All AbMole products are for research use only, cannot be used for human consumption.
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.
 |
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. |
| Cell Experiment | |
|---|---|
| Cell lines | M1 and M2 polarized macrophage |
| Preparation method | M1 and M2 polarized macrophages were treated with 20 µg/ml DMXAA (or dose response) or DMSO vehicle for an additional 24 hours. In addition, M2 polarized macrophages were treated with 20 µg/ml or 40 µg/ml 2′3′-cGAMP in the presence of Lipofectamine-2000. |
| Concentrations | 20 µg/ml |
| Incubation time | 24 hours |
| Animal Experiment | |
|---|---|
| Animal models | 4T1 tumor-bearing mice |
| Formulation | Not mentioned |
| Dosages | 2 mg/kg |
| Administration | i.v. injection |
| 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 |
| Related STING Products |
|---|
| G10
G10 is a activator of STING-dependent signaling. |
| 3′3′-cGAMP
3',3'-cGAMP is an endogenous second messenger in metazoans and triggers interferon production in response to cytosolic DNA. 3',3'-cGAMP activates stimulator of interferon genes (STING), which activates a signaling cascade leading to the production of type I interferons and other immune mediators. |
| diABZI (tautomerism)
diABZI (STING agonist 1; Tautomerism) is a selective stimulator of interferon genes (STING) receptor agonist, with EC50s of 130, 186 nM for human and mouse, respectively. |
| C-176
C-176 is a potent, selective and blood-brain barrier permeable inhibitor of STING. C-176 covalently targets transmembrane cysteine residue 91 and thereby blocking activation-induced palmitoylation of STING. |
| SR-717
SR-717 is a non-nucleotide STING agonist with EC50s of 2.1 μM and 2.2 μM in ISG-THP1 (WT) and ISG-THP1 cGAS KO (cGAS KO) cell lines, respectively. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2026 AbMole BioScience. All Rights Reserved.
