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
Warning
Toxicity: Carcinogenic / Teratogenic (D)
Sequence
cyclic(D-Phe-Pro-Gln-Ile-Met-Arg-Ile-Lys-Pro-His-Gln-Gly-Gln-His-Ile-Gly-Glu)
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.
Other Notes
Zilberberg, L., et al. 2003. J. Biol. Chem.278, 35564.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Molecular Weight: 1998.31. Empirical Formula: C90H140N28O22S. Quality Level: 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. Storage Class Code: 11 - Combustible Solids. WGK: WGK 1. Flash Point(F): Not applicable. Flash Point(C): Not applicable.- UPC:
- 12352200
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 676496-1MG