 117