A Simple LC-MS/MS Method for the Quantification of PDA-66 in Human Plasma

被引：0

作者：

Schwarz, Rico ^{[1
]}

Seiler, Elisabeth R. D. ^{[1
]}

Sender, Sina ^{[2
]}

Pews-Davtyan, Anahit ^{[3
]}

Murua Escobar, Hugo ^{[2
]}

Zechner, Dietmar ^{[4
]}

Beller, Matthias ^{[3
]}

Junghanss, Christian ^{[2
]}

Hinz, Burkhard ^{[1
]}

机构：

[1] Rostock Univ, Med Ctr, Inst Pharmacol & Toxicol, D-18057 Rostock, Germany

[2] Rostock Univ, Med Ctr, Clin Hematol Oncol & Palliat Care, D-18057 Rostock, Germany

[3] Univ Rostock, Leibniz Inst Catalysis eV, D-18059 Rostock, Germany

[4] Rostock Univ, Med Ctr, Rudolf Zenker Inst Expt Surg, D-18057 Rostock, Germany

来源：

MOLECULES | 2022年 / 27卷 / 03期

关键词：

PDA-66; human plasma; LC-MS; MS; validation; liquid-liquid extraction; STRATEGIES;

D O I：

10.3390/molecules27030974

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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 3 beta 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.

引用

页数：10

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