Vadimezan (Synonyms: DMXAA; ASA-404)

目录号: HY-10964 纯度: 99.80%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Vadimezan (DMXAA; ASA-404) 是血管破坏剂，是鼠干扰素基因 (STING) 刺激物，也是 I 型 IFN 和其他细胞因子的强效诱导剂。Vadimezan 具有抗流感病毒 H1N1-PR8 的活性。

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Vadimezan Chemical Structure

CAS No. : 117570-53-3

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥990	In-stock
5 mg	￥900	In-stock
10 mg	￥1200	In-stock
20 mg	￥2100	In-stock
50 mg	￥4700	In-stock
100 mg	现货	询价
200 mg		询价
500 mg		询价

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Customer Review

MCE 顾客使用本产品发表的 44 篇科研文献

: Vadimezan purchased from MCE. Usage Cited in: J Neuroinflammation. 2023 Apr 30;20(1):101. [Abstract]; Vadimezan (DMXAA; 20 mg/kg; i.p.; one dose) inhibits morphine-reduced spinal STING fluorescence intensity in mice.

: Vadimezan purchased from MCE. Usage Cited in: J Neuroinflammation. 2023 Apr 30;20(1):101. [Abstract]; Vadimezan (DMXAA; 20 mg/kg; i.p.; daily; two days) significantly upregulates the morphine-induced decreased expression of STING in the spinal dorsal horn of mice.

: Vadimezan purchased from MCE. Usage Cited in: Cell Rep. 2023 Feb 28;42(3):112145. [Abstract]; Vadimezan (DMXAA; 50 µM; 4, 6 h) significantly increases the level of IRG1 in RAW264.7 macrophages.

: Vadimezan purchased from MCE. Usage Cited in: Gastroenterology. 2018 May;154(6):1822-1835.e2. [Abstract]; Expression of IRF3, p-IRF3, p65 and p-p65 in whole pancreatic extract of acute pancreatitis (AP) mice shown by western blot.

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生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Vadimezan (DMXAA; ASA-404), the tumor vascular disrupting agent (tumor-VDA), is a murine agonist of the stimulator of interferon genes (STING) and also a potent inducer of type I IFNs and other cytokines. Vadimezan has anti-influenza virus H1N1-PR8 activities.

IC₅₀ & Target

STING^[1], type I IFNs^[2]

