A potent inhibitor of VEGFR2 and bFGF
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CP 547,632

Item No. 21773

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[(4-bromo-2,6-difluorophenyl)methoxy]-5-[[[[4-(1-pyrrolidinyl)butyl]amino]carbonyl]amino]-4-isothiazolecarboxamide
CAS Number
252003-65-9
Molecular Formula
C20H24BrF2N5O3S
Formula Weight
532.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 94 mM
λmax
258 nm
SMILES
NC(C1=C(N([H])C(N(CCCCN2CCCC2)[H])=O)SN=C1OCC3=C(F)C=C(Br)C=C3F)=O
InChi Code
InChI=1S/C20H24BrF2N5O3S/c21-12-9-14(22)13(15(23)10-12)11-31-18-16(17(24)29)19(32-27-18)26-20(30)25-5-1-2-6-28-7-3-4-8-28/h9-10H,1-8,11H2,(H2,24,29)(H2,25,26,30)
InChi Key
HXHAJRMTJXHJJZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
4°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $63

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    1 mg

    $118

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    5 mg

    $481

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    Product Description

    CP 547,632 is an orally bioavailable and potent inhibitor of the receptor tyrosine kinases VEGF receptor 2 (VEGFR2) and basic fibroblast growth factor (bFGF) with IC50 values of 11 and 9 nM, respectively, in an enzyme assay.1 It is selective for VEGFR2 and bFGF over EGFR, PDGF receptor β (PDGFRβ), and related tyrosine kinases. CP 547,632 inhibits VEGFR2 autophosphorylation induced by VEGF in porcine aortic endothelial cells transfected with VEGFR2 (IC50 = 6 nM) and in a xenograft mouse model using NIH3T3/H-Ras cells (EC50 = 590 nM). It decreases angiogenesis induced by VEGF or bFGF and suppresses tumor growth in athymic mice.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Beebe, J.S., Jani, J.P., Knauth, E., et al. Pharmacological characterization of CP-547,632, a novel vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor for cancer therapy. Cancer Res. 63(21), 7301-7309 (2003).