简介内容:GNE-8525 is a potent and selective pan-TRK inhibitor. GNE-8525 demonstrated potent antiproliferation activity with IC50 = μM. In a tumor xenograft model derived from the KM12 cell line, GNE-8525 demonstrated in vivo antitumor efficacy when administered at ascending doses twice daily (bid) for 14 days in rats. Deregulated kinase activities of tropomyosin receptor kinase (TRK) family members have been shown to be associated with tumorigenesis and poor prognosis in a variety of cancer type