Vactosertib (TEW-7197)

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.

Signaling Pathways >> TGF-beta/Smad >> TGF-β Receptor

Research Areas >> Cancer

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) | A 83-01 | LY2109761 | LDN193189 | RepSox | SB525334 | DMH-1 | GW788388 | LY364947 | SB505124 | LY3200882 | H-Leu-Ser-Lys-Leu-NH2 trifluoroacetate salt | ITD-1 | K 02288