Description

Product Description

Afatinib Dimaleate (CAS 850140-73-7) is a highly selective, irreversible inhibitor of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2) tyrosine kinases. By forming covalent bonds with the kinase domain, Afatinib irreversibly inhibits receptor phosphorylation and downstream signaling, providing a valuable tool for mechanistic studies in oncology, cell signaling, and drug resistance research.

In preclinical research, Afatinib is employed to dissect signaling pathways mediated by EGFR/HER2 in cancer cell lines and animal models. Its irreversible binding to cysteine residues within the ATP-binding site blocks autophosphorylation, suppresses MAPK, PI3K/AKT, and JAK/STAT pathways, and prevents proliferation of receptor-dependent cells. This selective inhibition is particularly valuable for exploring mechanisms of acquired resistance in models of non-small cell lung cancer (NSCLC) and other EGFR/HER2-driven malignancies.

Afatinib Dimaleate exhibits high selectivity for EGFR family receptors while minimizing off-target kinase interactions. Its pharmacological profile allows researchers to study:

• Signal transduction cascades downstream of EGFR and HER2.

• Molecular mechanisms of tyrosine kinase inhibitor resistance, including gatekeeper mutations.

• Crosstalk between receptor tyrosine kinases and downstream transcription factors.

• Cellular proliferation, apoptosis, and tumorigenic potential in preclinical models.

Supplied as a white to off-white crystalline powder with ≥99% purity, Afatinib Dimaleate is highly stable under refrigerated conditions (2–8 °C). It is soluble in DMSO, ethanol, and methanol, making it suitable for in vitro and in vivo studies. Quality assurance is confirmed by HPLC, MS, and NMR, ensuring batch-to-batch consistency.

In addition to oncology research, Afatinib Dimaleate serves as a mechanistic probe for investigating receptor tyrosine kinase interactions, downstream signaling modulation, and molecular adaptation in both normal and malignant cellular systems. Its covalent and irreversible mode of inhibition provides durable receptor blockade, enabling time-course studies and combination experiments with other targeted therapies.

The compound’s utility extends to preclinical evaluation of novel therapeutic combinations, receptor-targeted drug discovery, and validation of computational models of kinase-inhibitor interactions. Researchers can assess receptor occupancy, downstream phosphorylation kinetics, and compensatory pathway activation in response to prolonged inhibition.

Overall, Afatinib Dimaleate is a reliable and reproducible reagent for studies involving EGFR/HER2 signaling, kinase biology, drug resistance, and cancer pharmacology, providing mechanistic insights that support translational research initiatives.

Product Specifications 

Mechanism of Action

Afatinib Dimaleate functions as an irreversible tyrosine kinase inhibitor targeting EGFR (ErbB1) and HER2 (ErbB2). It covalently binds to cysteine residues in the ATP-binding pocket of these receptors, blocking autophosphorylation and downstream signaling cascades.

Inhibition of EGFR/HER2 disrupts multiple pathways, including MAPK, PI3K/AKT, and JAK/STAT, reducing cellular proliferation, promoting apoptosis, and modulating gene expression in receptor-dependent cells. Researchers use Afatinib to study mechanisms of receptor-driven tumorigenesis, acquired resistance mutations (e.g., T790M in EGFR), and compensatory signaling networks.

Preclinical models benefit from Afatinib’s selectivity, allowing precise analysis of receptor biology, downstream signaling, and combination therapy effects. Its irreversible binding provides durable inhibition, facilitating time-course and mechanistic studies.

Side Effects

For laboratory use, handle Afatinib with standard safety precautions:

• Avoid inhalation, ingestion, and skin or eye contact.

• Wear gloves, lab coat, and protective eyewear.

• Conduct experiments in a well-ventilated fume hood.

• Dispose of waste according to institutional safety protocols.

Observed experimental effects may include alterations in cell proliferation, apoptosis, or receptor signaling in in vitro or in vivo models. This product is strictly for laboratory research use only.

Keywords

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Shipping Guarantee

All Afatinib Dimaleate shipments are managed using validated cold-chain logistics to preserve compound integrity. Each order is sealed in moisture-proof, light-protected containers with secondary protective wrapping. Real-time temperature monitoring ensures stability during transit. Packages are shipped via international express couriers with full tracking and insurance coverage.

Trade Assurance

We Afatinib Dimaleate guarantee product authenticity and analytical verification via HPLC, MS, and NMR. Each batch comes with a Certificate of Analysis (CoA) confirming ≥99% purity. Trade assurance includes replacement or refund for any deviation from listed specifications, ensuring consistent quality for reproducible research.

Payment Support

Flexible and secure payment options include PayPal, major credit cards (Visa, MasterCard, American Express), telegraphic transfer (T/T), and cryptocurrencies (USDT, Bitcoin, Ethereum). All transactions are protected with advanced encryption and verified gateways.

Disclaimer

This Afatinib Dimaleate product is intended for laboratory research use only. It is not for human or veterinary administration. All researchers must follow proper safety protocols when handling bioactive compounds. Data obtained with Afatinib should not be interpreted as clinical evidence or therapeutic guidance.