General description

An oxazine that appears to mimic the pyranosidic moiety of heparin sulfate, and is shown to interact directly with several growth factors and cytokines including VEGF, TNF-α and heparin-binding-EGF in a surface plasmon resonance assay. At concentrations of 10-80 µM, this compound dose-dependently inhibits the proliferation of VEGF-expressing LM8G7 cells (IC₅₀ = 13 µM), and TNF-α-expressing OVSAHO cells (IC₅₀ = 19 µM). At 195 µM, a 99% reduction in cell growth is observed in HB-EGF-expressing SKOV-3 cultures. This compound inhibits heparanase-mediated degradation of heparin sulfate in LM8G7 cells (IC₅₀ = 65 µM and 104-206 µM, in an enzymatic and a cell based assay, respectively). At 0.5-5 µM, it markedly prevents the migration and invasion of the same culture, in a dose-dependent manner. In addition, it completely suppresses liver metastatic nodules of osteosarcoma mice injected with LM8G7 cells at 0.5 mg/kg without any signs of toxicity in vivo, and demonstrates a synergistic anti-tumor effect when dosed with heparin.

Legal Information

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

Other Notes

Basappa, et al. 2010. Cancer Lett.279, 231.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

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

Warning

Toxicity: Standard Handling (A)