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Vadimezan

产品编号 T6273 CAS 117570-53-3

别名: DMXAA, 伐地美生, 5,6-Dimethylxanthenone-4-acetic Acid, NSC 640488, ASA-404

Vadimezan (DMXAA) 是一种血管破坏剂，一种鼠 STING 激动剂，也是一种细胞因子如 I 型 IFN 的诱导剂。Vadimezan 具有抗肿瘤活性，可以诱导肿瘤中的血流快速停止，但不影响正常组织中的血流。

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Vadimezan, CAS 117570-53-3

规格	价格/CNY	货期
2 mg	￥ 415	现货
5 mg	￥ 747	现货
25 mg	￥ 2,150	现货
50 mg	￥ 3,783	现货
100 mg	￥ 4,470	现货
1 mL * 10 mM (in DMSO)	￥ 798	现货

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选择批次

纯度: 99.8%

纯度: 99.36%

纯度: 98.5%

纯度: 97.81%

纯度: 97.38%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Vadimezan (DMXAA) is a vascular disrupting agent, a murine STING agonist, and an inducer of cytokines such as type I IFN. Vadimezan has antitumor activity and induces a rapid cessation of blood flow in tumors without affecting blood flow in normal tissues.
靶点活性	DT diaphorase:20 μM(Ki)
体外活性	方法：DLBCL 细胞 LY1 和 LY3 用 Vadimezan (0-300 µM) 处理 24 h，使用 CCK-8 assay 检测细胞活力。结果：Vadimezan 处理以剂量依赖的方式降低 DLBCL 细胞的活力，对 LY1 和 LY3 的 IC50 分别为 177 μM 和 165 μM。[1] 方法：人肺癌细胞 A549 用 Vadimezan (0.1-1 µM) 处理 24 h，使用 Western Blot 检测靶点蛋白表达水平。结果：Vadimezan 诱导 cytochrome c 的胞浆水平和 caspase 3 的激活显著增加，最终导致 A549 细胞凋亡死亡。[2]
体内活性	方法：为检测体内抗肿瘤活性，将 Vadimezan (20 mg/kg) 和 BMS1166 (250 µg/mL) 腹腔注射给携带 DLBCL 肿瘤 LY1 的 Balb/c nude 小鼠，每天一次，持续八天。结果：Vadimezan 和 BMS1166 在有效浓度下发挥作用。与单药治疗相比，联合治疗显著抑制了 GCB 样 DLBCL 细胞的生长。[1] 方法：为检测体内抗肿瘤活性，将 Vadimezan (25,5,5,25 mg/kg；25,0,0,25 mg/kg；25,25,25,25 mg/kg) 腹腔注射携带小鼠间皮瘤 AE17 的 C57BL/6J 小鼠，每三天一次，给药四次。结果：在第 1 组中，治愈了 2/4 只小鼠，其中 2/4 只显示出长期存活，但观察到了毒性问题。在第 2 组中观察到更好、毒性更小的反应，所有 4 只小鼠均治愈并显示出长期存活。在第 3 组小鼠中，只有 1 只治愈，但没有一只长期存活，可能是由于相关的毒性问题。[3]
激酶实验	DT-diaphorase activity and kinetic analysis of enzyme inhibition : Purified DT-diaphorase enzyme activity is assayed by measuring the reduction of cytochrome c at 550 nm on a Beckman DU 650 spectrophotometer. Each assay contains cytochrome c (70 μM), NADH (variable concentrations), purified DT-diaphorase (0.032 μg), and menadione (variable concentrations) in a final volume of 1 mL Tris–HCl buffer (50 mM, pH 7.4) containing 0.14% BSA. The reaction is started by the addition of NADH. Rates of reduction are calculated over the initial part of the reaction curve (30 seconds), and results are expressed in terms of μmol cytochrome c reduced/min/mg protein using a molar extinction coefficient of 21.1 mM?1 cm?1 for reduced cytochrome c. Enzyme assays are carried out at room temperature and all reactions are performed in triplicate. Inhibition of purified DT-diaphorase activity is performed by the inclusion of DMXAA (at various concentrations) in the reaction, and inhibition characteristics are determined by varying the concentration of NADH (constant menadione) or menadione (constant NADH) at several concentrations of inhibitor. Ki values are obtained by plotting 1/V against. The activity of DT-diaphorase in DLD-1 cells is determined by measuring the dicumarol-sensitive reduction of DCPIP at 600 nm. Briefly, DLD-1 cells in mid-exponential growth are harvested by scraping into ice-cold buffer (Tris–HCl, 25 mM, pH 7.4 and 250 mM sucrose) and sonicated on ice. Enzyme assay conditions are 2 mM NADH, 40 μM DCPIP, 20 μL of dicumarol (when required) in a final volume of 1 mL Tris–HCl (25 mM, pH 7.4) containing BSA (0.7 mg/mL). Results are expressed as the dicumarol-sensitive reduction of DCPIP using a molar extinction coefficient of 21 mM?1 cm?1. Protein levels are determined using the Bradford assay
细胞实验	DLD-1 human colon carcinoma and H460 human non-small cell lung carcinoma cells are routinely maintained as monolayer cultures in RPMI 1640 culture medium supplemented with foetal calf serum (10%), sodium pyruvate (2 mM), penicillin/streptomycin (50 IU mL?1/50 μg mL-1) and l-glutamine (2 mM). Chemosensitivity is assessed using the MTT assay and all assays are performed under aerobic conditions. Briefly, cells are plated into each well of a 96-well culture plate and incubated overnight in an atmosphere containing 5% CO2. Culture medium is completely removed from each well and replaced with medium containing a range of drug concentrations. In the case of menadione alone, the duration of drug exposure is 1 hour, after which the cells are washed twice with Hanks' balanced salt solution prior to the addition of 200 μL fresh RPMI 1640 medium to each well of the plate. In the case of DMXAA alone, the duration of drug exposure is 3 hours. Following a four-day incubation, cell survival is determined using the MTT assay. For combinations of DMXAA with menadione, cells are initially set up and a non-toxic (>95% cell survival) concentration of DMXAA is selected. Cells are then initially exposed to DMXAA (2 mM) for a period of 2 hours, following which the medium is removed and replaced with medium containing the inhibitor (DMXAA at a constant concentration of 2 mM) and menadione (at a range of drug concentrations). Following a further 7-hour incubation, cells are washed twice with Hanks' balanced salt solution prior to the addition of growth medium.(Only for Reference)