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A549	IC₅₀	> 100 μM Compound: 6, Vadimezan	Cytotoxicity against human A549 cells after 48 hrs by MTT assay Cytotoxicity against human A549 cells after 48 hrs by MTT assay	10.1039/C3MD00372H
A549	IC₅₀	207.6 μM Compound: 1, DMXAA, Vadimezan	Indirect cytotoxicity against human A549 cells co-cultured with mouse RAW264.7 cells after 24 hrs by MTT assay Indirect cytotoxicity against human A549 cells co-cultured with mouse RAW264.7 cells after 24 hrs by MTT assay	[PMID: 24518295]
A549	IC₅₀	345 μM Compound: 1, DMXAA, Vadimezan	Cytotoxicity against human A549 cells after 24 hrs by MTT assay Cytotoxicity against human A549 cells after 24 hrs by MTT assay	[PMID: 24518295]
A549	IC₅₀	91 μM Compound: 1, DMXAA, Vadimezan	Indirect cytotoxicity against human A549 cells co-cultured with human PBMC after 24 hrs by MTT assay Indirect cytotoxicity against human A549 cells co-cultured with human PBMC after 24 hrs by MTT assay	[PMID: 24518295]
Bel-7402	IC₅₀	> 100 μM Compound: 6, Vadimezan	Cytotoxicity against human Bel7402 cells after 48 hrs by MTT assay Cytotoxicity against human Bel7402 cells after 48 hrs by MTT assay	10.1039/C3MD00372H
BeWo	IC₅₀	> 100 μM Compound: 6, Vadimezan	Cytotoxicity against human Bewo cells after 48 hrs by MTT assay Cytotoxicity against human Bewo cells after 48 hrs by MTT assay	10.1039/C3MD00372H
BGC-823	IC₅₀	> 100 μM Compound: 6, Vadimezan	Cytotoxicity against human BGC823 cells after 48 hrs by MTT assay Cytotoxicity against human BGC823 cells after 48 hrs by MTT assay	10.1039/C3MD00372H
BJ	CC₅₀	48.9 μM Compound: 1, DMXAA, Vadimezan	Cytotoxicity against human BJ cells after 24 hrs by MTT assay Cytotoxicity against human BJ cells after 24 hrs by MTT assay	[PMID: 24518295]
COLO 320	IC₅₀	39.5 μM Compound: DMXAA	Antiproliferative activity against human COLO320 cells after 48 hrs by CCK8 assay Antiproliferative activity against human COLO320 cells after 48 hrs by CCK8 assay	[PMID: 28376372]
H69AR	EC₅₀	> 100 μM Compound: 4; DMXAA	Agonist activity at STING in human THP1 Dual cells assessed as IRF reporter activation incubated for 20 hrs by quanti-blue SEAP reporter gene assay Agonist activity at STING in human THP1 Dual cells assessed as IRF reporter activation incubated for 20 hrs by quanti-blue SEAP reporter gene assay	[PMID: 35108011]
H69AR	EC₅₀	> 100 μM Compound: 4; DMXAA	Agonist activity at STING in human THP1-Dual cells assessed as NF-kappaB reporter activation incubated for 20 hrs by quanti-blue SEAP reporter gene assay Agonist activity at STING in human THP1-Dual cells assessed as NF-kappaB reporter activation incubated for 20 hrs by quanti-blue SEAP reporter gene assay	[PMID: 35108011]
HeLa	IC₅₀	> 100 μM Compound: 6, Vadimezan	Cytotoxicity against human HeLa cells after 48 hrs by MTT assay Cytotoxicity against human HeLa cells after 48 hrs by MTT assay	10.1039/C3MD00372H
HepG2	IC₅₀	100.2 μM Compound: DMXAA	Antiproliferative activity against human HepG2 cells after 48 hrs by CCK8 assay Antiproliferative activity against human HepG2 cells after 48 hrs by CCK8 assay	[PMID: 28376372]
HepG2	IC₅₀	100.2 μM Compound: DMXAA	Growth inhibition of human HepG2 cells after 24 hrs by MTT assay Growth inhibition of human HepG2 cells after 24 hrs by MTT assay	[PMID: 29609121]
HepG2	IC₅₀	100.2 μM Compound: DMXAA; D	Antiproliferative activity against human HepG2 cells after 24 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 24 hrs by MTT assay	[PMID: 29129511]
HepG2	IC₅₀	21.25 μM Compound: DMXAA; D	Antiproliferative activity against human HepG2 cells co-treated with pyranoxanthone at 1:1 molar ratio after 24 hrs by MTT assay Antiproliferative activity against human HepG2 cells co-treated with pyranoxanthone at 1:1 molar ratio after 24 hrs by MTT assay	[PMID: 29129511]
HL-60	IC₅₀	> 100 μM Compound: 6, Vadimezan	Cytotoxicity against human HL60 cells after 48 hrs by MTT assay Cytotoxicity against human HL60 cells after 48 hrs by MTT assay	10.1039/C3MD00372H
HT-29	IC₅₀	269.5 μM Compound: 1, DMXAA, Vadimezan	Cytotoxicity against human HT-29 cells after 24 hrs by MTT assay Cytotoxicity against human HT-29 cells after 24 hrs by MTT assay	[PMID: 24518295]
