Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 4, Issue 3, Pages 358-362Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ml4000063
Keywords
B-Raf; GSK2118436; dabrafenib; melanoma; MAP kinase
Categories
Funding
- Cancer Research UK [11566] Funding Source: Medline
- Cancer Research UK [11566] Funding Source: researchfish
Ask authors/readers for more resources
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. GSK2118436 was identified as a development candidate, and early clinical results have shown significant activity in patients with B-Raf mutant melanoma.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available