Vadimezan (DMXAA)

别名: ASA404, NSC 640488 中文名称:2,5-己酮可可碱

Vadimezan (DMXAA)是一种vascular disrupting agents (VDA),也是一种DT-diaphorase的竞争性抑制剂,无细胞试验中Ki为20 μM ,IC50为62.5 μM。DMXAA (Vadimezan) 也是一种STING 激动剂,具有潜在的抗肿瘤活性。DMXAA (Vadimezan) 在体外可有效诱导 IFN-βTNF-α 的表达,但对 TNF-α 影响相对较低。DMXAA (Vadimezan)具有抗病毒活性。Phase 3。

Vadimezan (DMXAA) Chemical Structure

Vadimezan (DMXAA) Chemical Structure

CAS: 117570-53-3

规格 价格 库存 购买数量
10mM (1mL in DMSO) 1138.26 现货
5mg 991.09 现货
10mg 1613.58 现货
25mg 3029.34 现货
100mg 7922.67 现货
1g 12039.3 现货
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相关信号通路图

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
MDA-MB-231 Apoptosis assay 24 to 96 uM 48 hrs Induction of apoptosis in human MDA-MB-231 cells assessed as increase in cleaved caspase-3 expression at 24 to 96 uM after 48 hrs by Western blot analysis 28376372
MDA-MB-231 Apoptosis assay 24 to 96 uM 48 hrs Induction of apoptosis in human MDA-MB-231 cells assessed as increase in cleaved PARP level at 24 to 96 uM after 48 hrs by Western blot analysis 28376372
MDA-MB-231 Function assay 24 to 96 uM 48 hrs Decrease in caspase-3 level in human MDA-MB-231 cells at 24 to 96 uM after 48 hrs by Western blot analysis 28376372
MDA-MB-231 Function assay 24 to 96 uM 48 hrs Increase in p53 level in human MDA-MB-231 cells at 24 to 96 uM after 48 hrs by Western blot analysis 28376372
MDA-MB-231 Function assay 24 to 96 uM 48 hrs Decrease in caspase-9 level in human MDA-MB-231 cells at 24 to 96 uM after 48 hrs by Western blot analysis 28376372
MDA-MB-231 Function assay 24 to 96 uM 48 hrs Decrease in MDM2 level in human MDA-MB-231 cells at 24 to 96 uM after 48 hrs by Western blot analysis 28376372
HepG2 Cell cycle arrest assay 0.2 uM 24 hrs Cell cycle arrest in human HepG2 cells assessed as accumulation at S phase at 0.2 uM after 24 hrs by propidium iodide staining-based flow cytometric method relative to control 29129511
HepG2 Apoptosis assay 0.2 uM 24 hrs Induction of apoptosis in human HepG2 cells assessed as increase in cleaved caspase-3 levels at 0.2 uM after 24 hrs by Western blot method 29129511
HepG2 Apoptosis assay 0.2 uM 24 hrs Induction of apoptosis in human HepG2 cells assessed as increase in cleaved caspase-9 levels at 0.2 uM after 24 hrs by Western blot method 29129511
HepG2 Apoptosis assay 0.2 uM 24 hrs Induction of apoptosis in human HepG2 cells assessed as increase in cleaved PARP levels at 0.2 uM after 24 hrs by Western blot method 29129511
HECPP cells Function assay 10 ug/mL Activation of NF-kappaB in HECPP cells at 10 ug/mL 17616114
human BJ cells Cytotoxic assay 24 h Cytotoxicity against human BJ cells after 24 hrs by MTT assay, CC50=48.9 μM 24518295
