A potent, orally available VEGFR2 inhibitor
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Ki8751

Item No. 18004

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(2,4-difluorophenyl)-N'-[4-[(6,7-dimethoxy-4-quinolinyl)oxy]-2-fluorophenyl]-urea
CAS Number
228559-41-9
Molecular Formula
C24H18F3N3O4
Formula Weight
469.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMF:PBS (pH 7.2)(1:3): 0.25 mg/mlDMSO: 20 mg/ml
λmax
243, 282, 308, 322 nm
SMILES
COC1=C(OC)C=C(C(OC2=CC(F)=C(NC(NC3=C(F)C=C(F)C=C3)=O)C=C2)=CC=N4)C4=C1
InChi Code
InChI=1S/C24H18F3N3O4/c1-32-22-11-15-20(12-23(22)33-2)28-8-7-21(15)34-14-4-6-19(17(27)10-14)30-24(31)29-18-5-3-13(25)9-16(18)26/h3-12H,1-2H3,(H2,29,30,31)
InChi Key
LFKQSJNCVRGFCC-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $68

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    10 mg

    $124

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    25 mg

    $258

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    50 mg

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    Product Description

    Ki8751 is a potent, orally available inhibitor of the kinase activity of VEGFR2 (IC50 = 0.9 nM).1 It less potently inhibits c-Kit, PDGRFα, and FGFR2 (IC50s = 40-170 nM) and has no significant effect against several other receptor tyrosine kinases. Ki8751 suppresses the growth of VEGF-stimulated human umbilical vein endothelial cells at nanomolar concentrations.1 It shows significant anti-tumor activity against assorted human tumor xenografts in nude mice.1 Ki8751 also induces cellular senescence in colorectal cancer cells.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kubo, K., Shimizu, T., Ohyama, S., et al. Novel potent orally active selective VEGFR-2 tyrosine kinase inhibitors: Synthesis, structure-activity relationships, and antitumor activities of N-phenyl-N'-{4-(4-quinolyloxy)phenyl}ureas. J. Med. Chem. 48(5), 1359-1366 (2005).

    2. Hasan, M.R., Ho, S.H.Y., Owen, D.A., et al. Inhibition of VEGF induces cellular senescence in colorectal cancer cells. Int. J. Cancer 129(9), 2115-2123 (2011).