Description

Product Overview

Erlotinib Hydrochloride is a highly selective EGFR inhibitor designed for research applications in oncology. Structurally, it belongs to the anilinoquinazoline class and exerts its activity by binding competitively to the ATP-binding pocket of EGFR. This binding prevents autophosphorylation of the receptor, subsequently downregulating multiple downstream signaling pathways responsible for cell proliferation, survival, migration, and invasion.

Supplied as a high-purity powder, Erlotinib Hydrochloride allows precise dosing for in vitro assays and in vivo preclinical studies. The availability of factory low-cost customization ensures that research laboratories can access large quantities for high-throughput studies and long-term projects without compromising quality.

Mechanistic Insights

EGFR Signaling Interference

• ATP-Competitive Binding: Erlotinib binds to the EGFR kinase domain, blocking autophosphorylation.

• MAPK/ERK Pathway Modulation: Downregulates cyclin D1 expression, reducing proliferation.

• PI3K/AKT/mTOR Suppression: Attenuates survival signals, sensitizing cells to apoptosis.

• STAT3 Inhibition: Reduces transcription of genes involved in survival and inflammation.

Induction of Apoptosis

• Promotes mitochondrial depolarization and cytochrome c release.

• Activates intrinsic caspase cascade (caspase-3 and -9).

• Increases reactive oxygen species (ROS), triggering oxidative stress-mediated cell death.

• Downregulates anti-apoptotic proteins, including BCL-2 and survivin.

Cell-Cycle and Proliferation Effects

• G1-phase arrest through suppression of cyclin D1/CDK4/6.

• Retinoblastoma protein (Rb) hypophosphorylation, preventing E2F-mediated S-phase entry.

• Inhibits DNA replication initiation, contributing to growth suppression.

Epithelial-Mesenchymal Transition (EMT) Inhibition

• Enhances E-cadherin expression while reducing N-cadherin and vimentin.

• Limits migration and invasion via FAK/AKT signaling inhibition.

• Reduces integrin-mediated adhesion dynamics.

Drug Resistance Exploration

• Useful for studying T790M EGFR mutation-mediated resistance.

• Evaluates MET amplification, HER2, and AXL overexpression effects.

• Examines EMT-related adaptive mechanisms.

• Supports combination therapy evaluation to overcome resistance.

Preclinical Applications

Erlotinib Hydrochloride powder is widely utilized in the following research areas:

1. EGFR-Dependent Tumor Model Studies: Lung adenocarcinoma, pancreatic, head and neck cancers.

2. Combination Therapy Research: With chemotherapeutics, targeted inhibitors, PARP inhibitors, or immunotherapy agents.

3. Resistance Mechanism Analysis: T790M mutation, MET/HER2 amplification, and EMT-mediated adaptive resistance.

4. Cell-Cycle & Apoptosis Studies: Caspase activation, mitochondrial depolarization, ROS induction, cyclin/CDK modulation.

5. Signal Crosstalk Investigation: Interaction of EGFR with PI3K/AKT/mTOR, MAPK, and JAK/STAT pathways.

6. In Vivo Pharmacology Studies: Xenograft models for tumor growth inhibition, PK/PD evaluation.

7. Factory Low-Cost Customization: Bulk supply with verified batch-to-batch consistency, enabling cost-efficient research scalability.

Product Specifications

Side Effects (Preclinical Observations)

Cellular Effects:

• EGFR phosphorylation inhibition

• G1-phase cell-cycle arrest

• DNA damage accumulation

• ROS-mediated oxidative stress

Apoptotic Effects:

• Caspase-3/-9 mediated mitochondrial apoptosis

• p53-dependent and independent pathways

• Nuclear condensation and membrane blebbing

Laboratory Handling:

• Use PPE and work in fume hood

• Avoid skin contact, inhalation, ingestion

• Dispose according to safety regulations

Keywords

Erlotinib Hydrochloride, EGFR inhibitor, Erlotinib powder, factory low-cost customization, apoptosis research, tyrosine kinase inhibitor, targeted therapy research compound, proliferation inhibition, EMT studies, drug resistance modeling, bulk powder, laboratory research reagent.

Shipping Guarantee

All shipments packaged with moisture-proof and temperature-controlled materials. International express shipping with tracking and insurance maintains compound integrity.

Trade Assurance

• ≥99% purity confirmed via HPLC, MS, NMR

• CoA provided for every batch

• Replacement or refund in case of specification deviation

Payment Support

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Disclaimer

Erlotinib Hydrochloride (CAS 183319-69-9) is for laboratory research only. Not intended for human or veterinary use, clinical application, or diagnostics. Handle in qualified laboratories under safety guidelines. Supplier assumes no liability for misuse.

References (Clickable)

• PubChem – Erlotinib Hydrochloride (CID 176870)

• ChEMBL – Erlotinib Bioactivity (CHEMBL120098)

• DrugBank – Erlotinib (DB00530)

• PubMed – EGFR inhibition and apoptosis

• IUPHAR/BPS Guide – EGFR inhibitors