In Vitro Efficacy Testing Services for Gastrointestinal Stromal Tumor

We provide robust and sensitive in vitro screening and characterization platforms for accelerating the discovery and screening of potential therapies for Gastrointestinal Stromal Tumor (GIST). Our services are designed to evaluate compound efficacy, mechanism of action, and molecular interactions relevant to GIST, with a focus on key targets such as KIT, PDGFRA, and downstream signaling pathways. These assays enable the investigation of cell proliferation, kinase activity, receptor-ligand interactions, and drug resistance mechanisms associated with GIST. By modeling the pathological processes of signal transduction and aberrant kinase activation, we support comprehensive preclinical assessment of candidate therapies.

We offer a diverse portfolio of in vitro assay platforms, including biochemical, cell-based, and binding assays, to assess drug activity and molecular interactions in GIST models. These methods enable precise evaluation of therapeutic candidates at multiple biological levels, supporting lead optimization and target validation. Our approach ensures comprehensive profiling of efficacy, specificity, and mechanism of action.

ATP assay: Measures cellular ATP levels as an indicator of cell viability and proliferation, crucial for evaluating cytotoxicity and antiproliferative effects of compounds.

Bioluminescence resonance energy transfer (BRET) assay: Detects real-time protein-protein or protein-ligand interactions, allowing investigation of signaling pathways and target engagement.

Chemiluminescent assay: Utilizes light emission from chemical reactions to quantify enzymatic activity or molecular binding, offering high sensitivity for detection of specific targets.

Competitive binding assay (qPCR): Assesses binding affinity of compounds to targets via competition, using qPCR for quantification and enabling precise measurement of inhibitor potency.

ELISA assay: Enzyme-linked immunosorbent assay enables detection and quantification of proteins, peptides, or antibodies, supporting biomarker analysis and target validation.

Fluorescent polarization assay: Measures binding interactions or enzymatic activity based on changes in fluorescence polarization, useful for screening inhibitors and characterizing binding kinetics.

Luciferine/luciferase assay: Quantifies cellular or enzymatic activity using luciferase-catalyzed light emission, facilitating assessment of cell viability or gene expression.

Peptide as substrate: Employs synthetic peptides to evaluate enzyme activity, particularly kinases, for detailed characterization of substrate specificity and inhibitor effects.

Poly(L-alanine/L-glutamic acid/L-lysine/L-tyrosine) as substrate: Uses defined synthetic polymers to assess broad kinase or protease activity, supporting specificity profiling.

Poly(glutamine/tyrosine) peptide as substrate: Tests enzyme activity against multi-residue peptides, aiding in the evaluation of substrate preferences and inhibitor selectivity.

Radioactivity assay: Uses radiolabeled substrates or ligands to measure enzyme activity or binding events, providing highly sensitive and quantitative data.

Rhodamine 123 accumulation assay: Evaluates mitochondrial function and efflux transporter activity, relevant for assessing drug resistance and cellular health.

Surface plasmon resonance assay: Analyzes real-time biomolecular interactions without labeling, offering kinetic and affinity data for drug-target binding.

We measure a range of pharmacological parameters that quantify compound potency, binding affinity, and inhibitory activity. These metrics are essential for comparing candidate drugs, optimizing lead compounds, and predicting in vivo efficacy. Accurate parameter assessment supports informed decision-making throughout the drug development process.

IC-50: The concentration of a compound required to inhibit a biological process or enzyme activity by 50%, widely used to compare compound potency.

Kd: The dissociation constant, representing the affinity between a ligand and its target; lower Kd values indicate stronger binding.

Ki: The inhibition constant, reflecting the binding affinity of an inhibitor to its target enzyme, crucial for characterizing inhibitory mechanisms.

MIC: Minimum inhibitory concentration, the lowest concentration of a compound that prevents visible growth of microorganisms or cells, important for assessing efficacy.

pIC-50: The negative logarithm of the IC-50 value, providing a standardized measure of compound potency for comparative analysis.

Recommended In Vitro Efficacy Tests

Abl Proto-Oncogene 1, Non-Receptor Tyrosine Kinase

Abl Proto-Oncogene 1, Non-Receptor Tyrosine Kinase (ABL1) plays a pivotal role in cell signaling and proliferation in Gastrointestinal Stromal Tumors (GIST). Testing ABL1 is crucial for identifying mutations that influence drug sensitivity and resistance. Key methods include PCR, sequencing, and immunohistochemistry. Main parameters assessed are mutation status, expression levels, and phosphorylation activity, guiding targeted therapy development and personalized treatment strategies for GIST.

Atp Binding Cassette Subfamily B Member 1

Atp Binding Cassette Subfamily B Member 1 (ABCB1) mediates drug efflux in Gastrointestinal Stromal Tumors (GIST), contributing to multidrug resistance. Testing ABCB1 function is crucial for optimizing therapeutic strategies and overcoming resistance. Our service uses the Rhodamine 123 accumulation assay to assess ABCB1 activity, with the Minimum Inhibitory Concentration (MIC) as a key parameter, enabling precise evaluation of candidate drugs’ efficacy in GIST drug development.

