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细胞凋亡诱导剂 VDA
/ Vadimezan

2,5-己酮可可碱 /Vadimezan {[allProObj[0].p_purity_real_show]}

货号：A140665 同义名： 伐地美生 / DMXAA;ASA-404

DMXAA is an apoptosis inducer with anti-vascular activity. It is mSTING agonist, selective for mouse STING over human STING. It Induces IFN-β and cytokine production from bone marrow-derived dendritic cells.

Vadimezan 化学结构 CAS号：117570-53-3
Vadimezan 化学结构
CAS号：117570-53-3
Vadimezan 3D分子结构
CAS号：117570-53-3
Vadimezan 化学结构 CAS号：117570-53-3
Vadimezan 3D分子结构 CAS号：117570-53-3
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Vadimezan 纯度/质量文件 产品仅供科研

货号：A140665 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

• Nat. Biomed. Eng., 2024, 8, 1412-1424. Ambeed. [ A538667 , A631746 ]
• JMC, 2024. Ambeed. [ A833302 , A475501 , A341986 , A356070 ]
• BMC Cancer, 2024, 24(1): 1415. Ambeed. [ A809692 , A209020 ]
• J. Am. Soc. Mass Spectrom., 2024, 35(12): 3192-3202. Ambeed. [ A166127 , A902473 , A753371 , A961334 , A292945 , A230770 , A300620 , A1114580 , A1159765 , A206238 ]
• PloS One, 2024, 19(11): e0308060. Ambeed. [ A302917 ]
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产品名称 VDA ↓ 其他靶点 纯度
Verteporfin ✔ 98%
Vadimezan ++

DT-diaphorase, Ki: 20 μM

 		98%
Plinabulin 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Vadimezan 生物活性

靶点

  • VDA

    DT-diaphorase, Ki:20 μM
描述 DMXAA is a competitive inhibitor of DT-diaphorase with an IC50 value of 62.5μM and a Ki value of 20μM. DMXAA blocked DT-diaphorase activity in DLD-1 cells with an IC50 value of 49.6μM. It led to approximate 25% inhibition of cytochrome b5 reductase, although the inhibition plateau was between 250μM and 2 mM[1]. DMXAA also showed potent inhibitory effect on vascular endothelial growth factor receptor (VEGFR) tyrosine kinases, as well as other protein kinases including homeodomain-interacting protein kinase 2, casein kinase 2, Haspin, Aurora kinases, PIM kinases, c-FMS, and tropomyosin-receptor kinases. The IC50 values of DMXAA against VEGFR1 and VEGFR2 were 119 and 11μM, respectively. DMXAA at 25μM showed partial anti-angiogenic effect in an embryonic zebrafish model. DMXAA at the concentration of 30μM significantly reduce the VEGF-induced activation of extracellular-signal-regulated kinase in human umbilical vein endothelial cells[2]. In female Wistar rats, a single dose of DMXAA (300mg/kg, i.p.) significantly delayed the growth of NMU-induced primary mammary tumors as compared to vehicle-treated group[3].

Vadimezan 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
HECPP cells 10 ug/mL Function assay 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

Vadimezan 动物研究

Dose Mice: 17.5 mg/kg, 20 mg/kg[3] (i.p.); 30 mg/kg[4] (p.o.)
Rat: 100 mg/kg - 350 mg/kg[5] (i.p.)
Administration i.p., p.o.
Pharmacokinetics
Animal Mice[4]
Dose 30 mg/kg (p.o.)
25 mg/kg (i.p. or i.v.)
Administration p.o.
i.p. or i.v.
Cmax 358 ± 25 μmol/l (p.o.)
570 ± 21 μmol/l (i.p.)
470 ± 12 μmol/l (i.v.)
T1/2 9.2 h (p.o.)
2.7 h (i.p.)
3.3 h (i.v.)
AUC 1392 μmol·h/l (p.o.)
1715 μmol·h/l (i.p.)
1595 μmol·h/l (i.v.)

