Comprehensive Predictive Biomarker Analysis for MEK Inhibitor GSK1120212

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Preclinical Development Comprehensive Predictive Biomarker Analysis for MEK Inhibitor GSK1120212

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The MEK1 and MEK2 inhibitor GSK1120212 is currently in phase II/III clinical development. To identify predictive biomarkers, sensitivity to GSK1120212 was profiled for 218 solid tumor cell lines and 81 hematologic malignancy cell lines. For solid tumors, RAF/RAS mutation was a strong predictor of sensitivity. Among RAF/RAS mutant lines, co-occurring PIK3CA/PTEN mutations conferred a cytostatic ...

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GSK1120212 (JTP-74057) is an inhibitor of MEK activity and activation with favorable pharmacokinetic properties for sustained in vivo pathway inhibition.

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ژورنال

عنوان ژورنال: Molecular Cancer Therapeutics

سال: 2011

ISSN: 1535-7163,1538-8514

DOI: 10.1158/1535-7163.mct-11-0505