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

Géfitinib (ZD1839) est un EGFR tyrosine kinase puissant, sélectif et actif par voie orale avec un IC50 de 33 nM. Géfitinib inhibe sélectivement la croissance des cellules tumorales stimulées par l'EGF (IC50 de 54 nM) et bloque l'autophosphorylation EGF-stimulée EGFR dans les cellules tumorales. Géfitinib induit également l'autophagie. Géfitinib a une activité antitumorale.

Gefitinib (ZD1839) ist ein potenter, selektiver und oral wirksamer EGFR tyrosine kinase-Inhibitor mit einem IC50 von 33 nM. Gefitinib hemmt selektiv das EGFR-stimulierte Wachstum von Tumorzellen (IC50 von 54 nM) und blockiert die b>EGFR-stimulierte EGFR-Autophosphorylierung in Tumorzellen. Gefitinib induziert auch autophagy. Gefitinib hat antitumorale Aktivität.

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 and cell apoptosis, which can be used for cancer related research, such as Lung cancer and breast cancer .

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

Gefitinib Chemical Structure

Gefitinib Chemical Structure

CAS No. : 184475-35-2

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 66 In-stock
Solution
10 mM * 1 mL in DMSO USD 66 In-stock
Solid
100 mg USD 60 In-stock
500 mg USD 72 In-stock
1 g USD 90 In-stock
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Customer Review

Based on 140 publication(s) in Google Scholar

Other Forms of Gefitinib:

Gefitinib Related Antibodies

Top Publications Citing Use of Products

130 Publications Citing Use of MCE Gefitinib

WB
Cell Viability Assay

    Gefitinib purchased from MedChemExpress. Usage Cited in: Kaohsiung J Med Sci. 2023 Apr 14.  [Abstract]

    Gefitinib (0-20 μM; 24 h) significantly inhibits the viability of A549 cells.

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

    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 MedChemExpress. Usage Cited in: Theranostics. 2018 Jul 30;8(15):4262-4278.  [Abstract]

    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, Gefitinib at 2.5 µM, SU 11248 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 MedChemExpress. Usage Cited in: Cell Death Dis. 2018 Feb 15;9(3):269.  [Abstract]

    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, GSK1120212, and U0126 in the Si RhoA transfected HepG2 and SMMC7721 cells for 48 h in HepG2 and SMMC7721 cells.

    Gefitinib purchased from MedChemExpress. Usage Cited in: Oncogene. 2018 Aug;37(31):4300-4312.  [Abstract]

    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 MedChemExpress. Usage Cited in: Oncol Rep. 2018 Oct;40(4):2242-2250.  [Abstract]

    Effects of Gefitinib(G) and SC 58635 (Cel) on ABCB1 (MDR1), FOXM1 and Bcl 2 protein levels in PC3/DR and DU145/DR cell lines. The effects of Gefitinib, SC 58635 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 MedChemExpress. Usage Cited in: Breast Cancer Res. 2017 Aug 4;19(1):90.  [Abstract]

    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 MedChemExpress. Usage Cited in: Exp Cell Res. 2017 Dec 15;361(2):246-256.  [Abstract]

    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 MedChemExpress. Usage Cited in: Mol Med Rep. 2017 Sep;16(3):3475-3481.  [Abstract]

    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).

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

    Changes in Bcl-2 protein expression in MCF-7 cells after treatment with 2CdA, BMS-354825 or Gefitinib alone or in combination for 12 h. Expression of Bcl-2 protein is analyzed by western blotting analysis.

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    • Biological Activity

    • 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 and cell apoptosis, which can be used for cancer related research, such as Lung cancer and breast cancer [1][2][5].

    IC50 & Target[1]

    EGFR

     

    In Vitro

    Gefitinib (0.01-0.1  μM, 72 h) results in increased phosphotyrosine load of the receptor, increased signalling to ERK and stimulation of proliferation and anchorage-independent growth[2].
    Gefitinib (1-2 μM, 72 h) significantly decreases EGFRvIII phosphotyrosine load, EGFRvIII-mediated proliferation and anchorage-independent growth[2].
    Gefitinib (0.62 μM, 24-72 h) inhibits IL-13-induced M2-like polarization of RAW 264.7 cells through the STAT6-dependent signaling pathway[3].
    Gefitinib (0.62 μM, 72 h) inhibits M2-like macrophage-promoted invasion and migration[3].
    Gefitinib (0-10 μM, 72 h) induces apoptosis (induction of BIM protein) in NSCLC Cell Lines (H3255 and HCC827 cells)[4].
    Gefitinib (100 nM, 24 h) suppresses macropinocytosis and increases the cellular uptake of extracellular vesicles( EVs) in HCC827 and A549 cells[6].
    Gefitinib (1.5-60 μM, 48 h) increases inhibition of proliferation in H358R and A549R cells (Cisplatin-resistant wtEGFR NSCLC cell lines)[7].