MCF7 Antiproliferative assay 24 hrs Antiproliferative activity against human MCF7 cells co-treated with pyranoxanthone at 1:1 molar ratio after 24 hrs by MTT assay, IC50 = 11.89 μM. 29129511
MDA-MB-231 Antiproliferative assay 24 hrs Antiproliferative activity against human MDA-MB-231 cells co-treated with pyranoxanthone at 1:1 molar ratio after 24 hrs by MTT assay, IC50 = 12.12 μM. 29129511
K562 Antiproliferative assay 24 hrs Antiproliferative activity against human K562 cells co-treated with pyranoxanthone at 1:1 molar ratio after 24 hrs by MTT assay, IC50 = 19.14 μM. 29129511
HepG2 Antiproliferative assay 24 hrs Antiproliferative activity against human HepG2 cells co-treated with pyranoxanthone at 1:1 molar ratio after 24 hrs by MTT assay, IC50 = 21.25 μM. 29129511
COLO320 Antiproliferative assay 48 hrs Antiproliferative activity against human COLO320 cells after 48 hrs by CCK8 assay, IC50 = 39.5 μM. 28376372
MDA-MB-231 Antiproliferative assay 48 hrs Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by CCK8 assay, IC50 = 48.4 μM. 28376372
MDA-MB-231 Growth inhibition assay 24 hrs Growth inhibition of human MDA-MB-231 cells after 24 hrs by MTT assay, IC50 = 48.42 μM. 29609121
MDA-MB-231 Antiproliferative assay 24 hrs Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay, IC50 = 48.44 μM. 29129511
HepG2 Cell cycle arrest assay 24 hrs Cell cycle arrest in human HepG2 cells assessed as accumulation at S phase co-treated with pyranoxanthone at 1:1 molar ratio after 24 hrs by propidium iodide staining-based flow cytometric method 29129511
HepG2 Apoptosis assay 24 hrs Induction of apoptosis in human HepG2 cells assessed as increase in cleaved PARP levels co-treated with pyranoxanthone at 1:1 molar ratio after 24 hrs by Western blot method 29129511
HepG2 Apoptosis assay 24 hrs Induction of apoptosis in human HepG2 cells assessed as increase in cleaved caspase-3 levels co-treated with pyranoxanthone at 1:1 molar ratio after 24 hrs by Western blot method 29129511
HepG2 Apoptosis assay 24 hrs Induction of apoptosis in human HepG2 cells assessed as increase in cleaved caspase-9 levels co-treated with pyranoxanthone at 1:1 molar ratio after 24 hrs by Western blot method 29129511
HepG2 Apoptosis assay 24 hrs Induction of apoptosis in human HepG2 cells assessed as downregulation of Bcl-xL expression co-treated with pyranoxanthone at 1:1 molar ratio after 24 hrs by Western blot method 29129511
HepG2 Apoptosis assay 24 hrs Induction of apoptosis in human HepG2 cells assessed as upregulation of Bid expression co-treated with pyranoxanthone at 1:1 molar ratio after 24 hrs by Western blot method 29129511
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
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生物活性

