1. Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
    Autophagy
  2. EGFR
    Autophagy
  3. Gefitinib

Gefitinib (Synonyms: ZD1839)

Cat. No.: HY-50895 Purity: 99.94%
Handling Instructions

Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity.

For research use only. We do not sell to patients.

Gefitinib Chemical Structure

Gefitinib Chemical Structure

CAS No. : 184475-35-2

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
100 mg USD 60 In-stock
Estimated Time of Arrival: December 31
500 mg USD 72 In-stock
Estimated Time of Arrival: December 31
1 g USD 90 In-stock
Estimated Time of Arrival: December 31
5 g USD 180 In-stock
Estimated Time of Arrival: December 31
10 g   Get quote  
50 g   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 52 publication(s) in Google Scholar

Other Forms of Gefitinib:

Top Publications Citing Use of Products

Publications Citing Use of MCE Gefitinib

    Gefitinib purchased from MCE. Usage Cited in: Breast Cancer Res. 2017 Aug 4;19(1):90.

    The effect of Gefitinib-FTY720 treatment on CD44 expression in TNBC cell lines. HCC1806, Hs578T, and MDA-MB-468 TNBC cell lines at ~40% confluence in 12-well plates are exposed for 24 h to Gefitinib (Gef: 0.1 to 10 μM), with or without the addition of 1.5 μM FTY720.

    Gefitinib purchased from MCE. Usage Cited in: Theranostics. 2018 Jul 30;8(15):4262-4278.

    BV2 cells are pretreated with 0.1% DMSO (Ctrl), JuA (25 µM) or JuA (25 µM) with the indicated antagonist of RTKs (Dovitinib at 1 µM, Gefinitib at 2.5 µM, Sunitinib at 2.5 µM and LDC1267 at 1 µM) for 30 min, followed by administration of Aβ42 (5 μM) for 12 h.

    Gefitinib purchased from MCE. Usage Cited in: Chem Pharm Bull (Tokyo). 2017 Aug 1;65(8):768-775.

    Changes in Bcl-2 protein expression in MCF-7 cells after treatment with Cladribine, Dasatinib or Gefitinib alone or in combination for 12 h. Expression of Bcl-2 protein is analyzed by western blotting analysis.

    Gefitinib purchased from MCE. Usage Cited in: Exp Cell Res. 2017 Dec 15;361(2):246-256.

    Western blot analysis for p21, p-p21, Cyclin D1. Bcl-2, Caspase 3, Cleaved Caspase 3, Caspase 9, Cleaved Caspase 9 and Bax in HCC827-GR and PC-9-GR cells treated with control, Efatutazone alone, Gefitinib alone, or Efatutazone combined with gefitinib for 48 h.

    Gefitinib purchased from MCE. Usage Cited in: Oncogene. 2018 Aug;37(31):4300-4312.

    Western blot analysis of E-cadherin and vimentin in HCC827 xenograft tumors treated with Gefitinib daily for 6-8 weeks until tumors regrown (resistant) or saline for 1 week (sensitive) (left panel).

    Gefitinib purchased from MCE. Usage Cited in: Cancer Cell. 2018 Jun 11;33(6):1061-1077.e6.

    WT mice are either treated with vehicle or Gefitinib (100 mg/kg/day) starting one day prior to DEN injection (100 mg/kg). Livers are collected at 3 and 48 hr after DEN injection and subjected to IB analyses with the indicated antibodies.

    Gefitinib purchased from MCE. Usage Cited in: Cell Death Dis. 2018 Feb 15;9(3):269.

    WB is used to detect the effect of EGF treatment for 4 h on the expression of YAP with the inhibitors of EGFR or its downsream members, including Gefitinib, LY294002, Wortmannin, GSK2334470, BX-795, MK-2206, Trametinib, and U0126 in the Si RhoA transfected HepG2 and SMMC7721 cells for 48 h in HepG2 and SMMC7721 cells.

    Gefitinib purchased from MCE. Usage Cited in: Oncol Rep. 2018 Oct;40(4):2242-2250.

    Effects of Gefitinib(G) and Celecoxib(Cel) on ABCB1 (MDR1), FOXM1 and Bcl 2 protein levels in PC3/DR and DU145/DR cell lines. The effects of Gefitinib, Celecoxib and their combination on ABCB1 (MDR1), FOXM1 and Bcl 2 expression in the PC3/DR and DU145/DR cell lines are determined by a western blot assay.

