Description

Product Description

Gefitinib (CAS 184475-35-2) is a small-molecule anilinoquinazoline derivative that acts as a reversible inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. By targeting the ATP-binding site of EGFR, Gefitinib suppresses receptor autophosphorylation, thereby inhibiting downstream signaling pathways such as RAS-RAF-MEK-ERK and PI3K-AKT, which regulate cell proliferation, survival, and apoptosis.

Physical and Chemical Properties:

• Molecular formula: C22H24ClFN4O3

• Molecular weight: 446.9 g/mol

• Appearance: White to off-white crystalline powder

• Solubility: Soluble in DMSO, ethanol; low aqueous solubility

• Stability: Stable at 2–8 °C; protect from light and moisture

Research Applications:

1. EGFR Signaling Studies: Gefitinib is extensively used to study EGFR phosphorylation, receptor internalization, and downstream signaling in cancer cell lines.

2. Antiproliferative Assays: Blocks proliferation of EGFR-dependent tumor cells; ideal for in vitro growth inhibition studies.

3. Apoptosis Research: Induces caspase-mediated apoptosis via inhibition of survival pathways (PI3K-AKT, ERK).

4. Drug Resistance Mechanisms: Useful for investigating acquired resistance, EGFR mutations (L858R, T790M), and compensatory pathway activation.

5. Combination Therapy Modeling: Evaluates synergy with other kinase inhibitors, chemotherapy agents, or immunomodulators.

6. Animal Models: Employed in murine xenografts and in vivo pharmacokinetic/pharmacodynamic studies.

7. Molecular Mechanistic Research: Studies EGFR internalization, ubiquitination, and feedback loop regulation, as well as crosstalk with other receptor tyrosine kinases.

Experimental Considerations:

• Handling: Powder should be managed with gloves, lab coat, and eye protection.

• Dosing: Concentration ranges depend on cell type and intended pathway inhibition.

• Solvent Compatibility: Dissolve in DMSO or ethanol prior to dilution in culture medium; verify solubility for experimental conditions.

• Storage: Store at 2–8 °C; avoid repeated freeze-thaw cycles to preserve chemical stability.

Gefitinib’s selective EGFR inhibition, high purity (≥99%), and well-characterized molecular mechanism make it an indispensable tool for research in targeted cancer therapy, receptor signaling, apoptosis, and drug resistance studies.

Product Specifications

Mechanism of Action

Gefitinib is a selective inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. It binds reversibly to the ATP-binding site of the EGFR intracellular domain, preventing autophosphorylation and subsequent activation of downstream signaling pathways.

Key Molecular Mechanisms:

1. EGFR Inhibition: Blocks receptor tyrosine kinase activity, suppressing phosphorylation at critical tyrosine residues (Tyr1068, Tyr1173) on EGFR.

2. Downstream Signaling Suppression: Inhibits the RAS-RAF-MEK-ERK and PI3K-AKT-mTOR pathways, which regulate cell proliferation, survival, and apoptosis.

3. Apoptosis Induction: Interruption of survival pathways leads to activation of caspases, mitochondrial depolarization, and Bcl-2 family modulation.

4. Cell Cycle Modulation: Gefitinib causes G1-phase arrest by downregulating cyclin D1 and CDK4/6, contributing to antiproliferative effects.

5. Drug Resistance Studies: Serves as a model for analyzing resistance mechanisms, including EGFR mutations (L858R, T790M) and compensatory pathway activation (MET, HER2, AXL).

Experimental Applications:

• In vitro: Assess EGFR phosphorylation, cell viability, apoptosis, signaling pathway modulation, and combination effects with other kinase inhibitors or chemotherapy agents.

• In vivo: Xenograft tumor models, pharmacokinetic/pharmacodynamic studies, and evaluation of tumor growth inhibition.

• Mechanistic Studies: Investigate receptor internalization, ubiquitination, feedback loops, and cross-talk with other receptor tyrosine kinases for pathway analysis.

Gefitinib’s selective EGFR inhibition and well-characterized molecular effects make it an indispensable tool in preclinical studies of receptor-mediated signaling, apoptosis, and targeted cancer therapy.

Side Effects

Gefitinib is a research-grade compound. Laboratory handling requires caution:

• Cytotoxicity: In vitro studies may show apoptosis, growth arrest, and reduced proliferation in EGFR-dependent and sensitive cell lines.

• Immune Modulation: Can indirectly influence cytokine production in some cell models.

• Handling Precautions:

  • Wear gloves, lab coat, and eye protection.

  • Handle in a fume hood to prevent inhalation.

• Storage: Keep at 2–8 °C; protect from light and moisture. Avoid repeated freeze-thaw cycles.

• Environmental Precautions: Dispose of contaminated materials according to biosafety protocols.

Experimental Observations:

• In vitro: Reduced EGFR phosphorylation, apoptosis induction, cell cycle arrest.

• In vivo: Tumor growth inhibition, signaling pathway modulation, pharmacokinetic effects.

Keywords

Gefitinib, CAS 184475-35-2, EGFR inhibitor, tyrosine kinase inhibitor, anticancer research, molecular targeted therapy, apoptosis induction, cell cycle arrest, RAS-RAF-MEK-ERK, PI3K-AKT, high purity, ≥99% purity, factory peptide/small-molecule supplier, peptide wholesale China, China peptide manufacturer, OEM & bulk peptide production.

Shipping Guarantee

All Gefitinib Tablets shipments of Gefitinib are handled via validated cold-chain logistics to maintain chemical stability. The powder is sealed in moisture-proof, light-protected containers with secondary packaging. Full tracking, insurance coverage, and international courier support are provided to ensure secure delivery.

Trade Assurance

Gefitinib authenticity is guaranteed, with ≥99% purity verified by HPLC, MS, and NMR. Each batch includes a Certificate of Analysis (CoA). Trade assurance covers replacement or refund for deviations from specifications, ensuring consistent high-purity product for preclinical research.

Payment Support

Secure global payment options: PayPal, major credit cards (Visa, MasterCard, American Express), telegraphic transfer (T/T), and cryptocurrencies (USDT, Bitcoin, Ethereum). All transactions are encrypted and verified for confidentiality and fund protection.

Disclaimer

This Gefitinib Tablets product is intended for laboratory research use only. It is not for human or veterinary administration. Researchers must follow institutional safety protocols. Data generated with Gefitinib should not be interpreted as clinical or therapeutic guidance.

References

1. PubChem: Gefitinib (CID 123631) ↗

2. ChEMBL: Gefitinib Bioactivity (ChEMBL ID CHEMBL190837) ↗

3. DrugBank: Gefitinib – DB01259 ↗

4. PubMed ID 12452916 – Gefitinib mechanism and preclinical evaluation ↗

5. IUPHAR/BPS Guide to Pharmacology: EGFR inhibitors ↗