Simultaneous determination of Z-SU5416 and its interconvertible geometric E-isomer in rat plasma by LC/MS/MS

SU5416 is a selective inhibitor of vascular endothelial growth factor (VEGF) receptor, which plays a major role in vascular angiogenesis. SU5416 exists as the thermodynamically stable and pharmacologically active cis isomer (Z-isomer) in the solid state. In light-exposed solutions the unstable trans...

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Veröffentlicht in:Journal of pharmaceutical and biomedical analysis 2004-05, Vol.35 (3), p.513-522
Hauptverfasser: Zhao, Yeping, Sukbuntherng, Juthamas, Antonian, Lida
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container_title Journal of pharmaceutical and biomedical analysis
container_volume 35
creator Zhao, Yeping
Sukbuntherng, Juthamas
Antonian, Lida
description SU5416 is a selective inhibitor of vascular endothelial growth factor (VEGF) receptor, which plays a major role in vascular angiogenesis. SU5416 exists as the thermodynamically stable and pharmacologically active cis isomer (Z-isomer) in the solid state. In light-exposed solutions the unstable trans isomer (E-isomer) is formed. The E-isomer is unstable for synthesis and isolation and the analytical standard of the E-isomer is unavailable. A new, simple, fast and reliable LC/MS/MS method was developed to quantify both isomers simultaneously in rat plasma samples in order to support the study of disposition kinetics of Z- and E-SU5416. This method is sensitive (LOQ=0.5 ng/ml), reproducible, and has a wide linear range (0.5–2500 ng/ml).
doi_str_mv 10.1016/j.jpba.2003.08.017
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source MEDLINE; ScienceDirect Journals (5 years ago - present)
subjects Analysis
Analytical, structural and metabolic biochemistry
Animals
Biological and medical sciences
E- and Z-isomers
Fundamental and applied biological sciences. Psychology
Gas Chromatography-Mass Spectrometry - methods
General pharmacology
Indoles - blood
LC/MS/MS
Medical sciences
Pharmacology. Drug treatments
Pyrroles - blood
Rats
Stereoisomerism
Technology, Pharmaceutical - methods
Z-SU5416
title Simultaneous determination of Z-SU5416 and its interconvertible geometric E-isomer in rat plasma by LC/MS/MS
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