HUVEC	IC₅₀	> 20 μM Compound: 6, Vadimezan	Cytotoxicity against HUVEC assessed as mitochondrial metabolism after 48 hrs by MTT assay Cytotoxicity against HUVEC assessed as mitochondrial metabolism after 48 hrs by MTT assay	10.1039/C3MD00372H
Ishikawa	IC₅₀	> 100 μM Compound: 6, Vadimezan	Cytotoxicity against human Ishikawa cells after 48 hrs by MTT assay Cytotoxicity against human Ishikawa cells after 48 hrs by MTT assay	10.1039/C3MD00372H
K562	IC₅₀	19.14 μM Compound: DMXAA; D	Antiproliferative activity against human K562 cells co-treated with pyranoxanthone at 1:1 molar ratio after 24 hrs by MTT assay Antiproliferative activity against human K562 cells co-treated with pyranoxanthone at 1:1 molar ratio after 24 hrs by MTT assay	[PMID: 29129511]
K562	IC₅₀	57.4 μM Compound: DMXAA	Antiproliferative activity against human K562 cells after 48 hrs by CCK8 assay Antiproliferative activity against human K562 cells after 48 hrs by CCK8 assay	[PMID: 28376372]
K562	IC₅₀	57.44 μM Compound: DMXAA; D	Antiproliferative activity against human K562 cells after 24 hrs by MTT assay Antiproliferative activity against human K562 cells after 24 hrs by MTT assay	[PMID: 29129511]
L02	IC₅₀	< 100 μM Compound: DMXAA	Cytotoxicity against human HL-7702 cells after 48 hrs by CCK8 assay Cytotoxicity against human HL-7702 cells after 48 hrs by CCK8 assay	[PMID: 28376372]
L02	IC₅₀	< 100 μM Compound: DMXAA	Cytotoxicity against human HL-7702 cells after 48 hrs in presence of DMXAA by CCK8 assay Cytotoxicity against human HL-7702 cells after 48 hrs in presence of DMXAA by CCK8 assay	[PMID: 28376372]
L02	IC₅₀	101.3 μM Compound: DMXAA; D	Antiproliferative activity against human HL-7702 cells after 24 hrs by MTT assay Antiproliferative activity against human HL-7702 cells after 24 hrs by MTT assay	[PMID: 29129511]
MCF7	IC₅₀	> 100 μM Compound: 6, Vadimezan	Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay	10.1039/C3MD00372H
MCF7	IC₅₀	11.89 μM Compound: DMXAA; D	Antiproliferative activity against human MCF7 cells co-treated with pyranoxanthone at 1:1 molar ratio after 24 hrs by MTT assay Antiproliferative activity against human MCF7 cells co-treated with pyranoxanthone at 1:1 molar ratio after 24 hrs by MTT assay	[PMID: 29129511]
MCF7	IC₅₀	54.4 μM Compound: DMXAA	Antiproliferative activity against human MCF7 cells after 48 hrs by CCK8 assay Antiproliferative activity against human MCF7 cells after 48 hrs by CCK8 assay	[PMID: 28376372]
MCF7	IC₅₀	54.4 μM Compound: DMXAA	Growth inhibition of human MCF7 cells after 24 hrs by MTT assay Growth inhibition of human MCF7 cells after 24 hrs by MTT assay	[PMID: 29609121]
MCF7	IC₅₀	54.41 μM Compound: DMXAA; D	Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay	[PMID: 29129511]
MDA-MB-231	IC₅₀	12.12 μM Compound: DMXAA; D	Antiproliferative activity against human MDA-MB-231 cells co-treated with pyranoxanthone at 1:1 molar ratio after 24 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells co-treated with pyranoxanthone at 1:1 molar ratio after 24 hrs by MTT assay	[PMID: 29129511]
MDA-MB-231	IC₅₀	48.4 μM Compound: DMXAA	Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by CCK8 assay Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by CCK8 assay	[PMID: 28376372]
MDA-MB-231	IC₅₀	48.42 μM Compound: DMXAA	Growth inhibition of human MDA-MB-231 cells after 24 hrs by MTT assay Growth inhibition of human MDA-MB-231 cells after 24 hrs by MTT assay	[PMID: 29609121]
MDA-MB-231	IC₅₀	48.44 μM Compound: DMXAA; D	Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay	[PMID: 29129511]
NIH3T3	IC₅₀	< 100 μM Compound: DMXAA	Cytotoxicity against mouse NIH/3T3 cells after 48 hrs by CCK8 assay Cytotoxicity against mouse NIH/3T3 cells after 48 hrs by CCK8 assay	[PMID: 28376372]
NIH3T3	IC₅₀	< 100 μM Compound: DMXAA	Cytotoxicity against mouse NIH/3T3 cells after 48 hrs in presence of DMXAA by CCK8 assay Cytotoxicity against mouse NIH/3T3 cells after 48 hrs in presence of DMXAA by CCK8 assay	[PMID: 28376372]
NIH3T3	IC₅₀	67.8 μM Compound: DMXAA; D	Antiproliferative activity against mouse NIH/3T3 cells after 24 hrs by MTT assay Antiproliferative activity against mouse NIH/3T3 cells after 24 hrs by MTT assay	[PMID: 29129511]
SiHa	IC₅₀	> 100 μM Compound: 6, Vadimezan	Cytotoxicity against human SiHa cells after 48 hrs by MTT assay Cytotoxicity against human SiHa cells after 48 hrs by MTT assay	10.1039/C3MD00372H

