Internalization Assay Services of Radiolabeled Compounds

At Alfa Cytology, we are experts in offering the full spectrum of radiopharmaceutical discovery and development services. We offer comprehensive internalization assay services , which ensures our clients get top-tier support in the development of their drug.

Introduction to Internalization Assays

Internalization means the uptake of substances, including radiopharmaceuticals, by the cells through the cell membrane. An in vitro internalization assay is important in assessing the activity of radiopharmaceuticals. Such an assay would reflect the way a radiopharmaceutical can effectively get into target cells, which was shown to be largely predictive of its eventual therapeutic efficiency and safety.

Fig. 1. Internalization assay reveals resonator uptake by different cell types. (Schubert M, et al., 2017)

Our Internalization Assay Services

We, Alfa Cytology, offer a full spectra of internalization assays, like receptor-mediated internalization, endocytosis, and intracellular trafficking assays. Our efficient team of scientists uses state-of-the-art instruments and techniques in an effort to provide accurate and reliable data related to the internalization of radiopharmaceuticals for project customers.

With our cell-based assay, you receive the information on the kinetics of internalization and the rate of radiolabelled compound internalization. Our internalization analysis can tell the difference between the radiolabelled compounds associated only with cell surface receptors and the fraction taken up.

Our Internalization Analysis Methodologies

We use techniques that apply advanced methodologies to ensure effective, accurate, and reliable internalization analysis.

• Radiolabeling Techniques
• Cellular Assays
• Advanced Imaging

Internalization Assay Validation

Validation is part of our internalization assay process. Every one of the assays is extensively validated to establish its reliability and reproducibility for established radiopharmaceuticals. Therefore, you are assured that the data produced are accurate and actional, thus very important in making a decision in your drug development process.

Our Technological Platform

We leverage cutting-edge technology platforms to support our internalization assays.

• Automated Liquid Handling Systems
• High-Performance Liquid Chromatography
• Flow Cytometry
• Gamma Counters
• Confocal Microscopy

Applications of Internalization Analysis

• Target Validation
• Mechanism of Action Studies
• Optimization of Drug Candidates
• Safety and Efficacy Assessment

Case Study: Internalization Assay of [³H]-Labeled Small Molecule

Conducted to evaluate the cellular internalization kinetics of a novel [³H]-labeled small molecule ligand targeting a specific intracellular pathway, the assay quantified and differentiated surface-bound versus internalized ligand fractions over time in two distinct cell models: DLD-1 and HEK-293T. Understanding the kinetics and extent of ligand internalization was deemed critical for assessing its potential as a targeted therapeutic or diagnostic agent, as these parameters directly influenced intracellular drug delivery and efficacy.

Fig.2 Time-dependent internalization of [³H]-labeled small molecule in DLD-1 and HEK-293T cells.

Marked divergence was observed in the [³H]-ligand internalization profiles between the two cell lines. Efficient internalization was demonstrated in DLD-1 cells, with a substantial proportion internalized after 24 hours. In contrast, the ligand remained predominantly surface-associated in HEK-293T cells. This indicated that DLD-1 cells possess a more active endocytic pathway for this molecule.

To learn more about our internalization assay services and how Alfa Cytology can support your radiopharmaceutical development efforts, please contact us. Our team is ready to provide the expertise and resources you need to advance your research.

Reference

1. Schubert M, Volckaert K, Karl M, et al. (2017). Lasing in Live Mitotic and Non-Phagocytic Cells by Efficient Delivery of Microresonators. Sci Rep. 7:40877.

For research use only. Not intended for any clinical use.