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DMXAA

Cat. No. M1999
DMXAA Structure
Synonym:

Vadimezan, ASA404

Size Price Availability Quantity
10mg USD 140 In stock
50mg USD 500 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

DMXAA (Vadimezan, ASA404) is a small-molecule tumour-vascular disrupting agent (Tumour-VDA). DMXAA 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, DMXAA was demonstrated to improve on the antigen specific immune responses and induce a preferential Th2 (Type-2) response. DMXAA 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. DMXAA 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. DMXAA is a VDA currently in advanced phase II clinical trials.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 282.29
Formula C17H14O4
CAS Number 117570-53-3
Purity >99%
Solubility DMSO
Storage at -20°C
Customer Product Validations & Biological Datas
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.
Rating
References

DMXAA (Vadimezan, ASA404) is a multi-kinase inhibitor targeting VEGFR2 in particular.
Buchanan CM, et al. Clin Sci (Lond). 2012 May 1;122(10):449-57. PMID: 22142330.

Randomised phase II study of ASA404 combined with carboplatin and paclitaxel in previously untreated advanced non-small cell lung cancer.
McKeage MJ, et al. Br J Cancer. 2008 Dec 16;99(12):2006-12. PMID: 19078952.

The chemotherapeutic agent DMXAA potently and specifically activates the TBK1-IRF-3 signaling axis.
Roberts ZJ, et al. J Exp Med. 2007 Jul 9;204(7):1559-69. PMID: 17562815.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: DMXAA, Vadimezan, ASA404 supplier, VEGFR/PDGFR, inhibitors

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