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LY3214996 is an inhibitor of ERK1 and ERK2 (IC50 = 5 nM for both).1 It inhibits cell proliferation of tumor cells in vitro, including those expressing B-RAF, N-Ras, or K-Ras mutations. LY3214996 inhibits tumor growth in B-RAF or N-Ras mutant melanoma, B-RAF or K-Ras mutant colorectal, lung, and pancreatic cancer mouse xenograft models, as well as patient-derived xenograft (PDX) mouse models.
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1. Abstract 4973: Discovery of LY3214996, a selective and novel ERK1/2 inhibitor with potent antitumor activities in cancer models with MAPK pathway alterations. Cancer Res. 77(Suppl. 13), (2017).