|Product Name||EW-7197||CAS No.||1352608-82-2|
|Molecular Weight||399.42||Molecular Formula||C22H18FN7|
EW-7197 is a highly potent, selective, and orally bioavailable TGF-β receptor ALK4/ALK5 inhibitor with IC50 of 13 nM and 11 nM, respectively. target: ALK4/ALK5 IC 50: 13 nM for TGF-β receptor ALK4, 11 nM for TGF-β receptor ALK5. In vitro: EW-7197 inhibits TGFβ-induced Smad2 or Smad3 phosphorylation and the epithelial-to-mesenchymal transition (EMT) in TGFβ-treated breast cancer cells. In addition, EW-7197 also abrogates TGFβ1-induced tumor cell migration and invasion in breast cells. EW-7197 inhibited Smad/TGFβ signaling, cell migration, invasion, and lung metastasis in mouse mammary tumor virus. In vivo: EW-7197 inhibition downregulates Smad4 in melanoma-bearing mice. EW-7197 induces ubiquitin-mediated degradation of Smad4 in melanoma-bearing mice. In a mouse B16 melanoma model, EW-7197 (2.5 mg/kg daily p.o.) suppresses the progression of melanoma with enhanced cytotoxic T-lymphocyte (CTL) responses. EW-7197 dissolved in artificial gastric fluid formulation (vehicle; ddH2O 900 ml, conc. HCl 7 ml, NaCl 2.0 g, pepsin 3.2 g) was given orally by feeding needle to mice from 4 days after inoculation.