An internal standard for the quantification of gefitinib
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Unlabeled Version(s)
13166Gefitinib
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Gefitinib-d6

Item No. 22364

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(3-chloro-4-fluorophenyl)-7-methoxy-6-[3-(4-morpholinyl)propoxy-1,1,2,2,3,3-d6]-4-quinazolinamine
CAS Number
1228664-49-0
Molecular Formula
C22H18ClD6FN4O3
Formula Weight
452.9
Purity
≥99% deuterated forms (d1-d6)
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/mlEthanol: 0.3 mg/ml
SMILES
COC1=CC2=C(C(NC3=CC=C(F)C(Cl)=C3)=NC=N2)C=C1OC([2H])([2H])C([2H])([2H])C([2H])([2H])N4CCOCC4
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)/i2D2,5D2,8D2
InChi Key
XGALLCVXEZPNRQ-AQCDAZAYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

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    Product Description

    Gefitinib-d6 is intended for use as an internal standard for the quantification of gefitinib (Item No. 13166) by GC- or LC-MS. 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).