Colony Stimulating Factor 1 Receptor

Colony Stimulating Factor 1 Receptor (CSF1R) plays a critical role in the tumor microenvironment of Gastrointestinal Stromal Tumors (GIST), influencing tumor growth and immune evasion. CSF1R testing is essential for drug development to evaluate inhibitor efficacy. Our service utilizes BRET, chemiluminescent, ATP, and ELISA assays to assess compound activity, with IC-50 as the primary parameter, providing robust, quantitative insights into CSF1R-targeted therapeutic potential.

Fms Related Receptor Tyrosine Kinase 1

Fms Related Receptor Tyrosine Kinase 1 (FLT1) is implicated in angiogenesis and tumor progression in Gastrointestinal Stromal Tumors (GIST). FLT1 testing is crucial for evaluating targeted drug efficacy. Our service utilizes ELISA assays to quantify FLT1 activity and determine drug inhibition potency, with IC-50 as the main parameter to assess compound effectiveness, supporting GIST drug development and candidate selection.

Fms Related Receptor Tyrosine Kinase 3

Fms Related Receptor Tyrosine Kinase 3 (FLT3) plays a pivotal role in the proliferation and survival of Gastrointestinal Stromal Tumor (GIST) cells. FLT3 testing is crucial for identifying candidate drugs that inhibit this kinase. Services employ chemiluminescent assays, ATP assays, and ELISA using Poly(L-alanine/L-glutamic acid/L-lysine/L-tyrosine) substrates to accurately quantify kinase activity. The primary parameter measured is IC-50, enabling precise evaluation of drug potency against FLT3.

Fms Related Receptor Tyrosine Kinase 4

Fms Related Receptor Tyrosine Kinase 4 (FLT4/VEGFR-3) is implicated in lymphangiogenesis and tumor progression in Gastrointestinal Stromal Tumors (GIST). Testing FLT4 expression and activity is vital for identifying therapeutic targets and monitoring drug efficacy. Key methods include immunohistochemistry, qPCR, and ELISA. Main parameters assessed are FLT4 protein levels, gene expression, and phosphorylation status, providing essential insights for GIST drug development.

Heat Shock Protein 90 Alpha Family Class A Member 1

Heat Shock Protein 90 Alpha Family Class A Member 1 (HSP90AA1) is crucial for stabilizing oncogenic proteins in Gastrointestinal Stromal Tumor (GIST). Testing its activity helps identify potential inhibitors for targeted drug development. We offer fluorescent polarization and radioactivity assays to evaluate HSP90AA1 inhibition, providing precise IC₅₀ and Kᵢ values—key parameters for assessing compound potency and binding affinity in GIST therapeutic research.

Kinase Insert Domain Receptor

The Kinase Insert Domain Receptor (KDR), or VEGFR2, drives angiogenesis in Gastrointestinal Stromal Tumors (GIST), influencing tumor growth and progression. Testing KDR activity is vital for screening potential therapeutics. Our service employs luciferin/luciferase, ATP, ELISA, radioactivity, and competitive binding (qPCR) assays, using poly(glutamine/tyrosine) peptides as substrates. We provide precise pIC-50 and IC-50 values, enabling robust evaluation of drug potency and efficacy in GIST drug development.

Kit Proto-Oncogene, Receptor Tyrosine Kinase

Kit Proto-Oncogene, Receptor Tyrosine Kinase (KIT) is a key driver mutation in Gastrointestinal Stromal Tumors (GIST), crucial for tumor growth and survival. KIT testing is vital for developing targeted therapies. Our service utilizes peptide substrate assays, ATP assays, and ELISA to evaluate KIT kinase activity, enabling precise assessment of inhibitor efficacy. The primary parameter measured is IC-50, indicating compound potency in inhibiting KIT function.

Platelet Derived Growth Factor Receptor Alpha

Platelet Derived Growth Factor Receptor Alpha (PDGFRA) is a key driver mutation in many Gastrointestinal Stromal Tumors (GIST), impacting tumor growth and drug response. PDGFRA testing is vital for identifying effective targeted therapies. Our service employs ATP and ELISA assays, peptide substrates, surface plasmon resonance, and radioactivity assays to assess inhibitor potency and binding. Main parameters measured include IC-50 (inhibitory concentration) and Kd (binding affinity), supporting robust GIST drug development.

Platelet Derived Growth Factor Receptor Beta

Platelet Derived Growth Factor Receptor Beta (PDGFRβ) plays a critical role in Gastrointestinal Stromal Tumor (GIST) pathogenesis by driving cell proliferation and survival. PDGFRβ testing is vital for identifying mutations and guiding targeted therapy development. Key methods include immunohistochemistry, PCR, and sequencing. Main parameters assessed are PDGFRβ expression levels, mutation status, and receptor activation, providing essential data for personalized GIST drug development.

Ret Proto-Oncogene

Ret Proto-Oncogene testing in Gastrointestinal Stromal Tumor (GIST) assesses mutations or aberrant expression that may drive tumorigenesis. This testing is crucial for identifying patients who may benefit from targeted therapies. Key methods include PCR, Sanger sequencing, and next-generation sequencing (NGS). Main parameters analyzed are mutation status, gene expression levels, and variant type, supporting precision drug development and personalized treatment strategies in GIST.