Supplementary Figures S1 - S6 from 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

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Supplementary Figure S1 - Structure of the BRAF kinase domain with BI 882370 and a bound glucose molecule Supplementary Figure S2 - Drug wash-out experiment prolonged phospho-ERK reduction in A375 melanoma cells treated with BI 882370 vs comparator compound. Supplementary Figure S3 - Pharmacokinetic analysis of BI 882370, dabrafenib and vemurafenib in nude mice bearing subcutaneous A375 melanoma tumors show higher concentration of BI 882370 in tumor than plasma. Supplementary Figure S4 - In vivo pharmacodynamic response shown by phospho-ERK reduction in A375 tumors in nude mice treated once with BI 882370. Supplementary Figure S5 - Efficacy of BI 882370 and vemurafenib in COLO 205 colorectal cancer xenograft model. Supplementary Figure S6 - Efficacy of BI 882370 or vemurafenib as single agents or BI 882370 in combination with ErbB family kinase inhibitor afatinib in HT-29 colorectal cancer model.

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