Description
DMXAA(ASA404) can inhibit DT-diaphorase with IC50 of 20 uM.
Alias
AS-1404, 5, 6-MeXAA, NSC-640488, Vadimezan
Storage
2 years at -20 centigrade
Synonyms
AS-1404, 5,6-MeXAA, NSC-640488, Vadimezan
Molecular Formula
C17H14O4
Chemical Name
2-(5,6-dimethyl-9-oxo-9H-xanthen-4-yl)acetic acid
Solubility
DSMO 7 mg/mL Water
In vitro
DMXAA is a competitive inhibitor of the enzyme DT-diaphorase (NAD(P)H:Quinone oxidoreductase EC 1.6.99.2) with respect to NADH, with Ki values of 20 microM, respectively. DMXAA partially inhibits cytochrome b5 reductase activity. And DMXAA is an antitumor agent which can halt tumor blood flow and cause hemorrhagic necrosis in transplantable murine tumors. In contrast to lipopolysaccharide, which induces high levels of serum TNF, DMXAA induces greater TNF production in tumors than in the spleen, liver, or serum.
In vivo
A single dose of DMXAA induced a prolonged reduction in the growth of xenografted tumours in animal models.In contrast to most agents, which require multiple dosing for an effect, DMXAA caused almost complete inhibition of bFGF-induced neovascularization of Matrigel implanted in athymic mice after a single administration of drug.
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