WebFeb 3, 2024 · TEPMETKO is an oral MET inhibitor that inhibits the oncogenic MET receptor signaling caused by MET (gene) alterations. Discovered and developed in-house at Merck KGaA, Darmstadt, Germany, TEPMETKO has a highly selective mechanism of action, with the potential to improve outcomes in aggressive tumors that have a poor prognosis and … WebNPS-1034 New. NPS-1034 is a dual Met (c-Met)/Axl inhibitor with IC50 of 48 nM and 10.3 nM, respectively.. Erlotinib (OSI-774) New Erlotinib (OSI-774, CP358774, NSC 718781, …

Type II c-Met inhibitors: molecular insight into crucial …

WebApr 5, 2024 · Meanwhile, high c-Met expression is closely associated with poor prognosis in cancer patients. Thus, it is extremely important to understand the role of c-Met in cancer. Tivantinib is a selective and orally active c-MET inhibitor. Tivantinib, formerly known as ARQ 197, is a selective, orally active, and non-ATP competitive inhibitor of c-MET. WebBhardwaj V, et al. C-Met inhibitor MK-8003 radiosensitizes c-Met-expressing non-small-cell lung cancer cells with radiation-induced c-Met-expression. J Thorac Oncol. 2012 … brazilian google

The role of MET in chemotherapy resistance Oncogene - Nature

WebCrizotinib (PF-02341066) is a potent inhibitor of c-Met and ALK with IC50 of 11 nM and 24 nM in cell-based assays, respectively. It is also a potent ROS1 inhibitor with Ki value less than 0.025 nM. Crizotinib induces autophagy through inhibition of the STAT3 pathway in multiple lung cancer cell lines. Foretinib (GSK1363089) WebSep 30, 2014 · C-MET inhibitors can be classified into three groups: small-molecule tyrosine kinase inhibitors of the c-MET receptor (crizotinib, tivantinib, cabozantinib, … c-Met inhibitors are a class of small molecules that inhibit the enzymatic activity of the c-Met tyrosine kinase, the receptor of hepatocyte growth factor/scatter factor (HGF/SF). These inhibitors may have therapeutic application in the treatment of various types of cancers. Many c-Met inhibitors are currently in … See more Early in the 1980s MET was described as the protein product of a transforming oncogene. Initial attempts to identify ATP-competitive c-Met inhibitors in 2002 led to the discovery of See more The c-Met RTK subfamily is different in structure to many other RTK families: The mature form has an extracellular α-chain (50kDa) and a … See more Even though the two classes are structurally different, they do share some properties: They both bind at the kinase hinge region (although they occupy different parts of … See more Status as of 2010 Since the discovery of Met and HGF, much research interest has focused on their roles in cancer. The Met pathway is one of the most … See more Receptor tyrosine kinases (RTKs) are a vital element in regulating many intracellular signal transduction pathways. Met tyrosine kinase is the receptor for hepatocyte growth factor (HGF), also known as scatter factor (SF). HGF is mostly expressed on See more Using information from the co-crystal structure of PHA-66752 and c-Met, the selective inhibitor PF-2341066 was designed. It was undergoing Phase I/II clinical trials in … See more Tivantinib Tivantinib (ARQ197) is a selective, orally bioavailable, clinically advanced low-molecular weight and well-tolerated c-MET inhibitor, which is currently in Phase III clinical trials in non-small cell lung cancer patients. ARQ197 … See more brazilian google translate