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

    Gefitinib Related Antibodies

    Western Blot Analysis[2]

    Cell Line: NR6wtEGFR, NR6W and NR6M
    Concentration: 1, 10, 100 μM
    Incubation Time: 5 h
    Result: Inhibited EGFR tyrosine phosphorylations.

    Cell Migration Assay [3]

    Cell Line: LLCs cell
    Concentration: 0.62 μM
    Incubation Time: 72 h
    Result: Abrogated M2-like macrophage promoted invasion and migration of LLCs.
    In Vivo

    Gefitinib (Oral administration, 75 mg/kg/d, 21 days) inhibits the M2-like polarization of macrophages in LLC mice metastasis model[3].
    Gefitinib (Oral administration, 75 mg/kg for the initial week, daily for 5 consecutive days per week) eliminates phosphorylation of HER2 and HER3 and signaling through MAPK and Akt in lobular hyperplasias and carcinomas, increases MAPK activity and cytokine production in splenocytes and lymph nodes[5]. Gefitinib (Oral gavage, 150 mg/kg, daily) enhances the anti-tumor effect of Cisplatin in H358R xenograft[7].

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

    Animal Model: LLC mice metastasis model[3]
    Dosage: 75 mg/kg/d, for 21 days.
    Administration: Oral administration
    Result: Reduced the number of lung metastasis nodules, down-regulated the expression of M2 marker genes and the percentages CD206+ and CD68+ macrophages in tumor tissues.
    Animal Model: BALB-NeuT transgenic mouse model[5]
    Dosage: 75 mg/kg for the initial week, and increased by 15 mg/kg every other week, daily for 5 consecutive days per week, followed by 2 days without treatment and repeated for 8–9 weeks.
    Administration: Oral administration
    Result: Reduced tumor multiplicity from 9.6 to 0.58 (83%), and reduced the number and size of lobules and lobular nodules in treated mice.
    Clinical Trial
    Molecular Weight

    446.90

    Formula

    C22H24ClFN4O3
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    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 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (223.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    90% Corn Oil

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

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    • Protocol 2

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

      Solubility: ≥ 2.08 mg/mL (4.65 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  Corn Oil

      Solubility: 5 mg/mL (11.19 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

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    g

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    % 
    +
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.94%

    COA (250 KB) LCMS (102 KB) Elemental Analysis Report (108 KB)

    Handling Instructions (2659 KB)
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.2376 mL 11.1882 mL 22.3764 mL 55.9409 mL
    5 mM 0.4475 mL 2.2376 mL 4.4753 mL 11.1882 mL
    10 mM 0.2238 mL 1.1188 mL 2.2376 mL 5.5941 mL
    15 mM 0.1492 mL 0.7459 mL 1.4918 mL 3.7294 mL
    20 mM 0.1119 mL 0.5594 mL 1.1188 mL 2.7970 mL
    25 mM 0.0895 mL 0.4475 mL 0.8951 mL 2.2376 mL
    30 mM 0.0746 mL 0.3729 mL 0.7459 mL 1.8647 mL
    40 mM 0.0559 mL 0.2797 mL 0.5594 mL 1.3985 mL
    50 mM 0.0448 mL 0.2238 mL 0.4475 mL 1.1188 mL
    60 mM 0.0373 mL 0.1865 mL 0.3729 mL 0.9323 mL
    80 mM 0.0280 mL 0.1399 mL 0.2797 mL 0.6993 mL
    100 mM 0.0224 mL 0.1119 mL 0.2238 mL 0.5594 mL
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    Gefitinib Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Gefitinib184475-35-2ZD1839ZD 1839ZD-1839EGFRAutophagyApoptosisEpidermal growth factor receptorErbB-1HER1EGFR tyrosine kinaseantitumourphosphorylationTAMstumor metastasislung cancerNSCLCsbreast cancerInhibitorinhibitorinhibit

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