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Updated: Aug 6, 2026
Fluorescence Molecular Tomography for In Vivo Imaging of Glioblastoma Xenografts
Published on: April 26, 2018
Novel EGFR tyrosine kinase inhibitors exhibiting intrinsic fluorescence
Amelia Kierasińska-Kałka1,2, Adrianna Rutkowska3,4, Jacek Mularski5
1Department of Research and Development, LEK-AM Pharmaceutical Company Ltd., Inwestycyjna 7, 95-050, Konstantynow Lodzki, Poland. amelia.kierasinska1@gmail.com.
Abstract:
Kinase inhibitors are commonly used in research and clinical practice. Among them, irreversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs), such as afatinib and osimertinib, constitute an important subclass. The aim of this study was to create an irreversible covalent EGFR TKI exhibiting endogenous fluorescence, i.e., intrinsic fluorescence without the need for additional fluorochromes. These compounds, designated SQI-2, SLT40, and SLT41, were successfully developed and shown to effectively inhibit the EGFR, EGFRL858R/T790M, and EGFRvIII kinases. The developed compounds are suitable for a range of cytochemical analyses, including real-time assays. The proposed TKIs may serve as research and diagnostic tools and represent precursors of new types of therapeutic compounds.
Insights
Researchers developed novel fluorescent irreversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs). These compounds effectively inhibit EGFR kinases and can be used for real-time cytochemical analyses as research tools.
Area of Science:
- Biochemistry
- Molecular Biology
- Medicinal Chemistry
Background:
- Irreversible tyrosine kinase inhibitors (TKIs) targeting the epidermal growth factor receptor (EGFR) are crucial in cancer research and therapy.
- Existing EGFR TKIs often require external labeling for fluorescence-based assays, limiting real-time applications.
Purpose of the Study:
- To design and synthesize novel irreversible covalent EGFR TKIs with intrinsic fluorescence.
- To evaluate the inhibitory activity of these fluorescent TKIs against various EGFR mutations.
Main Methods:
- Chemical synthesis of novel irreversible covalent EGFR TKIs (SQI-2, SLT40, SLT41).
- Biochemical assays to determine kinase inhibition against wild-type and mutant EGFR.
- Assessment of compound suitability for cytochemical analyses.
Main Results:
- Successful development of three novel irreversible covalent EGFR TKIs (SQI-2, SLT40, SLT41) exhibiting endogenous fluorescence.
- Demonstrated potent inhibition of EGFR, EGFRL858R/T790M, and EGFRvIII kinases.
- Confirmed suitability of the compounds for cytochemical analyses, including real-time assays.
Conclusions:
- The developed fluorescent irreversible EGFR TKIs serve as valuable tools for cytochemical research and diagnostics.
- These compounds represent a new class of potential therapeutic agents and research probes for EGFR-related studies.
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