Development and validation of a sensitive LC MS/MS method for the measurement of the checkpoint kinase 1 inhibitor prexasertib and its application in a cerebral microdialysis study

J Pharm Biomed Anal. 2018 Jul 15:156:97-103. doi: 10.1016/j.jpba.2018.04.018. Epub 2018 Apr 17.

Abstract

LC MS/MS methods to measure prexasertib in mouse plasma and Ringer's solution containing 0.5% BSA (Ringer's/BSA) were developed and validated. Liquid-liquid extraction with tert-butyl methyl ether was used to extract prexasertib from mouse plasma and Ringer's/BSA. Reverse phase chromatography with gradient elution was performed to separate prexasertib from the endogenous interference in the matrix, followed by MS detection using positive ion MRM mode. The initial calibration curve for mouse plasma samples ranged from 1 to 500 ng/ml, and after validation of that curve and use in a preliminary study another calibration curve (0.2-200 ng/ml) was created to enable the quantitation of prexasertib at lower concentrations. The method described was precise and accurate with %CV in precision studies of ≤ 6.7% and accuracies within 95.0-110% of nominal target concentration across all concentrations tested for both matrices. This validated method was successfully applied in the analysis of prexasertib in mouse plasma and dialysate samples collected during a cerebral microdialysis study.

Keywords: Chk1; LC–MS/MS; Liquid-liquid extraction; Microdialysis; Prexasertib; Ringer’s solution.

Publication types

  • Validation Study

MeSH terms

  • Animals
  • Blood-Brain Barrier
  • Brain / blood supply
  • Brain / metabolism
  • Calibration
  • Cerebellar Neoplasms / blood*
  • Cerebellar Neoplasms / drug therapy
  • Checkpoint Kinase 1 / antagonists & inhibitors
  • Child
  • Chromatography, Liquid
  • Chromatography, Reverse-Phase
  • Dialysis Solutions / analysis*
  • Female
  • Humans
  • Limit of Detection
  • Liquid-Liquid Extraction
  • Medulloblastoma / blood*
  • Medulloblastoma / drug therapy
  • Mice
  • Mice, Nude
  • Microdialysis
  • Protein Kinase Inhibitors / analysis*
  • Protein Kinase Inhibitors / therapeutic use
  • Pyrazines / analysis*
  • Pyrazines / therapeutic use
  • Pyrazoles / analysis*
  • Pyrazoles / therapeutic use
  • Reference Standards
  • Reproducibility of Results
  • Tandem Mass Spectrometry
  • Xenograft Model Antitumor Assays

Substances

  • Dialysis Solutions
  • Protein Kinase Inhibitors
  • Pyrazines
  • Pyrazoles
  • prexasertib
  • CHEK1 protein, human
  • Checkpoint Kinase 1