A Novel RAF Kinase Inhibitor with DFG-Out-Binding Mode: High Efficacy in BRAF-Mutant Tumor Xenograft Models in the Absence of Normal Tissue Hyperproliferation.

doi:10.1158/1535-7163.MCT-15-0617

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A Novel RAF Kinase Inhibitor with DFG-Out-Binding Mode: High Efficacy in BRAF-Mutant Tumor Xenograft Models in the Absence of Normal Tissue Hyperproliferation.

Molecular cancer therapeutics - 1 Mar 2016

Waizenegger Irene C, Baum Anke, Steurer Steffen, Stadtmüller Heinz, Bader Gerd, Schaaf Otmar, Garin-Chesa Pilar, Schlattl Andreas, Schweifer Norbert, Haslinger Christian, Colbatzky Florian, Mousa Sien, Kalkuhl Arno, Kraut Norbert, Adolf Günther R

Abstract excerpt

BI 882370 is a highly potent and selective RAF inhibitor that binds to the DFG-out (inactive) conformation of the BRAF kinase. The compound inhibited proliferation of human BRAF-mutant melanoma cells with 100× higher potency (1-10 nmol/L) than vemurafenib, whereas wild-type cells were not affected at 1,000 nmol/L. BI 882370 administered orally was efficacious in multiple mouse models of BRAF-mutant melanomas and...

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A Novel RAF Kinase Inhibitor with DFG-Out-Binding Mode: High Efficacy in BRAF-Mutant Tumor Xenograft Models in the Absence of Normal Tissue Hyperproliferation.

Abstract excerpt

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