Title : Discovery of a novel ERK inhibitor with activity in models of acquired resistance to BRAF and MEK inhibitors.

Pub. Date : 2013 Jul

PMID : 23614898






2 Functional Relationships(s)
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1 Here, we describe the identification and characterization of SCH772984, a novel and selective inhibitor of ERK1/2 that displays behaviors of both type I and type II kinase inhibitors. SCH772984 mitogen-activated protein kinase 3 Homo sapiens
2 Importantly, SCH772984 effectively inhibited MAPK signaling and cell proliferation in BRAF or MEK inhibitor-resistant models as well as in tumor cells resistant to concurrent treatment with BRAF and MEK inhibitors. SCH772984 mitogen-activated protein kinase 3 Homo sapiens