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Iressa

Catalog #: 3000
21 Citations Datasheet / COA / SDS
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Iressa | CAS No. 184475-35-2 | EGF Receptor Inhibitors
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Description: Orally active, selective EGFR inhibitor
Alternative Names: Gefitinib,ZD 1839

Chemical Name: N-(3-Chloro-4-fluorophenyl)-7-methoxy-6-[3-(4-morpholinyl)propoxy]-4-quinazolinamine

Purity: ≥98%

Product Details
Citations (21)
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Reviews
Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

Iressa is an orally active, selective inhibitor of EGFR tyrosine kinase (IC50 = 23 - 79 nM). Shows minimal activity against ErbB2, KDR, c-flt, PKC, MEK and ERK-2. Blocks EGFR autophosphorylation and inhibits tumor growth in mice bearing a range of human xenografts. Also inhibits growth of brain metastases in mouse model of non-small cell lung cancer.

View information regarding the usage of Iressa for non-clinical studies.

Technical Data

M.Wt:
446.9
Formula:
C22H24ClFN4O3
Solubility:
Soluble to 100 mM in DMSO and to 10 mM in ethanol
Purity:
≥98%
Storage:
Store at RT
CAS No:
184475-35-2

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
Sold for research purposes only under agreement from AstraZeneca
Other Product-Specific Information:

Background References

  1. Acquired resistance to anti-EGFR mAb ICR62 in cancer cells is accompanied by an increased EGFR expression, HER-2/HER-3 signalling and sensitivity to pan HER blockers.
    Khelwatty S, Essapen S, Seddon A, Fan Z, Modjtahedi H
    Br J Cancer, 2015;113(7):1010-9.
  2. Hematopoietic stem cell cytokines and fibroblast growth factor-2 stimulate human endothelial cell-pericyte tube co-assembly in 3D fibrin matrices under serum-free defined conditions.
    Smith A, Bowers S, Stratman A, Davis G
    PLoS ONE, 2013;8(12):e85147.
  3. CD200-positive cancer associated fibroblasts augment the sensitivity of Epidermal Growth Factor Receptor mutation-positive lung adenocarcinomas to EGFR Tyrosine kinase inhibitors
    M Ishibashi, S Neri, H Hashimoto, T Miyashita, T Yoshida, Y Nakamura, H Udagawa, K Kirita, S Matsumoto, S Umemura, K Yoh, S Niho, M Tsuboi, K Masutomi, K Goto, A Ochiai, G Ishii
    Sci Rep, 2017;7(0):46662.
  4. Promoter hypomethylation of EpCAM-regulated bone morphogenetic protein gene family in recurrent endometrial cancer.
    Hsu Y, Gu F, Huang Y, Liu J, Ruan J, Huang R, Wang C, Chen C, Jadhav R, Lai H, Mutch D, Goodfellow P, Thompson I, Kirma N, Huang T
    Clin Cancer Res, 2013;19(22):6272-85.
  5. The multi-targeted tyrosine kinase inhibitor vandetanib plays a bifunctional role in non-small cell lung cancer cells.
    Zhou, Yan, Zhang, Yuanlian, Zou, Hanbing, Cai, Ning, Chen, Xiaojing, Xu, Longmei, Kong, Xianming, Liu, Peifeng
    Sci Rep, 2015;5(0):8629.
  6. IL-17E synergizes with EGF and confers in vitro resistance to EGFR-targeted therapies in TNBC cells
    Y Merrouche, J Fabre, H Cure, C Garbar, C Fuselier, J Bastid, F Antonicell, R Al-Daccak, A Bensussan, J Giustinian
    Oncotarget, 2016;7(33):53350-53361.
  7. Synergistic effects of various Her inhibitors in combination with IGF-1R, C-MET and Src targeting agents in breast cancer cell lines
    A Stanley, GH Ashrafi, AM Seddon, H Modjtahedi
    Sci Rep, 2017;7(1):3964.
  8. Antitumor effect and potentiation of cytotoxic drugs activity in human cancer cells by ZD-1839 (Iressa), an epidermal growth factor receptor-selective tyrosine kinase inhibitor.
    Ciardiello et al.
    Clin.Cancer Res., 2000;6:2053
  9. ZD1839 ('Iressa'), as an anticancer agent.
    Baselga et al.
    Drugs, 2000;60:33
  10. Tumor penetration of gefi. (Iressa), an epidermal growth factor receptor tyrosine kinase inhibitor.
    McKillop et al.
    Mol.Cancer Ther., 2005;4:641
  11. Tyrosine kinase inhibitors show different anti-brain metastases efficacy in NSCLC: A direct comparative analysis of icotinib, gefitinib, and erlo. in a nude mouse model.
    Tan et al.
    Oncotarget., 2017;8:98771