体外研究
(In Vitro)

Vadimezan (DMXAA) 是一种血管破坏剂，是干扰素基因刺激因子 (STING) 的鼠类激动剂，也是 I 型 IFN 和其他细胞因子的强效诱导剂。Vadimezan 对 344SQ-ELuc 细胞活力没有不利影响。研究发现，Vadimezan 介导 NF-κB 通路上调，表现为 M2 巨噬细胞中 p65 磷酸化增加^[1]。结果表明，与培养基预处理的巨噬细胞相比，Vadimezan 处理的细胞在所有 MOI 下均免受 VSV 诱导的细胞毒性。Vadimezan 可有效抑制两种流感病毒株的生长，表明 Vadimezan 具有治疗耐药性人类流感病毒株的潜力^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

344SQ-ELuc NSCLC 皮下肿瘤对 Vadimezan (DMXAA) 反应显著，注射药物后生物发光 (BLI) 信号明显减少。Vadimezan 治疗 344SQ-ELuc 转移瘤不会导致光子发射率下降，治疗后肿瘤的组织学仍与对照相似。与大型皮下肿瘤一样，向患有小型皮下肿瘤的小鼠施用 Vadimezan 仍会导致 6 小时和 24 小时光子发射减少约 2 个对数^[1]。Vadimezan 是更有效的 IFN-β mRNA 诱导剂，而 TNF-α mRNA 诱导相对较弱。Vadimezan 给药可显著减少流感感染小鼠的体重减轻^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

282.29

Formula

C₁₇H₁₄O₄

CAS 号

117570-53-3

性状

固体

颜色

White to off-white

中文名称

2,5-己酮可可碱；伐地美生

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

溶解性数据

细胞实验：

DMSO 中的溶解度 : 7.14 mg/mL (25.29 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

7.5% sodium bicarbonate 中的溶解度 : 6.67 mg/mL (23.63 mM; 超声助溶)

配制储备液

浓度溶剂体积质量	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

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 0.71 mg/mL (2.52 mM); 澄清溶液

此方案可获得 ≥ 0.71 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 7.1 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

方案一

请依序添加每种溶剂： 50% PEG300 50% Saline
Solubility: 5 mg/mL (17.71 mM); 悬浊液; 超声助溶

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.80%

选择批次：

Data Sheet (648 KB) SDS (537 KB)

COA (194 KB) LCMS (267 KB)

产品使用指南 (1538 KB)

参考文献

[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(6):e99988. [Content Brief]

[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. [Content Brief]

Kinase Assay ^[1]	M2-polarized macrophages are treated with 20 µg/mL Vadimezan (ASA-404) or DMSO vehicle for 30 min. Cells are then lysed and protein denatured in SDS buffer and samples sent for RPPA analysis. Differential abundance of various proteins and/or their phosphorylation status in response to Vadimezan (ASA-404) is assessed^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[2]	RAW 264.7 macrophages are cultured and plated at 1×10⁵ cells/well in a 96-well plate. After overnight incubation at 37°C, cells are treated with medium containing vehicle or Vadimezan (DMXAA) (100 μg/mL). After 6 h, the culture medium is replaced with serum-free DMEM containing VSV at the indicated MOI for 1 h. Cells are then maintained in complete DMEM with 10% FBS. Twenty-four hours later, cells are washed with PBS, fixed with 10% buffered formalin, and rinsed thoroughly with distilled water. Adherent cells are stained with crystal violet^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Male 129/Sv mice (6 to 12 week old) are used in this study. To generate subcutaneous tumors, 5×10⁵ 344SQ-ELuc cells in 100 µL PBS are injected in both posterior flanks of mice. Tumor growth is monitored every 2 to 4 days via BLI. Once tumors are established (day 10 for systemic metastases; day 7 or day 14 for subcutaneous tumors), mice are given 25 mg/kg of Vadimezan (DMXAA), or DMSO vehicle by i.p. injection. BLI is carried out at 6 and 24 hours ^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[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(6):e99988. [Content Brief] [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. [Content Brief]

Vadimezan 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

7.5% sodium bicarbonate / DMSO	1 mM	3.5425 mL	17.7123 mL	35.4246 mL	88.5614 mL
	5 mM	0.7085 mL	3.5425 mL	7.0849 mL	17.7123 mL
	10 mM	0.3542 mL	1.7712 mL	3.5425 mL	8.8561 mL
	15 mM	0.2362 mL	1.1808 mL	2.3616 mL	5.9041 mL
	20 mM	0.1771 mL	0.8856 mL	1.7712 mL	4.4281 mL
DMSO	25 mM	0.1417 mL	0.7085 mL	1.4170 mL	3.5425 mL

Help & FAQs

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Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Vadimezan (Synonyms: DMXAA; ASA-404)

Customer Review

MCE 顾客使用本产品发表的 44 篇科研文献

Vadimezan 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

生物活性

实验参考方法

纯度 & 产品资料

参考文献

摩尔计算器

稀释计算器

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Vadimezan (Synonyms: DMXAA; ASA-404)

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