LY2109761

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.

The Uses of LY2109761

LY 2109761 is a novel transforming growth factor beta receptor type I and type II dual inhibitor that is potentially used to treat and suppress pancreatic cancer.

What are the applications of Application

LY2109761 is a small molecule inhibitor of the TGF-β receptor type 1/type II kinases

References

[1]melisi d, ishiyama s, sclabas gm et al. ly2109761, a novel transforming growth factor beta receptor type i and type ii dual inhibitor, as a therapeutic approach to suppressing pancreatic cancer metastasis. mol cancer ther 2008; 7: 829-840.
[2]li hy, mcmillen wt, heap cr et al. optimization of a dihydropyrrolopyrazole series of transforming growth factor-beta type i receptor kinase domain inhibitors: discovery of an orally bioavailable transforming growth factor-beta receptor type i inhibitor as antitumor agent. j med chem 2008; 51: 2302-2306.
[3]xu y, tabe y, jin l et al. tgf-beta receptor kinase inhibitor ly2109761 reverses the anti-apoptotic effects of tgf-beta1 in myelo-monocytic leukaemic cells co-cultured with stromal cells. br j haematol 2008; 142: 192-201.
[4]zhang m, kleber s, rohrich m et al. blockade of tgf-beta signaling by the tgfbetar-i kinase inhibitor ly2109761 enhances radiation response and prolongs survival in glioblastoma. cancer res 2011; 71: 7155-7167.
[5]flechsig p, dadrich m, bickelhaupt s et al. ly2109761 attenuates radiation-induced pulmonary murine fibrosis via reversal of tgf-beta and bmp-associated proinflammatory and proangiogenic signals. clin cancer res 2012; 18: 3616-3627.