Description

Product Description

Regorafenib is a high-purity, laboratory-grade small molecule kinase inhibitor developed for in vitro mechanistic and molecular pathway research. Its stable chemical structure and verified high purity make it a reliable tool for investigating signal transduction, kinase inhibition, and protein-ligand interactions in controlled laboratory environments.

This compound is widely used in biochemical and mechanistic studies, including enzyme assays, phosphorylation analysis, and molecular pathway modulation experiments. Its reproducible activity allows researchers to explore dose-response relationships, inhibitor selectivity, and molecular binding kinetics without interference from impurities or degradation products.

Regorafenib’s versatility makes it suitable for cell-free systems, purified enzyme assays, and synthetic protein models, where precise control over experimental conditions is required. Its high solubility in common organic solvents such as DMSO and DMF allows easy preparation of stock solutions for various in vitro assays.

The compound also supports analytical method development, serving as a reference for validating HPLC, mass spectrometry, and spectroscopic assays. Researchers can confidently integrate Regorafenib into high-throughput screening, kinase profiling, and structure-activity relationship studies, generating reproducible data to elucidate mechanistic pathways.

Factory-controlled production ensures bulk, wholesale, and customized supply options, including variable concentrations and packaging formats. Each batch is accompanied by a Certificate of Analysis (CoA) verifying chemical purity, solubility, and stability, ensuring consistency across laboratories.

By combining high purity, chemical stability, and reproducible activity, Regorafenib provides a robust platform for molecular mechanism research, kinase inhibition studies, and biochemical pathway analysis. Its application in in vitro experimental models enables laboratories to generate reliable, high-quality data supporting mechanistic insights, drug-target interaction studies, and pathway elucidation.

Regorafenib’s factory-manufactured, low-price wholesale availability ensures researchers can obtain sufficient quantities for extended studies without compromising on quality, reproducibility, or experimental integrity. Overall, it is a versatile and indispensable reagent for laboratories conducting in-depth mechanistic and molecular research.

Product Specifications

Notes

Regorafenib is manufactured under strict factory-controlled conditions to maintain chemical purity, stability, and reproducibility. Bulk and wholesale orders are supported with custom concentrations, packaging options, and batch-specific Certificates of Analysis (CoA). This ensures high-quality material for mechanistic, biochemical, and molecular pathway research.

Mechanism of Action

Regorafenib is a multi-kinase inhibitor designed for in vitro mechanistic studies. It targets a range of receptor tyrosine kinases (RTKs) and intracellular kinases, providing a valuable tool to investigate signal transduction, enzyme inhibition, and molecular pathway regulation in controlled laboratory settings.

1. Kinase Inhibition Mechanism

Regorafenib binds to the ATP-binding sites of kinases, inhibiting their catalytic activity. In vitro studies using purified kinases or cell-free systems can reveal dose-dependent inhibition, kinase selectivity, and interaction dynamics, allowing detailed mechanistic mapping.

2. Molecular Pathway Modulation

In biochemical assays, Regorafenib affects pathways involved in proliferation, angiogenesis, and stress response by modulating kinase activity. Researchers can examine downstream phosphorylation events, signal cascade alterations, and protein interaction networks under controlled conditions.

3. Drug-Target Binding Analysis

Mechanistic studies can include binding affinity measurements, enzyme kinetics, and conformational changes in target proteins. Techniques such as surface plasmon resonance (SPR), isothermal titration calorimetry (ITC), and spectroscopic analysis can be used to characterize molecular interactions.

4. Structural and Functional Studies

Regorafenib’s high purity and stability allow experiments on protein-ligand complex formation, structure-activity relationships, and kinase conformational dynamics. This supports reproducible, detailed in vitro studies of molecular mechanisms.

5. Analytical Validation

The compound can also serve as a reference standard for validating analytical assays, screening platforms, and high-throughput mechanistic studies, ensuring experimental accuracy and reproducibility.

Overall, Regorafenib provides a robust tool for in vitro mechanistic research, enabling laboratories to study kinase inhibition, molecular pathway modulation, and biochemical interactions under highly controlled conditions.

