General description
A macrocyclic 17-amino acid peptide derived from residues 79 - 93 of vascular endothelial growth factor that mediate its binding to VEGFR-2. It blocks the binding of VEGF165 to its receptors (IC50 = 700 nM for VEGFR1, 1.3 µM for VEGFR2) and exhibits anti-angiogenic activity as well as other VEGFR-mediated cellular functions, such as proliferation (IC50 = 5.8 µM), migration (IC50 = 8.2 µM), and activation of MAP kinases. Its anti-angiogenic activity has been successfully demonstrated in vivo using chick embryos and nude mice tumor models of human intracranial and syngeneic glioma.
A macrocyclic, 17-amino acid peptide derived from residues 79-93 of vascular endothelial growth factor (VEGF) that mediates the binding of VEGF to its receptor, VEGFR-2. Blocks the binding of VEGF165 to its receptors (IC50 = 70 nM for VEGFR-1, 1.3 µM for VEGFR-2) and exhibits anti-angiogenic properties. Also reported to block other VEGF-mediated cellular functions such as proliferation (IC50 = 5.8 µM), migration (IC50 = 8.2 µM), and activation of MAP kinases. Also reported to exhibit anti-angiogenic properties in vivo using chick embryo and nude mouse tumor models of human intracranial and syngeneic glioma.
Biochem/physiol Actions
Cell permeable: no
Primary Target
Blocks the binding of VEGF165 to its receptors
Product does not compete with ATP.
Reversible: no
Target IC50: 700 nM for VEGFR1, 1.3 µM for VEGFR2
Packaging
Packaged under inert gas
Physical form
Supplied as a trifluoroacetate salt.
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Zilberberg, L., et al. 2003. J. Biol. Chem.278, 35564.
cyclic(D-Phe-Pro-Gln-Ile-Met-Arg-Ile-Lys-Pro-His-Gln-Gly-Gln-His-Ile-Gly-Glu)
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Carcinogenic / Teratogenic (D)
| Quality Segment | 100 |
| assay | ≥97% (HPLC) |
| form | lyophilized solid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,desiccated (hygroscopic),protect from light |
| color | white |
| solubility | DMSO: 5 mg/mL,water: soluble |
| shipped in | wet ice |
| storage temp. | −20°C |
