Discovery of RAF265: A Potent mut-B-RAF Inhibitor for the Treatment of Metastatic Melanoma.
ACS Med Chem Lett
; 6(9): 961-5, 2015 Sep 10.
Article
em En
| MEDLINE
| ID: mdl-26396681
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 pharmacokinetic/pharmacodynamic (PKPD) and PD-efficacy relationships led to the identification of RAF265, 1, which has advanced into clinical trials.
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MEDLINE
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En
Ano de publicação:
2015
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Article