Applications

Regorafenib is widely used in in vitro mechanistic and molecular research due to its high-purity and stable formulation, making it suitable for studying kinase inhibition, signal transduction, and molecular pathway modulation.

1. Kinase Activity Assays

Regorafenib is ideal for investigating ATP-competitive kinase inhibition in purified enzyme systems or cell-free assays. Researchers can assess dose-response relationships, inhibitor selectivity, and catalytic activity modulation.

2. Molecular Pathway Studies

The compound allows laboratories to explore biochemical signaling cascades, including pathways regulating proliferation, stress response, and angiogenesis. Mechanistic studies can include phosphorylation monitoring, protein interaction analysis, and downstream signaling modulation.

3. Structure-Activity Relationship (SAR) Studies

High-purity Regorafenib supports protein-ligand binding studies, structural dynamics analysis, and SAR mapping. This enables detailed evaluation of kinase-inhibitor interactions and molecular conformational changes.

4. Analytical Method Development

It serves as a reference standard for validating HPLC, spectroscopy, mass spectrometry, and high-throughput screening assays, ensuring reproducible mechanistic data.

5. Computational Integration

Experimental results can be combined with molecular docking, predictive modeling, and in silico simulations to validate mechanistic hypotheses and refine pathway models.

6. High-Throughput Screening

Compatible with automated platforms, Regorafenib allows parallel testing of multiple conditions, including kinase variants, co-factors, and environmental parameters, enhancing throughput for mechanistic investigations.

Overall, Regorafenib provides a versatile platform for laboratories studying kinase inhibition, molecular signaling, and mechanistic biochemistry under fully controlled in vitro conditions.

Research Models

Regorafenib is designed for in vitro research models that allow detailed exploration of kinase inhibition, signal transduction, and molecular pathway modulation. Its high purity and stable formulation provide reproducible results across diverse mechanistic studies.

1. Enzyme-Based Models

In cell-free systems, Regorafenib can be applied to purified kinase assays to study ATP-competitive inhibition, catalytic kinetics, and dose-dependent activity modulation. These models allow precise measurement of enzyme-inhibitor interactions under controlled conditions.

2. Signal Transduction Pathway Models

The compound supports biochemical pathway studies, including analysis of phosphorylation cascades, downstream signaling effects, and protein-protein interactions. Controlled in vitro models provide reproducible mechanistic insights without cellular complexity.

3. Protein-Ligand Interaction Models

Regorafenib facilitates binding studies with target kinases, including evaluation of binding affinity, conformational changes, and structure-activity relationships. Analytical techniques such as SPR, ITC, and spectroscopy are commonly used to validate these models.

4. Analytical Validation Models

High-purity Regorafenib serves as a reference standard for validating analytical assays, including HPLC, mass spectrometry, fluorescence-based kinase assays, and high-throughput screening. These models ensure reproducibility and precision across laboratories.

5. Computational Integration Models

Experimental data from these in vitro models can be combined with molecular docking, predictive modeling, and systems biology simulations to explore mechanistic pathways and refine hypotheses.

Overall, Regorafenib enables robust in vitro research models that support mechanistic, structural, and kinetic studies of kinase inhibition and molecular signaling, providing reproducible, high-quality data for laboratory research.

Experimental Design Considerations

Designing experiments with Regorafenib requires careful attention to concentration, environmental conditions, and analytical methods to ensure reliable mechanistic insights.

1. Concentration Optimization

Determine optimal concentrations based on enzyme kinetics, assay sensitivity, and target protein interactions. Perform preliminary titrations to avoid oversaturation or underdetection in in vitro models.

2. Environmental Control

Maintain precise temperature, pH, and buffer conditions, as these parameters affect kinase activity, inhibitor binding, and chemical stability. Controlled conditions ensure reproducible mechanistic outcomes.

3. Time-Course Studies

Design experiments with defined time points to monitor kinase inhibition dynamics, downstream pathway modulation, and signal cascade kinetics. Time-course measurements provide detailed mechanistic data.

