WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 205798
Description: GFB-204 is a calixarene derivative that is a potent and selective inhibitor of VEGFR and PDGFR tyrosine phosphorylation. G FB-204 had been shown through several in-vivo and in-vitro studies to bind to VEGF and PDGF, block binding of VEGF and PDGF to their receptors and subsequently inhibit Flk-1 and PDGFR tyrosine phosphorylation and stimulation of the protein kinases Erk1, Erk2, and AKT and the signal transducer and activator of transcription STAT3. Since tumor angiogenesis depends on VEGF for initiation and PDGF for maintenance of blood vessels, an agent which suppresses the functions of both VEGF and PDGF would potentially be more effective in tumor control that an agent which targets only one of these two growth factors. Preclinical studies have also shown that GFB-204 inhibits capillary network formation in a dose-response manner and inhibits VEGF-dependent human brain endothelial cell migration. A lung xenograft study in mice has shown that GFB-204 is active in a dose dependent manner. (Source: http://kiraxcorp.com/gfb204.html).
MedKoo Cat#: 205798
Synonym: GFB204; GFB-204; GFB 204.
IUPAC/Chemical Name: NONE
GFB-204 , that binds PDGF and VEGF, blocks binding of PDGF and VEGF to their receptors (200-500 nM) and subsequently inhibits PDGFR and Flk-1 tyrosine phosphorylation and stimulation of the protein kinases Erk1, Erk2 and Akt and the signal transducer and activator of transcription STAT3. GFB-204 is selective for PDGF and VEGF and does not inhibit EGF, IGF-1 and FGF stimulation of Erk1/2, Akt and STAT3. GFB-204 inhibits endothelial cell migration and capillary network formation in vitro. Finally, treatment of mice with GFB-204 suppresses human tumor growth and angiogenesis. Thus, inhibition of VEGF and PDGF receptor binding with a synthetic molecule results in potent inhibition of angiogenesis and tumorigenesis. (source: Oncogene. 2005 Jul 7;24(29):4701-9.).
1: Sun J, Wang DA, Jain RK, Carie A, Paquette S, Ennis E, Blaskovich MA, Baldini L, Coppola D, Hamilton AD, Sebti SM. Inhibiting angiogenesis and tumorigenesis by a synthetic molecule that blocks binding of both VEGF and PDGF to their receptors. Oncogene. 2005 Jul 7;24(29):4701-9. PubMed PMID: 15897913.