1352608-82-2

1352608-82-2 structure

Name: Vactosertib (TEW-7197)
Chemical Name: 1H-Imidazole-2-methanamine, N-(2-fluorophenyl)-5-(6-methyl-2-pyridinyl)-4-[1,2,4]triazolo[1,5-a]pyridin-6-yl
CAS Number: 1352608-82-2
Molecular Formula: C₂₂H₁₈FN₇
Molecular Weight: 399.424
Catalog: Biochemical Inhibitor TGF-beta/Smad signaling pathway inhibitor (TGF-beta/Smad) TGF-beta/Smad inhibitor
Create Date: 2018-12-09 14:07:56
Modify Date: 2024-01-11 18:21:42
Vactosertib (EW-7197) is an ATP-competitive inhibitor of ALK5 with an IC50 of 12.9 nM. It also inhibits ALK2 and ALK4 at nanomolar concentrations.

Name	1H-Imidazole-2-methanamine, N-(2-fluorophenyl)-5-(6-methyl-2-pyridinyl)-4-[1,2,4]triazolo[1,5-a]pyridin-6-yl
Synonyms	2-Fluoro-N-{[4-(6-methyl-2-pyridinyl)-5-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-1H-imidazol-2-yl]methyl}aniline 1H-Imidazole-2-methanamine, N-(2-fluorophenyl)-5-(6-methyl-2-pyridinyl)-4-[1,2,4]triazolo[1,5-a]pyridin-6-yl- EW-7197 N-[[4-([1,2,4]Triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl]methyl]-2-fluoroaniline TEW-7197

Description	Vactosertib (EW-7197) is an ATP-competitive inhibitor of ALK5 with an IC50 of 12.9 nM. It also inhibits ALK2 and ALK4 at nanomolar concentrations.
Related Catalog	Signaling Pathways >> TGF-beta/Smad >> TGF-β Receptor Research Areas >> Cancer
Target	IC50: 12.9 nM (TRPV4)[1]
References	[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.