A potent, reversible, ATP-competitive and selective inhibitor of Flk-1 kinase (IC50 = 700 nM), a vascular endothelial growth factor (VEGF) receptor kinase. Also reduces the expression of ets-1, a transcription factor stimulated by VEGF. Has only a weak inhibitory effect on PDGF-receptor (IC50 >50 µM), EGF-receptor (IC50 >100 µM), and HER2 (IC50 >100 µM) kinases. Acts as an angiogenesis inhibitor as shown by its activity in the chorioallantoic membrane (CAM) assay and in an in vivo VEGF-induced permeability assay.
A potent, reversible, ATP-competitive and selective inhibitor of Flk-1 kinase (IC50 = 700 nM), a vascular endothelial growth factor (VEGF) receptor kinase. Has only a weak inhibitory effect on PDGF receptor (IC50 >50 µM), EGF-receptor (IC50 >100 µM), and HER-2 (IC50 >100 µM) kinases. Acts as an angiogenesis inhibitor as shown by its activity in the chorioallantoic membrane (CAM) assay and in an in vivo VEGF-induced permeability assay.
Biochem/physiol Actions
Primary Target Flk-1 kinase
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Arbiser, J.L., et al. 2000. Am. J. Pathol. 156, 1469. Strawn, L.M., et al. 1996. Cancer Res. 56, 3540.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 1
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
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