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网站主页 化工产品目录 生物化工 抑制剂 血管生成(Angiogenesis) VDA 化学产品 2,5-己酮可可碱 伐地美生
  • 伐地美生|T6273

伐地美生|T6273

Vadimezan
117570-53-3
￥415 2mg 起订
￥747 5mg 起订
￥2150 25mg 起订
上海 更新日期：2024-12-02

TargetMol中国（陶术生物）

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邮箱：marketing@targetmol.com

产品详情:

中文名称：
伐地美生
英文名称：
Vadimezan
CAS号：
117570-53-3
品牌：
TargetMol
产地：
美国
保存条件：
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
纯度规格：
≥98%
产品类别：
抑制剂
货号：
T6273

Product Introduction

Bioactivity

名称Vadimezan
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.
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)
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
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]
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度DMSO : 7.5 mg/mL (26.57 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 0.57 mg/mL (2.02 mM), Suspension. Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
关键字Interferon-α/β receptor | Stimulator of Interferon Genes | Vadimezan | Influenza Virus | MITA | TMEM173 | IFNAR | inhibit | Inhibitor | STING | NSC-640488 | MPYS | ERIS | ASA 404 | ASA404 | NSC640488 | Interferon-alpha/beta receptor
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相关库抗癌活性化合物库 | 经典已知活性库 | 已知活性化合物库 | 抗病毒库 | 抗肺癌化合物库 | 药物功能重定位化合物库 | 抗癌临床化合物库 | 表型筛选靶点鉴定库 | 抗癌药物库 | 抗前列腺癌化合物库
伐地美生|||NSC 640488|||DMXAA|||ASA-404|||5,6-Dimethylxanthenone-4-acetic Acid|TargetMol

公司简介

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。 从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。 经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期 (12年)
注册资本 566.2651万人民币
员工人数 100-500人
年营业额 ￥ 1亿以上
经营模式 贸易,试剂,定制,服务
主营行业 化学试剂,生物活性小分子

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