Gefitinib (ZD1839)

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    Gefitinib, also known as ZD1839 or Iressa, is a potent and orally-bioavailable small-molecule inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase with 50% inhibition concentration IC50 values of 0.033 μM and 0.027 μM in A431 membrane prep and baculovirus lysate respectively. Gefitinib binds to the kinase ATP binding site of EGFR interfering with the binding of adenosine triphosphate, which suppresses the EGFR tyrosine kinase activity and resultant signal transduction of EGFR. Gefitinib exhibits anti-angiogenic activities in a wide range of human tumor types, including head and neck, prostate, breast, ovarian, colon, small-cell lung and non-small-cell lung cancer. Moreover, geftinib has also been found to reduce proliferation, induce cell cycle arrest and increase apoptosis.
- Properties
  - Alternative Name
    
    Iressa, ZD-1839, Gefitinib; N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine
    
    CAS Number
    
    184475-35-2
    
    Molecular Formula
    
    C22H24ClFN4O3
    
    Molecular Weight
    
    446.90
    
    Appearance
    
    A solid
    
    Purity
    
    99.26%
    
    Solubility
    
    ≥22.34 mg/mL in DMSO; insoluble in H2O; ≥2.48 mg/mL in EtOH with ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Priscilla Cheung, Jordi Xiol, et al. "Regenerative Reprogramming of the Intestinal Stem Cell State via Hippo Signaling Suppresses Metastatic Colorectal Cancer." Cell Stem Cell. 2020 Oct 1;27(4):590-604.e9. PMID:32730753
    2. Lina Zhao, Ting Qiu, et al. "SGCE Promotes Breast Cancer Stem Cells by Stabilizing EGFR." Adv Sci (Weinh). 2020 Jun 8;7(14):1903700. PMID:32714745
    3. Lee YC, Wang LJ, et al. "Inhibition of EGFR pathway promotes the cytotoxicity of ABT-263 in human leukemia K562 cells by blocking MCL1 upregulation." Biochem Pharmacol. 2020;178:114047. PMID:32446890
    4. 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
    5. She K, Fang S, et al. "SCD1 is required for EGFR-targeting cancer therapy of lung cancer via re-activation of EGFR/PI3K/AKT signals." Cancer Cell Int. 2019 Apr 18;19:103. PMID:31019378
    6. Chen Z, Tian D, et al. "Apigenin Combined With Gefitinib Blocks Autophagy Flux and Induces Apoptotic Cell Death Through Inhibition of HIF-1α, c-Myc, p-EGFR, and Glucose Metabolism in EGFR L858R+T790M-Mutated H1975 Cells." Front Pharmacol. 2019 Mar 22;10:260. PMID:30967777
    7. Huang SZ, Wei MN, et al. "Targeting TF-AKT/ERK-EGFR Pathway Suppresses the Growth of Hepatocellular Carcinoma." Front Oncol. 2019 Mar 15;9:150. PMID:30931258
    8. Hu WT, Yeh CC, et al. "The O-glycosylating enzyme GALNT2 suppresses the malignancy of gastric adenocarcinoma by reducing EGFR activities." Am J Cancer Res. 2018 Sep 1;8(9):1739-1751. PMID:30323967
    9. 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
    10. Shih CH, Chang YJ, et al. "EZH2-mediated upregulation of ROS1 oncogene promotes oral cancer metastasis." Oncogene. 2017 Nov 23;36(47):6542-6554. PMID:28759046

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Gefitinib (ZD1839)

Background

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