Description
As a novel inhibitor, LY2109761 can TGF-beta receptor type I and TGF-beta receptor II with Ki of 38 nM and 300 nM, respectively.
Storage
2 years at -20 centigrade
Targets
TGF-beta receptor I, TGF-beta receptor II
Molecular Formula
C26H27N5O2
Chemical Name
7-(2-morpholinoethoxy)-4-(2-(pyridin-2-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)quinoline
In vitro
LY2109761 treatment induces a dose-dependent low-anchorage growth inhibition of L3.6pl/GLT cells, leading to ~33% or 73% inhibition at 2 uM and 20 uM. And LY2109761 treatment at 1 nM is sufficient to significantly block the migration and invasion but not adhesion of hepatocellular carcinoma cells by increasing E-cadherin expression.
In vivo
Administration of LY2109761 (50 mg/kg) alone or in combination with gemcitabine (25 mg/kg) significantly reduces the tumor volume by ~70% and ~90%. In consistent with the in vitro effect, administration of LY2109761 alone or in combination with radiation, markedly inhibits tumor growth in the orthotopical CSLC glioblastoma model by 43.4% and 76.3%, respectively.
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