1196546-33-4
中文名稱
化合物 GNF-8625
英文名稱
GNE-8525
CAS
1196546-33-4
分子式
C31H30FN7O
分子量
535.61
MOL 文件
1196546-33-4.mol
更新日期
2024/11/29 09:19:09
1196546-33-4 結(jié)構(gòu)式
應(yīng)用領(lǐng)域
用途一
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.