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Updated: Aug 17, 2026

Implementation of In Vitro Drug Resistance Assays: Maximizing the Potential for Uncovering Clinically Relevant Resistance Mechanisms
08:46

Implementation of In Vitro Drug Resistance Assays: Maximizing the Potential for Uncovering Clinically Relevant Resistance Mechanisms

Published on: December 9, 2015

Reversal of multidrug resistance by the staurosporine derivatives CGP 41251 and CGP 42700

I Utz1, M Spitaler, M Rybczynska

  • 1Institute of Medical Chemistry and Biochemistry, University of Innsbruck, Austria.

International Journal of Cancer
|June 25, 1998
PubMed

Insights

CGP 42700 effectively reverses multidrug resistance in serum, unlike CGP 41251. This staurosporine derivative shows potential as a less toxic anticancer agent with fewer side effects.

Area of Science:

  • Pharmacology
  • Cancer Biology
  • Drug Discovery

Background:

  • Staurosporine derivative CGP 41251 inhibits protein kinase C and multidrug resistance.
  • CGP 41251 is currently in clinical trials as an anticancer drug.
  • CGP 42700 is another staurosporine derivative with low protein kinase C inhibitory activity.

Purpose of the Study:

  • Compare the effects of CGP 41251 and CGP 42700.
  • Evaluate their efficacy in reversing multidrug resistance.
  • Assess their potential as anticancer agents with reduced toxicity.

Main Methods:

  • Cell-based assays using HeLa and KB cells.
  • Assessment of multidrug resistance reversal in KB-C1 and HeLa-MDR1 cells.
  • Rhodamine 123 accumulation and efflux assays using human CD8+ cells.

Main Results:

  • CGP 42700 lacks antiproliferative activity against HeLa and KB cells.
  • Both CGP 41251 and CGP 42700 reversed mdr1-mediated resistance.
  • CGP 42700 demonstrated superior inhibition of rhodamine 123 efflux in serum.

Conclusions:

  • CGP 42700 is more effective in reversing multidrug resistance in serum compared to CGP 41251.
  • CGP 42700's lack of protein kinase C inhibition suggests lower toxicity and fewer side effects.
  • CGP 42700 holds promise as a potential therapeutic agent for cancer patients.

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