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Vadimezan (DMXAA; ASA-404) acts as a tumor vascular disrupting agent (tumor-VDA), is also a murine agonist of the stimulator of interferon genes (STING) and also a potent inducer of type I IFNs and other cytokines. Vadimezan could enhance the immunogenicity of influenza split vaccine which led to significant increase in protective responses against live influenza virus challenge in mice compared to split vaccine alone. Using OVA as a model antigen, Vadimezan was demonstrated to improve on the antigen specific immune responses and induce a preferential Th2 (Type-2) response. Vadimezan has inhibitory effects against several kinases, with most potent effects being on members of the VEGFR (vascular endothelial growth factor receptor) tyrosine kinase family in blood during clinical trials. Vadimezan treatment of primary mouse macrophages resulted in robust IRF-3 activation and approximately 750-fold increase in IFN-beta mRNA, and in contrast to the potent Toll-like receptor 4 (TLR4) agonist lipopolysaccharide (LPS), signaling was independent of mitogen-activated protein kinase (MAPK) activation and elicited minimal nuclear factor kappaB-dependent gene expression. DMXAA-induced signaling was critically dependent on the IRF-3 kinase, TBK1, and IRF-3 but was myeloid differentiation factor 88-, Toll-interleukin 1 receptor domain-containing adaptor inducing IFN-beta-, IFN promoter-stimulator 1-, and inhibitor of kappaB kinase-independent, thus excluding all known TLRs and cytosolic helicase receptors. Vadimezan is a VDA currently in advanced phase II clinical trials.
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Source | Drug Des Devel Ther (2015). Figure 6. DMXAA |
| Method | Cell cycle analysis | |
| Cell Lines | A549 cells | |
| Concentrations | 1 μM | |
| Incubation Time | 24 h | |
| Results | Taken together, the results show that DMXAA can regulate the cell cycle distribution, contributing to its anticancer effect in A549 cells. |
| Molecular Weight | 282.29 |
| Formula | C17H14O4 |
| CAS Number | 117570-53-3 |
| Solubility (25°C) | DMSO 7 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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