EW-7197

Vactosertib (EW-7197) 是 ALK5 的 ATP 竞争性抑制剂,IC50 为 12.9 nM。抑制 ALK2 和 ALK4 在纳摩尔级别。

信号通路 >> TGF-beta/Smad 信号通路 >> TGF-β受体

研究领域 >> 癌症

IC50: 12.9 nM (TRPV4)[1]

[1]. Jin CH et al. Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/antifibrotic agent. J Med Chem, 2014 May 22, 57(10):4213-38.

[2]. Son JY et al. EW-7197, a novel ALK-5 kinase inhibitor, potently inhibits breast to lung metastasis, 2014 Jul, 13(7):1704-16.

[3]. Yoon JH et al. Activin receptor-like kinase5 inhibition suppresses mouse melanoma by ubiquitin degradation of Smad4,thereby derepressing eomesodermin in cytotoxic T lymphocytes. EMBO Mol Med, 2013 Nov, 5(11):1720-39.

SB431542 | Galunisertib (LY2157299) | 3-(6-甲基-2-吡啶基)-N-苯基-4-(4-喹啉基)-1H-吡唑-1-硫代甲酰胺 | 4-[5,6-二氢-2-(2-吡啶)-4H-吡咯并[1,2-b]吡唑-3-基]-7-[2-(4-吗啉)乙氧基]喹啉 | LDN193189 | 2-(3-(6-甲基吡啶-2-基)-1H-吡唑-4-基)-1,5-萘啶 | SB525334 | 4-[6-[4-异丙氧基苯基]吡唑并[1,5-a]嘧啶-3-基]喹啉 | 4-[4-[3-(吡啶-2-基)-1H-吡唑-4-基]吡啶-2-基]-N-(四氢吡喃-4-基)苯甲酰胺 | LY-364947 | SB-505124 | LY3200882 | LSKL, 血小板反应蛋白抑制剂 (TSP-1) | 4-[1,1'-联苯]-4-基-1,4,5,6,7,8-六氢-2,7,7-三甲基-5-氧代-3-喹啉羧酸乙酯 | K02288