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Gefitinib

based on 1 citations in multiple journalsGefitinib14.1 4
An EGFR kinase inhibitor
Catalog #: 1589
SKU-Size Size Price Qty
1589-5 5 mg
$110.00
1589-25 25 mg
$215.00
More Sizes Get Quote

Product Details

Alternate Name ZD-1839
Appearance White to off-white solid
CAS # 184475-35-2
Molecular Formula C₂₂H₂₄ClFN₄O₃
Molecular Weight 446.9
Purity ≥99% by HPLC
Solubility DMSO (100 mg/ml)
SMILES COC1=C(C=C2C(=C1)N=CN=C2NC3=CC(=C(C=C3)F)Cl)OCCCN4CCOCC4
InChi 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
PubChem CID 123631
MDL Number MFCD04307832
Handling Protect from light and moisture
Storage Conditions -20°C
Shipping Conditions RT
USAGE For Research Use Only! Not For Use in Humans.

Details

Gefitinib was found to be a potent inhibitor of EGFR kinase (Ki = 0.40 nM), but much weaker against ErbB-2 kinase (Ki = 870 nM) and ErbB-4 kinase (Ki = 1.1 µM). The IC₅₀ values for Gefitinib to inhibit HT-29 and LoVo cell growth were 23.6 - >100 µM and 7.3 - 48.5 µM, respectively, when the exposure times are from 18 hours to 3 days. The IC₅₀ values of Gefitinib to the breast cancer cell lines BT20, HCC1937, MDA-MB-231, BT474, and SKBR3 are 15.5±1.4, 8.4±1.5, 20.7±1.1, 0.25±0.05, 0.88±0.31 µM, respectively


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Leong et al., Targeting Cancer Stem Cell Plasticity Through Modulation of Epidermal Growth Factor and Insulin-Like Growth Factor Receptor Signaling in Head and Neck Squamous Cell Cancer. Stem Cells Trans Med, Sep 2014; 3: 1055 - 1065.
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