An EGFR inhibitor
Related Products
Active Metabolite(s)
22365O-Desmethyl Gefitinib
Labeled Version(s)
22364Gefitinib-d6
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Gefitinib

Item No. 13166

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(3-chloro-4-fluorophenyl)-7-methoxy-6-[3-(4-morpholinyl)propoxy]-4-quinazolinamine
CAS Number
184475-35-2
Synonyms
  • ZD 1839
Molecular Formula
C22H24ClFN4O3
Formula Weight
446.9
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/mlDMSO:PBS(pH7.2) (1:1): 0.5 mg/mlEthanol: 0.3 mg/ml
λmax
205, 226, 250, 332 nm
SMILES
COC1=CC2=C(C(NC3=CC=C(F)C(Cl)=C3)=NC=N2)C=C1OCCCN4CCOCC4
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)
InChi Key
XGALLCVXEZPNRQ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

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    100 mg

    $37

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    250 mg

    $82

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    500 mg

    $153

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    1 g

    $270

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    Product Description

    Gefitinib is an EGFR inhibitor (IC50s = 0.023-0.079 µM).1 It inhibits colony formation of GEO colon, ZR-75-1 and MCF-10A breast, and OVCAR-3 ovarian cancer cell lines in soft agar assays (IC50s = 0.2-0.4 µM).2 Gefitinib (0.1 to 1 µM) induces apoptosis and inhibits EGFR autophosphorylation in the same cells. In vivo, gefitinib (1.25, 2.5, and 5 mg/kg) reduces tumor volume and increases survival in a GEO mouse xenograft model. Formulations containing gefitinib have been used in the treatment of non-small cell lung cancer (NSCLC).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Mendelsohn, J., and Baselga, J. The EGF receptor family as targets for cancer therapy. Oncogene 19(56), 6550-6565 (2000).

    2. Ciardiello, F., Caputo, R., Bianco, R., et al. 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. Clin. Cancer Res. 6(5), 2053-2063 (2000).