Description

Product Description 

Imatinib Mesylate (CAS 220127-57-1) is a high-purity lyophilized powder widely utilized as a selective tyrosine kinase inhibitor, primarily targeting BCR-ABL, c-KIT, and PDGFR. As a first-generation small-molecule kinase inhibitor, Imatinib Mesylate has transformed research into chronic myeloid leukemia (CML) and gastrointestinal stromal tumors (GISTs). Its high specificity and reproducibility make it an indispensable tool for laboratory research, ranging from in vitro kinase profiling to in vivo translational studies.

Molecular Background and Scientific Significance

The discovery of Imatinib Mesylate revolutionized the understanding of tyrosine kinase-driven oncogenesis. BCR-ABL, generated by the t(9;22) chromosomal translocation, exhibits constitutive kinase activity, driving uncontrolled proliferation and survival of leukemic cells. Imatinib Mesylate binds the ATP-binding pocket of BCR-ABL in its inactive conformation, preventing autophosphorylation and downstream signaling. Beyond BCR-ABL, Imatinib Mesylate inhibits c-KIT and PDGFR, receptors critical in stem cell biology, hematopoiesis, and tumor angiogenesis.

Its utility in research extends to the study of apoptosis, cell cycle regulation, and mechanisms of drug resistance. By selectively inhibiting kinase activity, Imatinib Mesylate enables scientists to dissect signaling pathways with high precision, modeling disease progression and therapeutic interventions.

Research Applications

1. Kinase Profiling and Enzyme Kinetics

Imatinib Mesylate is a benchmark inhibitor in ATP-competitive kinase assays. Its lyophilized form allows long-term storage and reproducible performance. Researchers use Imatinib Mesylate to characterize enzyme kinetics, determine IC50 values, and compare inhibition across kinase families. This facilitates the validation of novel compounds and drug candidates in both academic and industrial settings.

2. Oncology Research

In leukemia and GIST models, Imatinib Mesylate is applied to investigate oncogenic signaling, proliferation, and apoptosis. Researchers assess the compound’s impact on leukemic stem cell survival, clonal expansion, and apoptotic induction. In GIST models, c-KIT inhibition by Imatinib Mesylate elucidates tumor dependency on receptor tyrosine kinases, supporting therapeutic modeling and resistance mechanism studies.

3. Signal Transduction Studies

By inhibiting downstream pathways such as MAPK/ERK, PI3K/AKT, and JAK/STAT, Imatinib Mesylate serves as a chemical probe for dissecting signal transduction cascades. It allows analysis of pathway crosstalk, feedback regulation, and compensatory mechanisms in kinase-driven cells. Researchers can explore gene expression changes, protein phosphorylation dynamics, and cellular responses in both normal and diseased cell lines.

4. Structural Biology and Computational Modeling

Imatinib Mesylate is widely used as a ligand in protein crystallography to understand kinase-ligand interactions. Computational modeling and molecular docking studies utilize Imatinib Mesylate to explore binding energy, conformational changes, and structure-activity relationships (SAR), providing insights for next-generation kinase inhibitor development.

5. Drug Resistance Mechanism Investigation

Resistance to kinase inhibitors often arises from point mutations in BCR-ABL or overactivation of compensatory pathways. Imatinib Mesylate facilitates the study of such mutations, supporting development of alternative strategies and combination therapies. Its consistent inhibitory profile makes it a valuable reference compound in evaluating secondary resistance mechanisms in vitro and in vivo.

6. Preclinical and Translational Models

In organoids, spheroids, and xenograft models, Imatinib Mesylate is used to assess tumor growth inhibition, angiogenesis suppression, and pathway modulation. Its application in pharmacokinetic/pharmacodynamic studies helps optimize dosage regimens and validate molecular targets for translational oncology research.

7. Cell Cycle and Apoptosis Research

Imatinib Mesylate induces cell cycle arrest and promotes apoptosis in kinase-dependent cells. Researchers employ flow cytometry, caspase assays, and western blotting to monitor effects of Imatinib Mesylate on cyclins, CDKs, and apoptotic markers. This provides mechanistic insights into therapeutic action and cellular responses to tyrosine kinase inhibition.

8. High-Throughput Screening (HTS) Applications

The compound is suitable for automated HTS platforms to evaluate combinatorial drug effects or to screen kinase inhibitors. Imatinib Mesylate provides a reference standard for assay calibration, quality control, and comparative analysis across multiple targets.

9. Translational and Personalized Medicine Research

Imatinib Mesylate is used to model patient-derived cells and evaluate individualized therapy responses. It allows scientists to investigate differential kinase dependence, resistance patterns, and the efficacy of experimental combinational treatments.

10. Toxicology and Safety Studies

Although not for clinical use, Imatinib Mesylate assists in studying cytotoxicity, off-target effects, and cellular stress responses, informing safer design of novel therapeutics.

Lyophilized Powder Advantages

• Enhanced stability for long-term storage

• Reduced degradation compared to solution forms

• Soluble in DMSO and compatible buffers

• Consistent batch-to-batch performance

• Optimal for high-throughput and long-term in vitro studies

Manufacturing and Quality Assurance

Produced in GMP-certified facilities, each batch of Imatinib Mesylate undergoes stringent quality control. Analytical verification includes HPLC, LC-MS, HRMS, and NMR. Certificates of Analysis (CoA) and safety data sheets (MSDS) accompany all shipments. Bulk production and factory customization ensure consistent quality and scalability for industrial and academic research purposes.

