CEP-11981(ESK981; BOL 303213X) is an orally active tyrosine kinase inhibitor (TKI), which can target TIE2, VEGFR1-3 and FGFR1, and has potential anti-tumor and anti-angiogenic effects.
CEP-11981(1μM, 72 h) can significantly inhibit the growth of RT4 cells[1].
CEP-11981(2.5 mg/kg, 5 mg/kg or 10 mg/kg, oral gavage, daily, five days a week for two weeks) significantly arrested the growth of UC xenografts compared to controlwith no change in weight in murine xenograft model of RT4 human UC tumor[1].
References:
[1]. Weiguo Jian, et al. The angiopoietin-TIE2 pathway is a potential therapeutic target in urothelial carcinoma. Anticancer Res. 2014 Jul;34(7):3377-82.