Vadimezan 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01031212 Tumors Phase 1 Withdrawn(The investigator has... 展开 >> left the institution (UCSF) prior to study start-up) 收起 << June 2013 United States, California ... 展开 >> UCSF Helen Diller Family Comprehensive Cancer Center San Francisco, California, United States, 94115 收起 <<
NCT00662597 Non-Small Cell Lung Cancer Phase 3 Terminated - -
NCT01057342 Lung Cancer Phase 2 Completed - Switzerland ... 展开 >> Saint Claraspital AG Basel, Switzerland, CH-4016 Universitaetsspital-Basel Basel, Switzerland, CH-4031 Istituto Oncologico della Svizzera Italiana - Ospedale San Giovanni Bellinzona, Switzerland, CH-6500 Inselspital Bern Bern, Switzerland, CH-3010 Spitalzentrum Biel Biel, Switzerland, CH-2501 Centre Hospitalier Universitaire Vaudois Lausanne, Switzerland, CH-1011 Kantonsspital Olten Olten, Switzerland, CH-4600 Onkologie Schaffhausen Schaffhausen, Switzerland, CH-8200 Kantonsspital - St. Gallen St. Gallen, Switzerland, CH-9007 Regionalspital Thun, Switzerland, 3600 Kantonsspital Winterthur Winterthur, Switzerland, CH-8400 Klinik Hirslanden Zurich, Switzerland, CH-8032 收起 <<

Vadimezan 参考文献

[1]Phillips RM. Inhibition of DT-diaphorase (NAD(P)H:quinone oxidoreductase, EC 1.6.99.2) by 5,6-dimethylxanthenone-4-acetic acid (DMXAA) and flavone-8-acetic acid (FAA): implications for bioreductive drug development. Biochem Pharmacol. 1999 Jul 15;58(2):303-10.

[2]Buchanan CM, Shih JH, Astin JW, Rewcastle GW, Flanagan JU, Crosier PS, Shepherd PR. DMXAA (Vadimezan, ASA404) is a multi-kinase inhibitor targeting VEGFR2 in particular. Clin Sci (Lond). 2012 May 1;122(10):449-57.

[3]Liu JJ, Ching LM, Goldthorpe M, Sutherland R, Baguley BC, Kirker JA, McKeage MJ. Antitumour action of 5,6-dimethylxanthenone-4-acetic acid in rats bearing chemically induced primary mammary tumours. Cancer Chemother Pharmacol. 2007 Apr;59(5):661-9.

[4]Zhao L, Kestell P, et al. Oral activity and pharmacokinetics of 5,6-dimethylxanthenone-4-acetic acid (DMXAA) in mice. Cancer Chemother Pharmacol. 2002 Jan;49(1):20-6.

Vadimezan 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.54mL

0.71mL

0.35mL

17.71mL

3.54mL

1.77mL

35.42mL

7.08mL

3.54mL

Vadimezan 技术信息

CAS号117570-53-3
分子式C17H14O4
分子量 282.291
别名 伐地美生 ;DMXAA;ASA-404;AS1404;5,6-Dimethylxanthenone-4-acetic Acid;NSC 640488
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C
溶解度

DMSO: 6 mg/mL(21.25 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

IP 2% DMSO+2% Tween80+30% PEG300+water 0.2 mg/mL clear

PO 0.5% CMC-Na 31 mg/mL suspension

Tags: Vadimezan | DMXAA;ASA-404;AS1404;5,6-Dimethylxanthenone-4-acetic Acid;NSC 640488 | 伐地美生 | Apoptosis Inducer | VDA | AmBeed-信号通路专用抑制剂 | Vadimezan 纯度/质量文件 | Vadimezan 亚型比较 | Vadimezan 生物活性 | Vadimezan 细胞研究 | Vadimezan 动物研究 | Vadimezan 临床数据 | Vadimezan 参考文献 | Vadimezan 实验方案 | Vadimezan 技术信息

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