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Citations for Iressa

The citations listed below are publications that use Tocris products. Selected citations for Iressa include:

21 Citations: Showing 1 - 10

  1. Epidermal growth factor receptor promotes glioma progression by regulating xCT and GluN2B-containing N-methyl-d-aspartate-sensitive glutamate receptor signaling.
    Authors: Suina Et al.
    Cancer Sci  2018;109:3874
  2. Drug resistance originating from a TGF-β/FGF-2-driven epithelial-to-mesenchymal transition and its reversion in human lung adenocarcinoma cell lines harboring an EGFR mutation.
    Authors: Kurimoto Et al.
    Oncol Rep  2016;48:1825
  3. Anticancer Effects of Paris Saponins by Apoptosis and PI3K/AKT Pathway in Gefitinib-Resistant Non-Small Cell Lung Cancer.
    Authors: Zhu Et al.
    Med Sci Monit  2016;22:1435
  4. Combined EGFR- and notch inhibition display additive inhibitory effect on glioblastoma cell viability and glioblastoma-induced endothelial cell sprouting in vitro.
    Authors: Staberg Et al.
    Cancer Cell Int  2016;16:34
  5. Architecture of Chimeric Spheroids Controls Drug Transport.
    Authors: Curran Et al.
    Cancer Microenviron  2015;8:101
  6. ANO1 interacts with EGFR and correlates with sensitivity to EGFR-targeting therapy in head and neck cancer.
    Authors: Bill Et al.
    PLoS One  2015;6:9173
  7. MetF. attenuates gefitinib-induced exacerbation of pulmonary fibrosis by inhibition of TGF-β signaling pathway.
    Authors: Li Et al.
    Oncotarget  2015;6:43605
  8. Monocyte-Induced Prostate Cancer Cell Invasion is Mediated by Chemokine ligand 2 and Nuclear Factor-κB Activity.
    Authors: Lindholm Et al.
    J Clin Cell Immunol  2015;6
  9. CI-988 Inhibits EGFR Transactivation and Proliferation Caused by Addition of CCK/Gastrin to Lung Cancer Cells.
    Authors: Moody Et al.
    J Mol Neurosci  2015;56:663
  10. Ad-p53 enhances the sensitivity of triple-negative breast cancer MDA-MB-468 cells to the EGFR inhibitor gefi.
    Authors: Wang Et al.
    Oncotarget  2015;33:526
  11. An Inducible TGF-β2-TGFβR Pathway Modulates the Sensitivity of HNSCC Cells to Tyrosine Kinase Inhibitors Targeting Dominant Receptor Tyrosine Kinases.
    Authors: Kleczko Et al.
    Life Sci  2015;10:e0123600
  12. Gefitinib and luteolin cause growth arrest of human prostate cancer PC-3 cells via inhibition of cyclin G-associated kinase and induction of miR-630.
    Authors: Sakurai Et al.
    PLoS One  2014;9:e100124
  13. Interactions of ABCG2 (BCRP) with epidermal growth factor receptor kinase inhibitors developed for molecular imaging.
    Authors: Qawasmi Et al.
    Front Pharmacol  2014;5:257
  14. MetF. sensitizes EGFR-TKI-resistant human lung cancer cells in vitro and in vivo through inhibition of IL-6 signaling and EMT reversal.
    Authors: Li Et al.
    Clin Cancer Res  2014;20:2714
  15. Fhit regulates EMT targets through an EGFR/Src/ERK/Slug signaling axis in human bronchial cells.
    Authors: Joannes Et al.
    J Biol Chem  2014;12:775
  16. SR48692 inhibits non-small cell lung cancer proliferation in an EGF receptor-dependent manner.
    Authors: Moody Et al.
    Mol Cancer Res  2014;100:25
  17. Role for the epidermal growth factor receptor in chemotherapy-induced alopecia.
    Authors: Bichsel Et al.
    PLoS One  2013;8:e69368
  18. Effect of MetF. on residual cells after chemotherapy in a human lung adenocarcinoma cell line.
    Authors: Kitazono Et al.
    Int J Oncol  2013;43:1846
  19. Comparative gene expression profiling of benign and malignant lesions reveals candidate therapeutic compounds for leiomyosarcoma.
    Authors: Edris Et al.
    Sarcoma  2012;2012:805614
  20. Stathmin is involved in the cooperative effect of zoled. acid and gefi. on bone homing breast cancer cells in vitro.
    Authors: Oda Et al.
    J Bone Oncol  2012;1:40
  21. Epidermal growth factor receptor signaling modulates chemokine (CXC) ligand 5 expression and is associated with villus angiogenesis after small bowel resection.
    Authors: McMellen Et al.
    Surgery  2010;148:364

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