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
This product is not in stock, which may be available by custom synthesis.
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Synonym: GFB204; GFB-204; GFB 204.
IUPAC/Chemical Name: NONE
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >5 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
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.
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.).