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1mg |
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Purity: ≥98%
Vadimezan (DMXAA, NSC-640488, AS1404, ASA-404) is a potent vascular disrupting agents (VDA) and competitive inhibitor of DT-diaphorase with potential antitumor activity. It inhibits VDA and DT-diaphorase with Ki of 20 μM and IC50 of 62.5 μM in cell-free assays, respectively.
ln Vitro |
Vadimezan (DMXAA) is a strong inducer of type I interferons and other cytokines, a vascular disruptor, and a mouse agonist of stimulator of interferon genes (STING). There is no negative impact on the viability of 344SQ-ELuc cells by vadimezan (DMXAA). Research has revealed that Vadimezan-mediated activation of the NF-κB pathway is indicated by enhanced p65 phosphorylation in M2 macrophages [1]. The findings demonstrated that Vadimezan (DMXAA)-treated cells were shielded from VSV-induced cytotoxicity at all MOIs in contrast to medium-pretreated macrophages. Two influenza virus strains were successfully suppressed by vadimezan (DMXAA), indicating the drug's potential to treat drug-resistant strains of human influenza [2].
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ln Vivo |
Vadimezan (DMXAA) significantly reduces bioluminescence (BLI) signals in 344SQ-ELuc NSCLC subcutaneous tumors after injection. When vadimezan (DMXAA) is administered to 344SQ-ELuc metastases, photon emission rates do not drop and the tumors retain their histological resemblance to controls. When mice with tiny subcutaneous tumors are administered Vadimezan (DMXAA), photon output falls by approximately 2 logarithmic units at 6 and 24 hours, just like with large subcutaneous tumors [1]. When administered intraperitoneally to influenza-infected mice, Vadimezan (DMXAA) is a substantially less powerful inducer of IFN-β mRNA and a rather poor inducer of TNF-α mRNA in vivo[2].
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Animal Protocol |
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References |
[1]. Downey CM, et al. DMXAA causes tumor site-specific vascular disruption in murine non-small cell lung cancer, and like the endogenous non-canonical cyclic dinucleotide STING agonist, 2'3'-cGAMP, induces M2 macrophage repolarization. PLoS One. 2014 Jun 18;9
[2]. Shirey KA, et al. The anti-tumor agent, 5,6-dimethylxanthenone-4-acetic acid (DMXAA), induces IFN-beta-mediated antiviral activity in vitro and in vivo. J Leukoc Biol. 2011 Mar;89(3):351-7 |
Molecular Formula |
C17H14O4
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Molecular Weight |
282.29
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CAS # |
117570-53-3
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Related CAS # |
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SMILES |
O=C(O)CC1=CC=CC(C2=O)=C1OC3=C2C=CC(C)=C3C
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Chemical Name |
(5,6-Dimethyl-9-oxo-9H-xanthen-4-yl)-acetic acid
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Synonyms |
NSC 640488, NSC-640488, NSC640488, ASA-404, Vadimezan; ASA404; ASA 404; AS1404; AS 1404; AS1404; DMXAA
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.71 mg/mL (2.52 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 7.1 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 0.71 mg/mL (2.52 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 7.1 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 30% PEG400+0.5% Tween80+5% propylene glycol:30 mg/mL Solubility in Formulation 4: 5 mg/mL (17.71 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.5425 mL | 17.7123 mL | 35.4246 mL | |
5 mM | 0.7085 mL | 3.5425 mL | 7.0849 mL | |
10 mM | 0.3542 mL | 1.7712 mL | 3.5425 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT01299415 | Terminated | Drug: Vadimezan™ | Solid Tumors | Novartis Pharmaceuticals | August 2009 | Phase 1 |
NCT01285453 | Completed | Drug: vadimezan | Advanced or Recurrent Solid Tumors | Novartis Pharmaceuticals | March 2009 | Phase 1 |
NCT01290380 | Terminated | Drug: ASA404, DMXAA, DXAA | Solid Tumor Malignancies | Novartis Pharmaceuticals | February 2010 | Phase 1 |
NCT01299701 | Terminated | Drug: ASA404 | Advanced Solid Tumors | Novartis Pharmaceuticals | December 2008 | Phase 1 |
DMXAA inhibits influenza A/Wuhan and Tamiflu®-resistant influenza A/Br replication in vitro.J Leukoc Biol.2011 Mar;89(3):351-7. td> |
Differential induction of IFN-β and TNF-α mRNA expression by DMXAA and LPS in vivo.J Leukoc Biol.2011 Mar;89(3):351-7. td> |
IFN-β-dependent, DMXAA-mediated protection of mice against influenza-induced lethality.J Leukoc Biol.2011 Mar;89(3):351-7. td> |