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    Gefitinib (ZD 1839)
    Gefitinib (ZD 1839)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0534
    CAS #: 184475-35-2 Purity ≥98%

    Description: Gefitinib (formerly ZD1839, ZD-1839 or trade name: Iressa) is a potent and orally bioavailable EGFR inhibitor with potential anticancer activity. It inhibits EGFR Tyr1173, Tyr992, Tyr1173 and Tyr992 in the NR6wtEGFR and NR6W cells with IC50 of 37 nM, 37nM, 26 nM and 57 nM, respectively. 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. In May 2003, the FDA approved Gefitinib for non-small cell lung cancer (NSCLC). It was approved as monotherapy for the treatment of patients with locally advanced or metastatic NSCLC after failure of both platinum-based and docetaxel chemotherapies. i.e. as a third-line therapy.

    References: Br J Cancer. 2005;93(8):915-23.; Br J Cancer. 2002; 86(7): 1157–1161.; Clin Cancer Res. 2000;6(12):4885-92.

    Related CAS: 184475-55-6 (HCl salt)

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    Molecular Weight (MW)446.90
    FormulaC22H24ClFN4O3
    CAS No.184475-35-2 (free base);
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 89 mg/mL (199.1 mM)
    Water: <1 mg/mL
    Ethanol: 4 mg/mL (9.0 mM)
    Solubility (In vivo)5% DMSO+corn oil: 2.5 mg/mL
    SynonymsZD-1839; ZD1839; ZD 1839; Gefitinib; Brand name: Iressa. 

    Chemical Name: N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholinopropoxy)quinazolin-4-amine

    InChi Key: XGALLCVXEZPNRQ-UHFFFAOYSA-N

    InChi Code: InChI=1S/C22H24ClFN4O3/c1-29-20-13-19-16(12-21(20)31-8-2-5-28-6-9-30-10-7-28)22(26-14-25-19)27-15-3-4-18(24)17(23)11-15/h3-4,11-14H,2,5-10H2,1H3,(H,25,26,27)

    SMILES Code: COC1=CC2=NC=NC(NC3=CC=C(F)C(Cl)=C3)=C2C=C1OCCCN4CCOCC4


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    In Vitro

    In vitro activity: Gefitinib effectively inhibits all tyrosine phosphorylation sites on EGFR in both the high and low-EGFR-expressing cell lines including NR6, NR6M and NR6W cell lines. The phosphorylation sites Tyr1173 and Tyr992 are less sensitive requiring higher concentrations of Gefitinib for inhibition. Gefitinib effectively blocks the phosphorylation of PLC-γ, with IC50 of 27nM, in NR6W cells. The NR6wtEGFR and NR6M cell lines has low levels of PLC-γ phosphorylation but the level in the NR6M cell line is more resistant to inhibition by Gefitinib with IC50 of 43 nM and 369 nM, respectively. Gefitinib inhibits Akt phosphorylations, with IC50 of 220 and 263nM, in the low-EGFR- and -EGFRvIII-expressing cell lines, respectively. Gefitinib in the dose range from 0.1 to 0.5μM significantly facilitates, rather than abrogates, colony formation of NR6M cells. However, at a concentration of 2 μM Gefitinib completely blocks NR6M colony formation. Gefitinib rapidly and in a dose-dependent manner inhibits EGFR and ERK phosphorylation up to 72 hours after EGF stimulation in both the high- and low-EGFR-expressing cell lines. Gefitinib is the monolayer growth of these EGF-driven untransformed MCF10A cells with an IC50 of 20 NM. The combination of Gefitinib (0.2 μM and 0.5 μM) with irradiation lead to a significant growth inhibition in LoVo cells, compared with radiation alone.


    Kinase Assay: Gefitinib hydrochloride is an inhibitor that specifically binds and inhibits the EGFR tyrosine kinase, with the IC50 value of 2-37 nM in NR6wtEGFR cells. Gefitinib effectively blocks the phosphorylation of PLC-γ, with IC50 of 27nM, in NR6W cells. The NR6wtEGFR and NR6M cell lines has low levels of PLC-γ phosphorylation but the level in the NR6M cell line is more resistant to inhibition by Gefitinib with IC50 of 43 nM and 369 nM, respectively. Gefitinib inhibits Akt phosphorylations, with IC50 of 220 and 263nM, in the low-EGFR- and -EGFRvIII-expressing cell lines, respectively.


    Cell Assay: Exponentially growing cells including NR6, NR6M, NR6M and NR6W cells are seeded in sextuple in 96-well plates at a concentration of 2000 cells/well, allowed to adhere and subsequently washed in PBS and incubated overnight in medium containing 0.5% FCS. Cells are then treated with varying concentrations (0-2 μM) of Gefitinib or the solute control DMSO and EGF. The optimal EGF concentration for inducing proliferation of NR6wtEGFR and NR6W cells has previously been determined and hence NR6wtEGFR and NR6W cells are supplemented with 10 nM and 0.1 nM EGF, respectively. EGF is not added to NR6 and NR6M cells. After 72 hours the amount of cells are measured by performing a MTT proliferation assay.

    In VivoGefitinib (100 mg/kg) improves the anti-tumor effect of radiotherapy in LoVo tumor xenografts. Gefitinib treatment of nude mice bearing established human GEO colon cancer xenografts reveals a reversible dose-dependent inhibition of tumor growth because GEO tumors resumes the growth rate of controls at the end of the treatment.
    Animal modelNude mice (cba nu/nu) are intra-dermal injected with LoVo cells.
    Formulation & DosageDissolved in 0.5% polysorbate; 100 mg/kg; Oral gavage
    ReferencesBr J Cancer. 2005 Oct 17;93(8):915-23.; Br J Cancer. 2002 Apr 8; 86(7): 1157–1161.; Clin Cancer Res. 2000 Dec;6(12):4885-92.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Gefitinib (ZD1839)

    A, effect of metformin (MET) alone and in combination with gefitinib (GEF) on cell proliferation, on anchorage-independent growth ability of NSCLC cell lines, and on the induction of apoptosis in CALU-3, CALU-3 GEF-R, and H1299 cell lines.  2013 Jul 1;19(13):3508-19.

    Gefitinib (ZD1839)

    Effects on the downstream pathway by combined treatment of metformin and gefitinib. Western blotting of EGFR, MAPK, AKT p70S6K, and S6 activation following treatment with the indicated concentration of metformin and gefitinib in CALU-3 and CALU-3 GEF-R cell lines. β-Actin was included as a loading control.  2013 Jul 1;19(13):3508-19.

    Gefitinib (ZD1839)

    Effects of the combination treatment of metformin and gefitinib on NSCLC tumor xenografts.  2013 Jul 1;19(13):3508-19.

    Gefitinib (ZD1839)
    Gefitinib (ZD1839)


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