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A Simple LC-MS/MS Method for the Quantification of PDA-66 in Human Plasma
Rico Schwarz1, Elisabeth R D Seiler1, Sina Sender2
1Institute of Pharmacology and Toxicology, Rostock University Medical Centre, 18057 Rostock, Germany.
Abstract:
The treatment of cancer is one of the most important pharmacotherapeutic challenges. To this end, chemotherapy has for some time been complemented by targeted therapies against specific structures. PDA-66, a structural analogue of the inhibitor of serine-threonine kinase glycogen synthase kinase 3β SB216763, has shown preclinical antitumour effects in various cell lines, with the key pathways of its anticancer activity being cell cycle modulation, DNA replication and p53 signalling. For the monitoring of anticancer drug treatment in the context of therapeutic drug monitoring, the determination of plasma concentrations is essential, for which an LC-MS/MS method is particularly suitable. In the present study, a sensitive LC-MS/MS method for the quantification of the potential anticancer drug PDA-66 in human plasma with a lower limit of quantification of 2.5 nM is presented. The method was successfully validated and tested for the determination of PDA-66 in mouse plasma and sera.
Insights
A new liquid chromatography-tandem mass spectrometry (LC-MS/MS) method quantifies the potential anticancer drug PDA-66 in human plasma. This method is crucial for therapeutic drug monitoring and cancer treatment research.
Area of Science:
- Pharmacology and Therapeutics
- Analytical Chemistry
- Cancer Biology
Background:
- Cancer treatment relies on chemotherapy and targeted therapies.
- PDA-66, a glycogen synthase kinase 3β inhibitor analogue, exhibits preclinical anticancer effects.
- Key anticancer mechanisms of PDA-66 involve cell cycle, DNA replication, and p53 signaling.
Purpose of the Study:
- To develop and validate a sensitive LC-MS/MS method for quantifying PDA-66 in human plasma.
- To establish a reliable method for therapeutic drug monitoring of PDA-66.
- To assess the utility of the method for quantifying PDA-66 in animal plasma and sera.
Main Methods:
- Development of a liquid chromatography-tandem mass spectrometry (LC-MS/MS) assay.
- Quantification of PDA-66 in human plasma samples.
- Method validation and application to mouse plasma and sera.
Main Results:
- A sensitive LC-MS/MS method for PDA-66 quantification was established.
- The method achieved a lower limit of quantification of 2.5 nM in human plasma.
- The method was successfully validated and applied to mouse plasma and sera.
Conclusions:
- The developed LC-MS/MS method enables sensitive and reliable quantification of PDA-66.
- This method is suitable for therapeutic drug monitoring in cancer patients.
- The validated method supports preclinical and clinical studies of PDA-66.
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