Article
Antitumor activity of the ERK inhibitor SCH772984 [corrected] against BRAF mutant, NRAS mutant and wild-type melanoma.
Molecular cancer - 20 Aug 2014
Wong Deborah J L, Robert Lidia, Atefi Mohammad S, Lassen Amanda, Avarappatt Geetha, Cerniglia Michael, Avramis Earl, Tsoi Jennifer, Foulad David, Graeber Thomas G, Comin-Anduix Begonya, Samatar Ahmed, Lo Roger S, Ribas Antoni
Abstract excerpt
BACKGROUND: In melanoma, dysregulation of the MAPK pathway, usually via BRAF(V600) or NRAS(Q61) somatic mutations, leads to constitutive ERK signaling. While BRAF inhibitors are initially effective for BRAF-mutant melanoma, no FDA-approved targeted therapies exist for BRAF-inhibitor-resistant BRAF(V600), NRAS mutant, or wild-type melanoma. METHODS: The 50% inhibitory concentration (IC50) of SCH772984, a novel...
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