Document Detail

High performance liquid chromatography analysis of a 4-anilinoquinazoline derivative (PD153035), a specific inhibitor of the epidermal growth factor receptor tyrosine kinase, in rat plasma.
MedLine Citation:
PMID:  15686998     Owner:  NLM     Status:  MEDLINE    
The quinazoline derivative, 4-N-(3'-bromo-phenyl)amino-6,7-dimethoxyquinazoline (PD153035), has recently been identified as a potential drug for the treatment of proliferative disease. Here, we report a sensitive high performance liquid chromatography (HPLC)-based quantitative detection method for measurement of PD153035 levels in rat plasma. Sample pretreatment involved a two-step extraction with chloroform. The analytes were separated on a column packed with OmniSpher C18 material and eluted with acetonitrile-0.1 M ammonium acetate, pH 7.2 (70:30, v/v). The column effluent was monitored by UV detection at 330 nm. A linear response was achieved over the concentration range 0.50-100.00 microM using multilevel calibration with an internal standard. The analytical method inter- and intra-run accuracy and precision were better than +/-15%. The lower limit of quantification was 0.50 microM. The method has been applied to study the preclinical pharmacokinetics of this compound in rats.
Silvana Aparecida Rocco; Jesus Antonio Velho; Rodrigo Miguel Marin; Luís de Arruda Rolim Filho; Anibal Eugênio Vercesi; Roberto Rittner; Kleber Gomes Franchini
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't; Validation Studies    
Journal Detail:
Title:  Journal of chromatography. B, Analytical technologies in the biomedical and life sciences     Volume:  817     ISSN:  1570-0232     ISO Abbreviation:  J. Chromatogr. B Analyt. Technol. Biomed. Life Sci.     Publication Date:  2005 Mar 
Date Detail:
Created Date:  2005-02-02     Completed Date:  2005-09-01     Revised Date:  2009-11-19    
Medline Journal Info:
Nlm Unique ID:  101139554     Medline TA:  J Chromatogr B Analyt Technol Biomed Life Sci     Country:  United States    
Other Details:
Languages:  eng     Pagination:  297-302     Citation Subset:  IM    
Department of Internal Medicine, School of Medicine, Universidade Estadual de Campinas (UNICAMP), Zeferino Vaz Street, Barao Geraldo, 13083-970 Campinas, Sao Paulo, Brazil.
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MeSH Terms
Chromatography, High Pressure Liquid / methods*
Enzyme Inhibitors / blood*,  pharmacokinetics
Quinazolines / blood*,  pharmacokinetics
Rats, Wistar
Receptor, Epidermal Growth Factor / antagonists & inhibitors*
Reference Standards
Reproducibility of Results
Sensitivity and Specificity
Spectrophotometry, Ultraviolet
Reg. No./Substance:
0/4-((3-bromophenyl)amino)-6,7-dimethoxyquinazoline; 0/Enzyme Inhibitors; 0/Quinazolines; EC, Epidermal Growth Factor

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