产品描述 Vadimezan (DMXAA)是一种vascular disrupting agents (VDA),也是一种DT-diaphorase的竞争性抑制剂,无细胞试验中Ki为20 μM ,IC50为62.5 μM。DMXAA (Vadimezan) 也是一种STING 激动剂,具有潜在的抗肿瘤活性。DMXAA (Vadimezan) 在体外可有效诱导 IFN-βTNF-α 的表达,但对 TNF-α 影响相对较低。DMXAA (Vadimezan)具有抗病毒活性。Phase 3。
特性 DMXAA(ASA404)是DT-心肌黄酶竞争性抑制剂。
靶点
DT-diaphorase [1]
(Cell-free assay)
DT-diaphorase [1]
(Cell-free assay)
20 μM(Ki) 20 μM(Ki)
体外研究(In Vitro)
体外研究活性 在体外, DMXAA(ASA404)抑制纯化的DT-心肌黄酶,IC50为62.5 μM,Ki为20 μM。DMXAA(ASA404)作用于DLD-1人结肠癌细胞, 抑制DT-心肌黄酶活性,IC50为 49.6 μM,而对细胞色素 b5 还原酶和细胞色素P450还原酶没有显著作用效果。[1] DMXAA(ASA404)为抗病毒药物,作用于RAW 264.7巨噬细胞,抑制VSV-诱导的细胞毒性,也抑制流感病毒复制。[2] 最新研究显示DMXAA(ASA404)作用于VEGFR几种激酶成员,如人人脐静脉内皮细胞中的VEGFR2信号,具有非免疫调节的抑制效果。[3]
激酶实验 DT-心肌黄酶活性和酶抑制动力学分析
通过在Beckman DU 650分光光度计上检测细胞色素 c 在 550 nm处减少量而测定纯化的DT-心肌黄酶活性。每组实验含细胞色素c(70 μM), NADH(多种浓度), 纯化的DT-心肌黄酶(0.032 μg),及溶于含0.14% BSA终体积为1 mL Tris–HCl buffer(50 mM, pH 7.4)的维生素K(多种浓度)。加入NADH开始反应。根据反应曲线初始部分(30秒)计算减少率, 结果表示为μmol 减少的细胞色素/min/mg 蛋白,使用21 mM−1 cm−1 摩尔消光系数表示减少的细胞色素c。在室温下进行酶反应,所有反应做三次平行。反应中含有的DMXAA(ASA404) (不同浓度) 用来表示纯化的 DT-心肌黄酶抑制活性,通过改变NADH (维生素K不变)维生素K (NADH不变) 的浓度测定抑制特性。获得Ki值。通过测量对Dicumarol敏感的DCPIP在 600 nm处的减少量而测定DT-心肌黄酶作用于DLD-1细胞的活性收集处于指数生长中期的DLD-1细胞,置于冰冻buffer (Tris–HCl, 25 mM, pH 7.4和 250 mM蔗糖),然后在冰上进行超声处理。酶反应条件为2 mM NADH, 40 μM DCPIP, 溶于含BSA (0.7 mg/mL)终体积为1 mL Tris–HCl (25 mM, pH 7.4) 的 20 μL Dicumarol。使用21 mM−1 cm−1 的摩尔消光系数表示对Dicumarol敏感的 DCPIP减少量。通过 Bradford检测测定蛋白水平。
细胞实验 细胞系 DLD-1和 H460
浓度 0 到2 mM
孵育时间 96 小时
方法 DLD-1人结肠癌和H460人非小细胞肺癌细胞单层培养在RPMI 1640培养基中,培养基中补充胎牛血清 (10%), 丙酮酸钠(2 mM), 青霉素/链霉亲和素 (50 IU mL−1/50 μg mL-1) 及l-谷氨酰胺(2 mM)。在有氧条件下进行MTT 实验和所有其他实验,检测药物敏感性。细胞接种在96孔板上,然后在含5% CO2的环境下温育过夜。完全移除培养基,使用含多种药物浓度的培养基替代。在只有维生素K时,药物处理时间为1小时,然后细胞在Hanks’平衡盐溶液中冲洗两次,然后在每孔中加入200 μL 新鲜RPMI 1640培养基。 在只有DMXAA(ASA404) 存在时,药物处理时间为3小时。 随后温育4天,使用MTT检测测定细胞存活情况。为了DMXAA(ASA404)和维生素K联用,初步建立细胞 ,选择非毒性(细胞存活率>95%)浓度的DMXAA(ASA404)。细胞使用DMXAA(ASA404) (2 mM)先处理2小时,随后移除培养基,使用含抑制剂 (DMXAA(ASA404),持续浓度为2 mM)和维生素K(多种浓度)的培养基更换。再温育7小时,使用Hanks’平衡盐溶液冲洗细胞,再加入生长培养基。
实验图片 检测方法 检测指标 实验图片 PMID
Western blot p-p38 / p38 p-MK2 / pERK / p-JNK 21819972
Growth inhibition assay Cell proliferation 30138430
体内研究(In Vivo)
体内研究活性 DMXAA(ASA404)显著延迟化学致癌物诱导的细胞生长, 提高肿瘤倍增时间,且提高从治疗到安乐死的时间。DMXAA(ASA404)处理携带肿瘤的动物后, 平均肿瘤倍增时间,平均肿瘤变三倍时间,及从治疗到安乐死的平均时间分别提高4.4-, 1.8- 2.7-倍。[4] DMXAA(ASA404)处理显著保护感染200 p.f.u.小鼠适应的H1N1流感 PR8病毒的C57BL/6J小鼠,使存活率达60%, 而对照组存活率只为20%。[2]
动物实验 Animal Models 注射化学致癌物 (NMU)的雌性 Wistar大鼠
Dosages ≤300 mg/kg
Administration 腹腔注射
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00856336 Completed
Refractory Tumors
Antisoma Research
May 2003 Phase 1
NCT00863733 Completed
Solid Tumors
Cancer Research UK|Cancer Society Auckland
May 1996 Phase 1

化学信息&溶解度

分子量 282.29 分子式

C17H14O4

CAS号 117570-53-3 SDF Download Vadimezan (DMXAA) SDF
Smiles CC1=C(C2=C(C=C1)C(=O)C3=CC=CC(=C3O2)CC(=O)O)C
储存条件(自收到货起)

体外溶解度
批次:

7.5%Sodium bicarbonate : 10 mg/mL (35.42 mM)

DMSO : 7 mg/mL ( (24.79 mM) ;DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Water : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

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