Biochem/physiol Actions

Cell permeable: no

Reversible: no

Product does not compete with ATP.

Primary TargetBlocks the binding of VEGF165 to its receptors

Target IC₅₀: 700 nM for VEGFR1, 1.3 µM for VEGFR2

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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Zilberberg, L., et al. 2003. J. Biol. Chem.278, 35564.

Packaging

1 mg in Plastic ampoule

Packaged under inert gas

Physical form

Supplied as a trifluoroacetate salt.

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Sequence

cyclic(D-Phe-Pro-Gln-Ile-Met-Arg-Ile-Lys-Pro-His-Gln-Gly-Gln-His-Ile-Gly-Glu)

Warning

Toxicity: Carcinogenic / Teratogenic (D)