DMBO

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.

Packaged under inert gas

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

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

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

Toxicity: Standard Handling (A)