    Gefitinib purchased from MCE. Usage Cited in: Mol Med Rep. 2017 Sep;16(3):3475-3481.

    Cyclin B1 and Cdk1 protein expression levels are significantly downregulated in NCI-H1975 cells treated with the combination of DHA (5 µM) and Gefitinib (10 µM).
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity[1][2].

    IC50 & Target[1]

    EGFR

     

    In Vitro

    Gefitinib (0.01-0.1 mM) results in increased phosphotyrosine load of the receptor, increased signalling to ERK and stimulation of proliferation and anchorage-independent growth, presumably by inducing EGFRvIII dimerisation in long-term exposure of EGFRvIII-expressing cells. On the other hand, gefitinib (1-2 mM) significantly decreases EGFRvIII phosphotyrosine load, EGFRvIII-mediated proliferation and anchorage-independent growth[1]. Gefitinib (ZD1839) inhibits the monolayer growth of these EGF-driven untransformed cells with IC50 of 20 nM[2]. Gefitinib leads to an inhibition of CALU-3 and GLC82 cell proliferation, with an IC50 of 2 μM[3].

    In Vivo

    Gefitinib (150 mg/kg, p.o.) in conbination with Metformin induces a significant reduction in tumor growth in nude mice bearing H1299 or CALU-3 GEF-R cells that are grown subcutaneously as tumor xenografts[3]. In irradiated rats, Gefitinib treatment augmentes lung inflammation, including inflammatory cell infiltration and pro-inflammatory cytokine expression, while Gefitinib treatment attenuates fibrotic lung remodeling due to the inhibition of lung fibroblast proliferation[4].

    Clinical Trial
    Molecular Weight

    446.90

    Formula

    C₂₂H₂₄ClFN₄O₃

    CAS No.

    184475-35-2

    SMILES

    ClC1=C(C=CC(NC2=NC=NC3=C2C=C(C(OC)=C3)OCCCN4CCOCC4)=C1)F

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 50 mg/mL (111.88 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2376 mL 11.1882 mL 22.3764 mL
    5 mM 0.4475 mL 2.2376 mL 4.4753 mL
    10 mM 0.2238 mL 1.1188 mL 2.2376 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (5.59 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (5.59 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [3]

    Cancer cells are seeded in 96-well plates and are treated with different doses of Gefitinib (0.01-20 μM), Metformin or both for 72 hours. Cell proliferation is measured with the MTT assay. The IC50 values are determined by interpolation from the dose-response curves. Results represent the median of 3 separate experiments each conducted in quadruplicate. The results of the combined treatment are analyzed according to the method of Chou and Talalay by using the CalcuSyn software program[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [3][4]

    Mice[3]
    Four- to 6-week old female balb/c athymic (nu+/nu+) mice are acclimatized for 1 week before being injected with cancer cells and injected subcutaneously with 107 H1299 and CALU-3 GEF-R cells that has been resuspended in 200 μL of Matrigel. When established tumors of approximately 75 mm3 in diameter are detected, mice are left untreated or treated with oral administrations of metformin (200 mg/mL metformin diluted in drinking water and present throughout the experiment), gefitinib (150 mg/kg daily orally by gavage), or both for the indicated time periods. Each treatment group consists of 10 mice. Tumor volume is measured using the formula π/6×larger diameter×(smaller diameter)2.
    Rats[4]
    The rats are randomly assigned to 1 of 4 experimental groups: 1) the unirradiated rats treated with oral administration of vehicle (0.1% Tween 80) once daily; 2) the unirradiated rats treated with oral administration of gefitinib (50 mg/kg/day) once daily; 3) the irradiated rats treated with oral administration of vehicle once daily; 4) the irradiated rats treated with oral administration of gefitinib once daily. Each experimental group comprised 5-6 rats and all treatments are delivered for 14 days.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Purity: 99.94%

    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.
    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Keywords:

    GefitinibZD1839ZD 1839ZD-1839EGFRAutophagyEpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product name

     

    Salutation

    Applicant name *

     

    Email address *

    Phone number *

     

    Organization name *

    Country or Region *

     

    Requested quantity *

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product name:
    Gefitinib
    Cat. No.:
    HY-50895
    Quantity:
    MCE Japan Authorized Agent: