2. Academic Validation
  3. Potent and selective pyrazole-based inhibitors of B-Raf kinase

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

Affiliation

  • 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.

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Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-50864
    99.69%, B-Raf Inhibitor
    Raf