Description

Product Description

Erlotinib Hydrochloride (CAS 183319-69-9) is a potent and selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, widely used in preclinical molecular oncology, pharmacology, and cell biology research. As an anilinoquinazoline derivative, it binds competitively to the ATP-binding domain of EGFR, preventing receptor autophosphorylation and downstream signaling. Its research-grade powder form ensures precise dosing for in vitro and in vivo preclinical models, enabling reproducible investigation of EGFR-dependent cellular processes, apoptosis, proliferation inhibition, epithelial–mesenchymal transition (EMT), and drug resistance.

Mechanistic Overview

Erlotinib Hydrochloride inhibits EGFR-mediated signaling pathways:

• RAS/RAF/MEK/ERK Pathway – blocks cell proliferation

• PI3K/AKT/mTOR Pathway – reduces cell survival and sensitizes to apoptosis

• JAK/STAT Pathway – decreases transcription of pro-survival genes

• EMT Regulatory Networks – inhibits migration and invasion potential

These effects contribute to apoptosis induction, G1-phase cell-cycle arrest, suppression of metastatic phenotypes, and enhanced sensitivity to combination therapies.

Preclinical Applications

Erlotinib Hydrochloride powder is widely employed in:

1. EGFR-Dependent Tumor Growth Inhibition – lung, pancreatic, head and neck cancer models

2. Combination Therapy Evaluation – with chemotherapeutics, kinase inhibitors, PARP inhibitors, or immunomodulatory agents

3. Drug Resistance Modeling – T790M mutations, MET amplification, HER2 or AXL overexpression, EMT-mediated adaptive resistance

4. Apoptosis and Cell-Cycle Mechanistic Studies – caspase activation, mitochondrial depolarization, ROS generation, cyclin/CDK regulation

5. Pathway Crosstalk and Biomarker Validation – EGFR, PI3K/AKT/mTOR, MAPK, JAK/STAT interactions

6. In Vivo Xenograft Models – pharmacokinetic/pharmacodynamic evaluation and tumor growth inhibition

Its Erlotinib Hydrochloride powder form offers chemical stability, precise concentration preparation, and compatibility with multiple solvents (DMSO, ethanol, methanol), facilitating reproducible experimental outcomes.

Product Specifications

Mechanism of Action

EGFR Tyrosine Kinase Inhibition

• Competitive binding to ATP-binding pocket of EGFR

• Prevents receptor autophosphorylation

• Suppresses downstream signaling: RAS/RAF/MEK/ERK, PI3K/AKT/mTOR, JAK/STAT

Apoptosis Induction

• Mitochondrial depolarization and cytochrome c release

• Caspase-3 and -9 activation

• ROS generation contributing to oxidative stress

• Downregulation of anti-apoptotic proteins (BCL-2, survivin)

• p53-dependent and independent apoptosis pathways

Cell-Cycle Arrest

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

• Rb hypophosphorylation leading to E2F inactivation

• Inhibition of DNA replication initiation

EMT and Migration Inhibition

• Upregulation of E-cadherin

• Downregulation of N-cadherin and vimentin

• Inhibition of FAK/AKT signaling

• Suppression of integrin-mediated adhesion and motility

Resistance Mechanisms

• EGFR T790M mutation

• MET amplification

• HER2 or AXL overexpression

• EMT-mediated adaptive resistance

• KRAS/NRAS feedback loops

Combination Therapy Applications

• Chemotherapeutics: cisplatin, gemcitabine, paclitaxel

• Targeted inhibitors: MET, ALK, PI3K/AKT inhibitors

• DNA damage response modulators: PARP inhibitors, CHK1/2 inhibitors

• Immunomodulatory agents

  

Erlotinib Hydrochloride Side Effects (Preclinical Observations)

Cellular Effects

• Inhibition of EGFR phosphorylation

• G1-phase cell-cycle arrest

• DNA damage and replication stress

• ROS-mediated oxidative stress

Apoptotic Effects

• Caspase-dependent mitochondrial apoptosis

• p53-dependent and independent cell death

• Membrane blebbing and nuclear condensation

Laboratory Handling

• Handle with PPE in a fume hood

• Avoid inhalation, ingestion, or skin contact

• Dispose of waste according to institutional safety protocols

Keywords

Erlotinib Hydrochloride, EGFR inhibitor, Erlotinib powder, EGFR signaling inhibitor, apoptosis research, tyrosine kinase inhibitor, cancer signaling research, Erlotinib bulk powder, proliferation inhibition, oncogenic EGFR models, targeted therapy research compound, laboratory research reagent.

Shipping Guarantee

All Erlotinib Hydrochloride shipments of Erlotinib Hydrochloride powder are packaged with moisture-resistant material and temperature-stable logistics. International express shipping with tracking and insurance ensures compound integrity.

Trade Assurance

• ≥99% purity verified by HPLC, MS, NMR

• Certificate of Analysis (CoA) included for each batch

• Replacement or refund provided for deviations from listed specifications

Payment Support

Global options:

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• T/T bank transfer

• USDT / Bitcoin / Ethereum

All transactions are encrypted and secure.

Disclaimer

Erlotinib Hydrochloride (CAS 183319-69-9) is provided strictly for laboratory research purposes only. It is not intended for human or veterinary use, clinical applications, or diagnostic purposes. Handle only in qualified laboratories following institutional safety guidelines. The supplier assumes no responsibility for misuse.

References 

• PubChem – Erlotinib Hydrochloride (CID 176870)

• ChEMBL – Erlotinib Bioactivity Data (CHEMBL120098)

• DrugBank – Erlotinib (DB00530)

• PubMed – EGFR inhibition and apoptosis studies

• IUPHAR/BPS Guide to Pharmacology – EGFR inhibitors