A broad-spectrum tyrosine kinase inhibitor
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Foretinib

Item No. 16249

Technical Information
Formal Name
N-[3-fluoro-4-[[6-methoxy-7-[3-(4-morpholinyl)propoxy]-4-quinolinyl]oxy]phenyl]-N'-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide
CAS Number
849217-64-7
Synonyms
  • GSK1363089
  • XL880
Molecular Formula
C34H34F2N4O6
Formula Weight
Purity
≥98%
A crystalline solid
DMF: 25 mg/mlDMSO: 16 mg/mlEthanol: 25 mg/mlEthanol:PBS (pH 7.2) (1:3): 0.25 mg/ml
λmax
242 nm
SMILES
COC(C=C(C(OC1=CC=C(NC(C2(CC2)C(NC3=CC=C(F)C=C3)=O)=O)C=C1F)=CC=N4)C4=C5)=C5OCCCN6CCOCC6
InChi Code
InChI=1S/C34H34F2N4O6/c1-43-30-20-25-27(21-31(30)45-16-2-13-40-14-17-44-18-15-40)37-12-9-28(25)46-29-8-7-24(19-26(29)36)39-33(42)34(10-11-34)32(41)38-23-5-3-22(35)4-6-23/h3-9,12,19-21H,2,10-11,13-18H2,1H3,(H,38,41)(H,39,42)
InChi Key
CXQHYVUVSFXTMY-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Foretinib is a broad-spectrum tyrosine kinase (TK) inhibitor that targets members of the HGF and VEGF receptor TK families, as well as KIT, Flt-3, PDGFRβ, and Tie-2, at nanomolar concentrations.1,2 It blocks HGF-induced Met phosphorylation and VEGF-induced ERK phosphorylation, preventing HGF-induced responses in tumor cells and HGV/VEGF-induced responses in endothelial cells.1,3 Foretinib is functional in vivo, reducing tumor burden in an experimental model of lung metastasis.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Qian, F., Engst, S., Yamaguchi, K., et alInhibition of tumor cell growth, invasion, and metastasis by EXEL-2880 (XL880, GSK1363089), a novel inhibitor of HGF and VEGF receptor tyrosine kinases. Cancer Res. 69(20), 8009-8016 (2009).

    2. Davis, M.I., Hunt, J.P., Herrgard, S., et alComprehensive analysis of kinase inhibitor selectivity. Nat. Biotechnol. 29(11), 1046-1051 (2011).

    3. Mughal, A., Aslam, H.M., Sheikh, A., et alc-Met inhibitors. Infect. Agent. Cancer 8, 13 (2013).