LY2109761 is a potent, selective and orally active TGF-β RI/II dual inhibitor with Ki of 38/300 nM, respectively.
LY2109761 completely inhibits TGF-β-induced Sma2 phosphorylation on tumor cells or the liver microenviroment, inhibits the L3.6pl/GLT soft agar growth。
LY2109761 suppresses both basal and TGF-β1-induced cell migration and invasion, and stimulates anoikis in vitro。
LY2109761 significantly reduces the tumor burden as well as spontaneous abdominal metastases, and prolongs survival combined with gemicitabine in vivo model of pancreatic cancer.
