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Discovery of RAF 265: A Potent mut-B-RAF Inhibitor for the Treatment of Metastatic Melanoma

Poon, Daniel and Williams, Teresa and Subramanian, Sharadha and Verhagen, Joelle and McBride, Christopher M. and Costales, Abran and Sung, Leonard and Antonios-McCrea, William and McKenna, Maureen and Louie, Alicia K. and Ramurthy, Savithri and Levine, Barry and Shafer, Cynthia and Machajewski, Timothy and Renhowe, Paul A. and Appleton, Brent A. and Amiri, Payman and Chou, James and Stuart, Darrin and Aardalen, Kimberly (2015) Discovery of RAF 265: A Potent mut-B-RAF Inhibitor for the Treatment of Metastatic Melanoma. ACS Medicinal Chemistry Letters.

Abstract

Abrogation of errant signaling along the MAPK pathway through the inhibition of B-RAF kinase is a validated approach for the treatment of pathway dependent cancers. We report the development of imidazo-benzimidazoles as potent B-RAF inhibitors. Robust in vivo efficacy coupled with correlating PKPD and PD-efficacy relationships led to the identification of RAF265, 1, which has advanced into clinical trials.

Item Type: Article
Keywords: RAF, VEGF, serine-threonine kinases, tyrosine kinases, MAPK
Date Deposited: 09 May 2016 23:45
Last Modified: 09 May 2016 23:45
URI: https://oak.novartis.com/id/eprint/24218

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