[CAS NO. 117570-53-3]  Vadimezan (ASA404)

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PRODUCTS SPECIFICATIONS [117570-53-3]

Store
Catalog
SLK-S1537
Brand
Selleck
CAS
117570-53-3

DESCRIPTION [117570-53-3]

Overview

MDLMFCD00870555
Molecular Weight282.29
Molecular FormulaC17H14O4
SMILESC(C(O)=O)C1=C2C(C(=O)C=3C(O2)=C(C)C(C)=CC3)=CC=C1

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM3.5425 mL17.7123 mL35.4246 mL
5 mM0.7085 mL3.5425 mL7.0849 mL
10 mM0.3542 mL1.7712 mL3.5425 mL
50 mM---

Description

Vadimezan (ASA404, NSC 640488, DMXAA) is a and competitive inhibitor of with Ki of 20 μM and IC50 of 62.5 μM in cell-free assays, respectively. DMXAA (Vadimezan) is also a agonist with potential antineoplastic activity. DMXAA (Vadimezan) potently induces but relatively low expression in vitro. DMXAA (Vadimezan) has antiviral activity. Phase 3.

Targets

DT-diaphorase [1]
(Cell-free assay)
DT-diaphorase [1]
(Cell-free assay)
20 μM(Ki)20 μM(Ki)

In vitro

In DLD-1 human colon carcinoma cells, DMXAA inhibits DT-diaphorase activity without significant effects on the activity of cytochrome b5 reductase and cytochrome P450 reductase. Combination of menadione and DMXAA leads to an increase in the antiproliferative activity of DLD-1 cells. DMXAA, as an antiviral agent, inhibits VSV-induced cytotoxicity and influenza virus replication in RAW 264.7 macrophages. A recent study shows that DMXAA has non-immune-mediated inhibitory effects against several kinase members of VEGFR (vascular endothelial growth factor receptor), such as VEGFR2 signalling in human umbilical vein endothelial cells.

In vivo

DMXAA treatment significantly protects C57BL/6J mice infected i.n. with 200 p.f.u. mouse-adapted H1N1 influenza PR8 virus with 60% survival, while the control group only exhibited 20% survival. DMXAA significantly delays tumor growth induced by chemical carcinogen, increases the time to tumor doubling and increases time from treatment to euthanasia. After the treatment of DMXAA, median tumor doubling time, median tumour tripling time and median time from treatment to euthanasia in tumor-bearing animals are increased by approximately 4.4-, 1.8- and 2.7-fold, respectively.


Synonyms

9H-Xanthene-4-acetic acid, 5,6-dimethyl-9-oxo-
5,6-Dimethyl-9-oxo-9H-xanthene-4-acetic acid
5,6-Dimethylxanthenone-4-acetic acid
NSC 640488
DMXAA
AS 1404
5,6-Dimethyl-9-oxo-9H-xanthen-4-ylacetic acid
Vadimezan
ASA 404
2-(5,6-Dimethyl-9-oxo-9H-xanthen-4-yl)acetic acid
D5817
2-(5,6-Dimethyl-9-oxoxanthen-4-yl)acetic acid