4. Analytical Method Integration

Select analytical techniques such as HPLC, mass spectrometry, SPR, or fluorescence spectroscopy to detect molecular interactions, structural changes, and pathway modulation. Integration of multiple methods enhances data robustness.

5. Replication and Controls

Include appropriate controls, replicates, and blank conditions to validate results. Document lot numbers, storage conditions, and experimental procedures for reproducibility.

6. Computational Modeling

Combine experimental data with in silico modeling, docking studies, and pathway simulations to refine hypotheses and validate mechanistic interpretations.

By following these considerations, laboratories can achieve high-precision, reproducible in vitro experiments with Regorafenib, yielding robust data on kinase inhibition, molecular pathway modulation, and biochemical mechanisms.

Laboratory Safety & Handling Guidelines

Regorafenib is a high-purity laboratory reagent intended exclusively for in vitro mechanistic and molecular research. Proper handling ensures chemical stability, experimental reproducibility, and laboratory safety.

1. Personal Protective Equipment (PPE)

Always wear gloves, lab coat, and eye protection when handling Regorafenib. Work in a controlled laboratory environment to prevent contamination and maintain chemical integrity.

2. Handling and Preparation

Use dedicated laboratory consumables to avoid cross-contamination. Dissolve or dilute the compound carefully to preserve molecular integrity and activity.

3. Storage Conditions

Store in sealed, light-protected containers at 2–8°C. Avoid exposure to heat, light, or repeated freeze-thaw cycles, which can affect stability and purity.

4. Spill and Decontamination Procedures

Contain spills immediately with approved absorbents. Clean surfaces using appropriate buffers or decontamination solutions, and dispose of contaminated materials according to institutional chemical waste protocols.

5. Documentation and Traceability

Maintain records of lot numbers, storage conditions, and experimental usage. This ensures reproducibility and supports troubleshooting in mechanistic studies.

6. Laboratory Equipment

Use chemically compatible glassware, pipettes, and plates to prevent adsorption or chemical degradation.

Following these guidelines ensures safe handling, reproducible results, and reliable mechanistic insights in laboratory-based in vitro studies.

Integration with Multi-Omic & Computational Studies

Regorafenib can be integrated into multi-omic workflows and computational modeling to explore kinase inhibition, molecular pathway modulation, and signal transduction mechanisms in vitro. Its stable, high-purity formulation enables reproducible data collection suitable for proteomic, structural, and computational analyses.

1. Proteomic and Structural Integration

In vitro studies with Regorafenib can generate data on kinase-ligand interactions, phosphorylation changes, and protein network modulation. Techniques such as mass spectrometry, western blotting, and structural analyses can map interactions and validate mechanistic hypotheses.

2. Computational Modeling Applications

Data from in vitro assays can be combined with molecular docking, predictive simulations, and pathway modeling. Computational integration helps predict inhibitor-target interactions, refine mechanistic pathways, and corroborate experimental findings.

3. Multi-Omic Correlation

Experimental results can be correlated with transcriptomic, proteomic, or metabolomic datasets from controlled systems to identify mechanistic relationships and pathway modulation. This integration allows robust hypothesis generation and mechanistic validation.

4. Analytical Method Validation

Regorafenib can serve as a reference standard to validate HPLC, fluorescence, or mass spectrometry assays. Integration with computational studies enhances interpretation and reproducibility of mechanistic experiments.

Overall, Regorafenib supports a comprehensive approach combining experimental in vitro data with computational and multi-omic analyses, providing deep mechanistic insights into kinase inhibition and molecular signaling pathways.

Things to Note

1. Laboratory Use Only
   Regorafenib is intended exclusively for in vitro mechanistic, structural, and biochemical research. It is not suitable for human or veterinary use, clinical applications, or diagnostic purposes.

2. Handling and Safety
   Always use appropriate PPE, including gloves, lab coat, and eye protection. Handle in a controlled laboratory environment to maintain chemical stability and experimental integrity.

