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TAK 733

Known as: MEK Inhibitor TAK-733, TAK-733, TAK733 
An orally bioavailable small-molecule inhibitor of MEK1 and MEK2 (MEK1/2) with potential antineoplastic activity. MEK inhibitor TAK-733 selectively… 
National Institutes of Health

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PyridonesPyrimidinones

Papers overview

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2018
2018
TAK-733, a Selective MEK Inhibitor, Enhances Voreloxin-induced Apoptosis in Myeloid Leukemia Cells
Background/Aim: MEK inhibitors are new promising anticancer drugs. The aim of this study was to investigate the effect of the… 
2017
2017
Chemical-biology approach to delineate the mechanism of action of HIV-1 latency reversing agents
Prostratin exhibits potent HIV-1 latency reversing activity, yet its molecular mechanism of action has not been defined in detail… 
2013
2013
Phase I, dose-escalation study of the investigational drug TAK-733, an oral MEK inhibitor, in patients (pts) with advanced solid tumors.
2528 Background: This first-in-human study evaluated the safety, pharmacokinetics (PK), pharmacodynamics (PD), MTD, and efficacy… 
2013
2013
Synthesis of TAK-733
Significance: MEK kinases regulate the pathway that mediates proliferative and anti-apoptotic signaling factors that promote… 
2012
2012
Abstract 3739: TAK-733, an investigational, selective MEK1/2 inhibitor, in combination with alisertib (MLN8237), an investigational, selective Aurora A kinase inhibitor is tolerated and results in…
MEK and Aurora A kinase inhibitors (AAK) have profound impacts on cell cycle progression. Inhibition of MEK leads to defects in… 
2012
2012
393 TAK-733, an Investigational Novel MEK Inhibitor, Suppresses Colorectal Cancer (CRC) Tumor Growth in Biomarker Positive Patient-derived Human Tumor Explants
2011
2011
First-in-human, multicenter, dose-escalation, phase I study of the investigational drug TAK-733, an oral MEK inhibitor, in patients (pts) with advanced nonhematologic malignancies and melanoma.
TPS145 Background: The Ras/Raf/MEK/ERK cascade is frequently activated in human cancers; MEK inhibition is an attractive… 
2010
2010
Abstract 5217: Evaluation of the therapeutic efficacy of MEK inhibitor (TAK-733) using [18F]FDG-PET in the human lung xenograft model A549
Introduction: TAK-733 is a novel, potent, selective, non-ATP competitive, allosteric inhibitor of MEK kinase, which has a… 
2010
2010
600 Preclinical pharmacokinetics–pharmacodynamics (PK-PD) modeling of TAK-733, an investigational MEK inhibitor
2010
2010
Abstract 2520: TAK-733, a novel MEK1/2 inhibitor, inhibits tumor angiogenesis without affecting vascular permeability
Proceedings: AACR 101st Annual Meeting 2010‐‐ Apr 17‐21, 2010; Washington, DC TAK-733 is a highly potent, selective, and non-ATP… 
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