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CAS:700874-71-1 LY2109761

NAME:LY2109761 CAS:700874-71-1 MF:C26H27N5O2 MW:441.52 PURITY:98%

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Material Chemistry

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Product introduction

NAME	LY2109761
CAS	700874-71-1
MF	C26H27N5O2
MW	441.52
DENSITY	1.34
BP	640.9±55.0 °C
STORAGE	Store at -20°C

Description
LY2157299 is a small molecule inhibitor of the TGF-β receptor type 1/type II kinases (IC50 = 69 nM). It has been used to study the role of TGF-β signaling in tumor cell migration and metastasis in pancreatic tumor cell lines where 5 μM of the compound completely disrupts Smad-2 phosphorylation, an immediate downstream target of the kinase activity. It can also suppress radiation-induced inflammatory cytokine signaling and proangiogenic genes, including ID1, in human primary fibrobalsts.
LY2109761 is a novel transforming growth factor beta receptor type I and type II dual inhibitor. The effect of LY2109761 has been evaluated on soft agar growth, migration, invasion using a fibroblast coculture model, and detachment-induced apoptosis (anoikis) by Annexin V flow cytometric analysis. The efficacy of LY2109761 on tumor growth, survival, and reduction of spontaneous metastasis have been evaluated in an orthotopic murine model of metastatic pancreatic cancer expressing both luciferase and green fluorescence proteins (L3.6pl/GLT). In vivo, LY2109761, in combination with gemcitabine, significantly reduced the tumor burden, prolonged survival, and reduced spontaneous abdominal metastases.

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