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Cellagen Technology
cMET inhibitor
SU-11274 is an oxindole-based, ATP-competitive, Met inhibitor with activity of 20 nM and is >500-fold selective against a variety of other kinases such as PDGFR, EGFR, cdk2, src, and FGFR. [1] SU11274 induces G1 cell cycle arrest and apoptosis with increased caspase 3 activity. Reduction of phosphorylation in the PI3K and Ras pathway components, such as Akt, GSK-3, and FKHR. [1] SU11274 inhibits cell viability, c-Met/HGF and downstream cell proliferation in c-Met-expressing NSCLC cells. [2]
More recently, SU11274 has been extensively studied for the treatment of hepatocellular carcinoma (HCC). In particular, cells postiive for des-gamma-carboxyprothrombin (DCP), an agent that interacts with c-Met to activate HCC cell growth, were inhibited by SU11274. [3]
Cellagen Technology
cMET inhibitor
SU-11274 is an oxindole-based, ATP-competitive, Met inhibitor with activity of 20 nM and is >500-fold selective against a variety of other kinases such as PDGFR, EGFR, cdk2, src, and FGFR. [1] SU11274 induces G1 cell cycle arrest and apoptosis with increased caspase 3 activity. Reduction of phosphorylation in the PI3K and Ras pathway components, such as Akt, GSK-3, and FKHR. [1] SU11274 inhibits cell viability, c-Met/HGF and downstream cell proliferation in c-Met-expressing NSCLC cells. [2]
More recently, SU11274 has been extensively studied for the treatment of hepatocellular carcinoma (HCC). In particular, cells postiive for des-gamma-carboxyprothrombin (DCP), an agent that interacts with c-Met to activate HCC cell growth, were inhibited by SU11274. [3]
