Article
The selective intravenous inhibitor of the MET tyrosine kinase SAR125844 inhibits tumor growth in MET-amplified cancer.
Molecular cancer therapeutics - 1 Feb 2015
Egile Coumaran, Kenigsberg Mireille, Delaisi Christine, Bégassat Françoise, Do-Vale Véronique, Mestadier Jessica, Bonche Fabrice, Bénard Tsiala, Nicolas Jean-Paul, Valence Sandrine, Lefranc Céline, Francesconi Elisa, Castell Christelle, Lefebvre Anne-Marie, Nemecek Conception, Calvet Loreley, Goulaouic Hélène
Abstract excerpt
Activation of the MET/HGF pathway is common in human cancer and is thought to promote tumor initiation, metastasis, angiogenesis, and resistance to diverse therapies. We report here the pharmacologic characterization of the triazolopyridazine derivative SAR125844, a potent and highly selective inhibitor of the MET receptor tyrosine kinase (RTK), for intravenous administration. SAR125844 displayed nanomolar...
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