Potent and selective pyrazole-based inhibitors of B-Raf kinase

  • Bioorg Med Chem Lett. 2008 Aug 15;18(16):4692-5. doi: 10.1016/j.bmcl.2008.07.002.
Joshua D Hansen  1 ,  Jonas Grina ,  Brad Newhouse ,  Mike Welch ,  George Topalov ,  Nicole Littman ,  Michele Callejo ,  Susan Gloor ,  Matthew Martinson ,  Ellen Laird ,  Barbara J Brandhuber ,  Guy Vigers ,  Tony Morales ,  Rich Woessner ,  Nikole Randolph ,  Joseph Lyssikatos ,  Alan Olivero
Affiliations
  • 1. Lead Optimization, Array BioPharma, 3200 Walnut Street, Boulder, CO 80301, USA. [email protected]
PMID: 18676143 DOI: 10.1016/j.bmcl.2008.07.002
Abstract

Herein we describe a novel pyrazole-based class of ATP competitive B-Raf inhibitors. These inhibitors exhibit both excellent cellular potency and striking B-Raf selectivity. A subset of these inhibitors has demonstrated the ability to inhibit downstream ERK phosphorylation in LOX tumors from mouse xenograft studies.

Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-50864
    GDC-0879
    99.49%, B-Raf Inhibitor
    target: Raf
    Research Areas: Cancer