Compounds Were Evaluated

- Jan 30, 2019 -

In general, compounds were evaluated for their ability to inhibit recombinant BRAF V600E in a biochemical assay monitoring ADP formation via the coupled pyruvate kinase/lactate dehydrogenase system. Wild type BRAF, CRAF, and MEK biochemical assays were run with recombinant protein in a filter binding format. Cellular profiling consisted of monitoring the change in phospho-ERK in the BRAF V600E driven melanoma cell line A375 as well as antiproliferative activity in the same line upon compound treatment for 72 h. Further cellular profiling was performed in the KRAS G13D mutant (BRAF WT) cell line HCT116, again measuring both impact on phospho-ERK and proliferation upon compound treatment.

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