Erlotinib Hydrochloride

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    Erlotinib hydrochloride (the trade name Tarceva?) is a directly acting inhibitor of epidermal growth factor receptor (EGFR/HER-1) tyrosine kinase with an IC50 of 2 nM.
    Epidermal growth factor receptor (EGFR) is one member of the ErbB family which includes EGFR (ErbB1), ErbB2, ErbB3 and ErbB4. The activation of EGFR is dependent on the binding of peptide growth factors to the receptor. In many carcinomas, the presence of EGFR mutation leads to the activation of EGFP, which causes cell proliferation and other cancer processes [1].
    Selective inhibition of EGFR tyrosine kinase by erlotinib hydrochloride leads to the disruption of cancer growth and development which include cell migration, proliferation, angiogenesis, and apoptosis. For instance, erlotinib hydrochloride was shown to induce cell apoptosis and G0/G1 cell cycle arrest in hepatocellular cancer cells, Bxpc-3 and PANC-1 cells, thereby enhancing chemosensitivity towards cytostatics [2, 3].
    In addition, this product is widely researched and used for the treatment of human advanced non-small cell lung cancer (NSCLC) [4]. In pancreatic cancer, erlotinib hydrochloride was also reported to exhibit an anti-tumour effect [5].
    
    1. Melosky B. Review of EGFR TKIs in Metastatic NSCLC, Including Ongoing Trials. Front Oncol 2014,4:244.
    2. Zheng YT, Yang HY, Li T, Zhao B, Shao TF, Xiang XQ, et al. Amiloride sensitizes human pancreatic cancer cells to erlotinib in vitro through inhibition of the PI3K/AKT signaling pathway. Acta Pharmacol Sin 2015,36:614-626.
    3. Huether A, Hopfner M, Sutter AP, Schuppan D, Scherubl H. Erlotinib induces cell cycle arrest and apoptosis in hepatocellular cancer cells and enhances chemosensitivity towards cytostatics. J Hepatol 2005,43:661-669.
    4. Singh N, Jindal A, Behera D. Erlotinib usage after prior treatment with gefitinib in advanced non-small cell lung cancer: A clinical perspective and review of published literature. World J Clin Oncol 2014,5:858-864.
    5. Renouf DJ, Tang PA, Hedley D, Chen E, Kamel-Reid S, Tsao MS, et al. A phase II study of erlotinib in gemcitabine refractory advanced pancreatic cancer. Eur J Cancer 2014,50:1909-1915.
- Properties
  - Alternative Name
    
    Tarceva; CP-358774; OSI-774; NSC 718781; N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine;hydrochloride
    
    CAS Number
    
    183319-69-9
    
    Molecular Formula
    
    C22H24ClN3O4
    
    Molecular Weight
    
    429.91
    
    Appearance
    
    A solid
    
    Purity
    
    99.20%
    
    Solubility
    
    insoluble in H2O; insoluble in EtOH; ≥6.44 mg/mL in DMSO with gentle warming
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Panagi I, Jennings E, et al. "Salmonella Effector SteE Converts the Mammalian Serine/Threonine Kinase GSK3 into a Tyrosine Kinase to Direct Macrophage Polarization." Cell Host Microbe. 2020;27(1):41–53.e6. PMID:31862381
    2. White SM, Avantaggiati ML, et al. "YAP/TAZ Inhibition Induces Metabolic and Signaling Rewiring Resulting in Targetable Vulnerabilities in NF2-Deficient Tumor Cells." Dev Cell. 2019 May 6;49(3):425-443.e9. PMID:31063758
    3. Cheriyan VT, Alsaab H, et al. "A CARP-1 functional mimetic compound is synergistic with BRAF-targeting in non-small cell lung cancers." Oncotarget. 2018 Jul 3;9(51):29680-29697. PMID:30038713
    4. Deng W, Gu L, et al. "CD24 associates with EGFR and supports EGF/EGFR signaling via RhoA in gastric cancer cells." J Transl Med. 2016 Feb 1;14:32. PMID:26830684

We Also Recommend

Embelin

$204

Embelin

$180

Regorafenib

$212

SKLB610

$241

Erlotinib Hydrochloride

Background

We Also Recommend

Embelin

Embelin

Regorafenib

SKLB610