别名	DMXAA, 伐地美生, 5,6-Dimethylxanthenone-4-acetic Acid, NSC 640488, ASA-404
分子量	282.29
分子式	C17H14O4
CAS No.	117570-53-3

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 5.7 mg/mL (20 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
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
	20 mM	0.1771 mL	0.8856 mL	1.7712 mL	4.4281 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Cai Y, et al. Activation of STING by SAMHD1 Deficiency Promotes PANoptosis and Enhances Efficacy of PD-L1 Blockade in Diffuse Large B-cell Lymphoma. Int J Biol Sci. 2023 Aug 28;19(14):4627-4643. 2. Pan ST, et al. Proteomic response to 5,6-dimethylxanthenone 4-acetic acid (DMXAA, vadimezan) in human non-small cell lung cancer A549 cells determined by the stable-isotope labeling by amino acids in cell culture (SILAC) approach. Drug Des Devel Ther. 2015 Feb 17;9:937-68. 3. Graham PT, et al. The STING agonist, DMXAA, reduces tumor vessels and enhances mesothelioma tumor antigen presentation yet blunts cytotoxic T cell function in a murine model. Front Immunol. 2022 Nov 18;13:969678. 4. Liu JJ, et al. Cancer Chemother Pharmacol. 2007, 59(5), 661-669. 5. Chen C, Yan W, Zhang Y, et al. ANP Attenuates Intestinal Inflammation by Regulating STING Pathway[J]. Available at SSRN 3756807. 6. Zhao M, Wang B, Zhang C, et al. The DJ1-Nrf2-STING axis mediates the neuroprotective effects of Withaferin A in Parkinson’s disease[J]. Cell Death & Differentiation. 2021: 1-19.

文献引用

1. Zhao M, Wang B, Zhang C, et al. The DJ1-Nrf2-STING axis mediates the neuroprotective effects of Withaferin A in Parkinson’s disease. Cell Death & Differentiation. 2021: 1-19. 2. Chen C, Zhang Y, Tao M, et al. Atrial Natriuretic Peptide Attenuates Colitis via Inhibition of the cGAS-STING Pathway in Colonic Epithelial Cells. International Journal of Biological Sciences. 2022, 18(4): 1737-1754.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Vadimezan 117570-53-3 Angiogenesis Immunology/Inflammation Microbiology/Virology Influenza Virus VDA STING IFNAR Interferon-α/β receptor DMXAA Stimulator of Interferon Genes MITA TMEM173 伐地美生 inhibit 5,6-Dimethylxanthenone-4-acetic Acid Inhibitor NSC 640488 NSC-640488 MPYS ERIS ASA 404 ASA404 NSC640488 Interferon-alpha/beta receptor ASA-404 inhibitor

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Vadimezan

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords