Erlotinib

- Overview
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    Background
    
    Erlotinib (also known as NSC 718781 or CP 358,774) is a potent and orally-bioavailable inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase that selectively and reversibly inhibits EGFR-associated intracellular autophosphorylation of tyrosine kinase. Erlotinib inhibits purified EGFR tyrosine kinase and EGFR autophosphorylation intact cells with 50% inhibition concentration IC50 values of 2 nmol/L and 20 nmol/L respectively. Erlotinib competes for the ATP-binding sits on the intracellular domain of EGFR resulting in the inhibition of downstream signaling pathway involved in angiogenesis, cell propagation and cell survival. Erlotinib concentration-dependently inhibits EGFR-mediated propagation signals transduction, displays prominent anti-tumor activity against neoplasms harboring EGFR expression and exhibits a tolerable toxicologic profile.
- Properties
  - Alternative Name
    
    NSC 718781;OSI-744;R-1415;OSI744;OSI 744;R1415;R 1415; N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine
    
    CAS Number
    
    183321-74-6
    
    Molecular Formula
    
    C22H23N3O4
    
    Molecular Weight
    
    393.44
    
    Appearance
    
    A solid
    
    Purity
    
    99.33%
    
    Solubility
    
    insoluble in H2O; ≥19.65 mg/mL in DMSO; ≥30.27 mg/mL in EtOH with gentle warming
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Min P, Zhao S, et al. "MICAL-L2 potentiates Cdc42-dependent EGFR stability and promotes gastric cancer cell migration." J Cell Mol Med. 2019 Jun;23(6):4475-4488. PMID:31034158
    2. Shen M, Jiang YZ, et al. "Tinagl1 Suppresses Triple-Negative Breast Cancer Progression and Metastasis by Simultaneously Inhibiting Integrin/FAK and EGFR Signaling." Cancer Cell. 2019 Jan 14;35(1):64-80.e7. PMID:30612941
    3. Zheng J, Duan B, et al."Folliculin Interacts with Rab35 to Regulate EGF-Induced EGFR Degradation." Front Pharmacol. 2017 Sep 26;8:688. PMID:29018350
    4. Wang Y, Deng W, et al. "MICAL2 Promotes Breast Cancer Cell Migration by Maintaining EGFR Stability and EGFR/P38 Signaling Activation." Acta Physiol (Oxf). 2017 Jul 18. PMID:28719045
    5. Lee HS, Park SB, et al. "A novel HDAC inhibitor, CG200745, inhibits pancreatic cancer cell growth and overcomes gemcitabine resistance." Sci Rep. 2017 Jan 30;7:41615. PMID:28134290

Erlotinib

Background

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