1196546-33-4

GNE-8525 is a potent and selective pan-TRK inhibitor. GNE-8525 demonstrated potent antiproliferation activity with IC50 = 0.003 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 types. In particular, several chromosomal rearrangements involving TRKA have been reported in colorectal, papillary thyroid, glioblastoma, melanoma, and lung tissue that are believed to be the key oncogenic driver in these tumors.

GNF-8625 是一种广谱的 TRK 抑制剂，能够与 Thalidomide 结合形成 PROTAC 降解剂。GNF-8625 抑制 TRKA、TRKB、TRKC 的 IC50 分别为 0.8 nM、22 nM、5.4 nM。