Ontology highlight
ABSTRACT:
SUBMITTER: Rheault TR
PROVIDER: S-EPMC4027516 | biostudies-literature | 2013 Mar
REPOSITORIES: biostudies-literature
ACS medicinal chemistry letters 20130207 3
Hyperactive signaling of the MAP kinase pathway resulting from the constitutively active B-Raf(V600E) mutated enzyme has been observed in a number of human tumors, including melanomas. Herein we report the discovery and biological evaluation of GSK2118436, a selective inhibitor of Raf kinases with potent in vitro activity in oncogenic B-Raf-driven melanoma and colorectal carcinoma cells and robust in vivo antitumor and pharmacodynamic activity in mouse models of B-Raf(V600E) human melanoma. GSK2 ...[more]