3. Storage and Stability
   Store in sealed, light-protected containers at 2–8°C. Avoid heat, light exposure, and repeated freeze-thaw cycles, which can compromise chemical purity and activity.

4. Analytical Verification
   Before experiments, confirm purity, solubility, and chemical integrity using techniques such as HPLC, mass spectrometry, or spectroscopy to ensure reproducibility.

5. Waste Management
   Dispose of residual material and contaminated consumables according to institutional chemical waste protocols. Decontaminate surfaces and equipment after use.

6. Experimental Considerations
   Design experiments considering environmental sensitivity, target protein stability, and inhibitor concentration to ensure reliable mechanistic insights.

Following these notes ensures safe handling, reproducible data, and robust mechanistic results in laboratory-based in vitro studies.

Keywords

Regorafenib, high-purity kinase inhibitor, laboratory-grade regorafenib, in vitro mechanistic studies, kinase signaling pathway research, molecular pathway modulation, protein-ligand interaction reagent, enzymatic inhibition assay, biochemical mechanism research, high-throughput in vitro screening, structural dynamics reagent, proteomic and computational integration, factory-manufactured research reagent, bulk and wholesale laboratory supply, mechanistic pathway analysis reagent, controlled laboratory workflow reagent, high-purity solution for in vitro assays, analytical method validation kinase inhibitor, Tumor (compound) Research, multi-omic integration reagent.

Shipping Guarantee

Factory-manufactured Regorafenib is securely packaged to maintain chemical stability, purity, and experimental integrity during transport. Bulk and wholesale orders are supported with secure shipment and tracking, ensuring the product arrives in optimal condition for in vitro mechanistic and molecular studies. Shipments are handled to minimize exposure to heat, light, or contamination.

Trade Assurance

• Low-price wholesale supply directly from the factory.

• Bulk order customization available, including solution concentration and packaging formats.

• Guaranteed high-purity compound for in vitro kinase inhibition and molecular pathway research.

• Factory-direct supply ensures consistent quality and reproducibility across multiple batches.

Payment Support

Multiple secure payment options are available for global laboratory procurement:

• PayPal

• Cryptocurrency

• Bank Transfer (TT)

• Credit Card

• Verified online payment systems

These options provide flexible and secure payment methods for bulk and wholesale orders.

Disclaimer

Regorafenib is intended exclusively for laboratory research use. It is not approved for human or veterinary applications, diagnostic purposes, or therapeutic interventions. All experiments must be conducted in controlled in vitro, molecular, or mechanistic studies. Users must follow institutional safety protocols and chemical handling procedures. The product should never be administered to living organisms or used outside research settings.

References

1. Subramonian D., Phanhthilath N., Rinehardt H., et al. “Regorafenib is effective against neuroblastoma in vitro and in vivo and inhibits the RAS/MAPK, PI3K/Akt/mTOR and Fos/Jun pathways.” British Journal of Cancer, 2020; 123: 568–579. Nature

2. Mesa‑Torrejón A., Verzini E., Romeo C., et al. “Regorafenib reduces cell proliferation and viability in vitro in neuroendocrine tumor models and alters signaling pathways.” British Journal of Cancer, 2023. Nature

3. “Regorafenib (BAY 73‑4506) – multi‑target kinase inhibitor.” Supplier/Research‑use catalog listing (e.g. manufacturer datasheet), notes inhibition of VEGFRs, PDGFRβ, KIT, RET, RAF, etc.; used widely in vitro kinase and signal‑transduction assays. medkoo.com+1

4. “Regorafenib, CAS 755037-03-7 — chemical properties and kinase target profile.” Chemical database entry summarizing molecular formula, CAS, purity, solubility, and main kinase targets (VEGFRs, PDGFR, KIT, RET, RAF). ChemicalBook+1

5. “Pharmacologic activity and pharmacokinetics of metabolites of Regorafenib in preclinical models.” Preclinical study detailing kinase inhibition by parent compound and metabolites, useful for in vitro biochemical and mechanistic research design. PubMed