2-[4-[1-(喹啉-6-甲基)-1H-[1,2,3]三唑并[4,5-B]吡嗪-6-基]-1H-吡唑-1-基]乙醇

PF-04217903是ATP竞争性c-Met抑制剂,IC50为4.8 nM,对突变型Y1230C无活性。

信号通路 >> 蛋白酪氨酸激酶 >> c-Met的/HGFR

研究领域 >> 癌症

[1]. Timofeevski SL, et al. Enzymatic characterization of c-Met receptor tyrosine kinase oncogenic mutants and kinetic studies with aminopyridine and triazolopyrazine inhibitors. Biochemistry, 2009, 48(23), 5339-5349.

[2]. Shojaei F, et al. HGF/c-Met acts as an alternative angiogenic pathway in sunitinib-resistant tumors. Cancer Res, 2010, 70(24), 10090-10100.

[3]. Krumbach R, et al. Primary resistance to cetuximab in a panel of patient-derived tumour xenograft models: activation of MET as one mechanism for drug resistance. Eur J Cancer, 2011, 47(8), 1231-1243.

苯扎米特 | Foretinib | PHA-665752 | BMS 777607 | 益智二肽 | 沃利替尼 | (3R,4R)-3-(5,6-二氢-4H-吡咯并[3,2,1-IJ]喹啉-1-基)-4-(1H-吲哚-3-基)吡咯烷-2,5-二酮 | 特泊替尼 | 美乐替尼 | 6-[[6-(1-甲基-1H-吡唑-4-基)-1,2,4-噻唑并[4,3-b]吡嗪-3-基]硫代]喹啉 | N-[2,5-二氟-4-[[2-(1-甲基-1H-吡唑-4-基)-4-吡啶基]氧基]苯基]-N'-苯基-1,1-环丙烷二甲酰胺 | N-(3-氯苯基)-N-甲基-3-[[3,5-二甲基-4-[(4-甲基哌嗪-1-基)羰基-1H-吡咯-2-基]亚甲基]-2-氧代-2,3-二氢-1H-吲哚-5-磺酰胺 | 恩沙替尼(X-376) | CEP-40783 | 6-[二氟[6-(1-甲基-1H-吡唑-4-基)-1,2,4-三唑并[4,3-b]哒嗪-3-基]甲基]喹啉