Product Specifications 

Mechanism of Action 

Imatinib Mesylate selectively inhibits ATP-binding sites of BCR-ABL, c-KIT, and PDGFR, stabilizing kinases in inactive conformations. This prevents phosphorylation of substrates, blocking downstream signal transduction and altering transcriptional programs.

BCR-ABL Inhibition

• Blocks autophosphorylation and substrate phosphorylation

• Suppresses MAPK/ERK, PI3K/AKT, and STAT5 pathways

• Induces apoptosis via mitochondrial pathways

c-KIT and PDGFR Inhibition

• Interferes with stem cell proliferation and differentiation

• Inhibits angiogenesis through VEGF and PDGF signaling

• Reduces tumor growth in GIST models

ATP-Competitive Mechanism

Imatinib Mesylate occupies the ATP-binding cleft, forming hydrogen bonds and hydrophobic interactions. Structural studies confirm that it locks kinases in inactive conformations, preventing substrate engagement.

Impact on Downstream Pathways

• Modulates transcription factors controlling cell cycle and apoptosis

• Alters expression of anti-apoptotic proteins (BCL-2, MCL-1)

• Activates caspases and promotes DNA fragmentation

Drug Resistance Studies

• Facilitates modeling of BCR-ABL mutations (T315I, E255K)

• Evaluates compensatory pathway activation

• Supports testing of second-generation inhibitors

Applications in Cell Biology

• Flow cytometry to monitor apoptosis and cell cycle

• Western blot and ELISA to assess protein phosphorylation

• Kinase profiling assays to determine selectivity

Preclinical Models

• Organoids, xenografts, and spheroids

• Pharmacokinetics and pharmacodynamics modeling

• Combined therapy evaluation

High-Throughput Screening

• Standard reference in automated kinase assays

• Assists in assay calibration and validation

• Supports structure-activity relationship studies
  

Side Effects 

Cellular Effects

• Apoptosis induction in BCR-ABL, c-KIT, PDGFR-dependent cells

• Growth inhibition in sensitive cell lines

• Off-target modulation of alternative pathways

Molecular Effects

• Caspase activation and mitochondrial depolarization

• Alteration of cyclin/CDK expression

• DNA fragmentation in apoptosis assays

Experimental Handling Considerations

• Use gloves, lab coat, and fume hood

• Avoid ingestion and inhalation

• Proper disposal according to institutional guidelines

Storage and Stability

• Lyophilized powder maintains activity at 2–8°C

• Protect from light and moisture

• Reconstitution in DMSO or compatible buffers for immediate use

Safety Precautions

• Follow local and national safety protocols

• Do not use in humans or animals

• Ensure training for laboratory personnel

Keywords

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Shipping Guarantee 

Our Imatinib Mesylate is shipped worldwide using cold-chain logistics to ensure product stability and bioactivity. Packaging includes insulated, moisture-proof containers with temperature monitoring. All shipments include tracking, insurance, and customs documentation for secure delivery. Bulk orders are packaged with reinforced insulation to maintain integrity throughout transit. Lyophilized Imatinib Mesylate maintains consistent activity and purity during shipping, enabling researchers to receive reliable, high-quality kinase inhibitor powder for large-scale laboratory and preclinical applications.

Trade Assurance 

Each batch of Imatinib Mesylate undergoes stringent quality control to ensure ≥99% purity, verified via HPLC, LC-MS, HRMS, and NMR. Certificates of Analysis (CoA) and MSDS accompany all shipments. Factory-direct supply, GMP-grade customization, and bulk production are available for research laboratories and industrial clients. Our trade assurance guarantees replacement or refund in case of inconsistencies, providing confidence in purchasing high-purity Imatinib Mesylate for kinase profiling, oncology research, and preclinical studies.

Payment Support 

We accept PayPal, credit cards, T/T bank transfers, USDT, Bitcoin, and Ethereum for all Imatinib Mesylate orders. Transactions are secure, encrypted, and verified for global clients. Flexible payment supports both small-scale research and bulk purchases. International customers can procure Imatinib Mesylate conveniently, ensuring timely access to high-purity kinase inhibitors for academic and industrial research applications, including large-scale preclinical studies and translational oncology projects.

Disclaimer 

Imatinib Mesylate is intended strictly for laboratory research purposes. It is not for human, veterinary, or clinical use. Researchers must adhere to institutional, local, and national safety regulations. Personal protective equipment (PPE) such as gloves, lab coats, and safety goggles is mandatory. Avoid ingestion, inhalation, or direct skin contact. Follow proper storage, handling, and disposal protocols. Imatinib Mesylate should only be used by trained personnel in appropriate laboratory facilities to ensure experimental integrity and safety.

References

1. PubChem: Imatinib Mesylate

2. ChEMBL: Imatinib

3. DrugBank: Imatinib

4. IUPHAR/BPS Guide: Imatinib

5. PubMed: Imatinib Mechanism