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Vadimezan (DMXAA)

Cat. No. M1999
Vadimezan (DMXAA) Structure
Synonym:

ASA404; DMXAA

Size Price Availability Quantity
5mg USD 90  USD90 In stock
10mg USD 122  USD122 In stock
50mg USD 480  USD480 In stock
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Quality Control & Documentation
Biological Activity

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.

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.
Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Buchanan CM, et al. Clin Sci (Lond). DMXAA (Vadimezan, ASA404) is a multi-kinase inhibitor targeting VEGFR2 in particular.

[2] McKeage MJ, et al. Br J Cancer. Randomised phase II study of ASA404 combined with carboplatin and paclitaxel in previously untreated advanced non-small cell lung cancer.

[3] Roberts ZJ, et al. J Exp Med. The chemotherapeutic agent DMXAA potently and specifically activates the TBK1-IRF-3 signaling axis.

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Keywords: Vadimezan (DMXAA), ASA404; DMXAA supplier, STING, inhibitors, activators


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