Vadimezan | DMXAA;ASA-404;AS1404;5,6-Dimethylxanthenone-4-acetic Acid;NSC 640488 | 伐地美生 | Apoptosis Inducer | VDA

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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 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]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

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VDA 亚型比较

产品名称	VDA ↓ ↑	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 K_i 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.
C_max	358 ± 25 μmol/l (p.o.) 570 ± 21 μmol/l (i.p.) 470 ± 12 μmol/l (i.v.)
T_1/2	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

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 <<
NCT00111618	Prostate Cancer	Phase 2	Completed	-	-
NCT00003697	Unspecified Adult Solid Tumor,... 展开 >> Protocol Specific 收起 <<	Phase 1	Completed	-	United Kingdom ... 展开 >> Mount Vernon Hospital Northwood, England, United Kingdom, HA6 2RN 收起 <<
NCT01240642	Metastatic Cancer With Impaire... 展开 >>d Renal Function Metastatic Cancer With Normal Renal Function 收起 <<	Phase 1	Terminated	-	Belgium ... 展开 >> Novartis Investigative Site Charleroi, Belgium Novartis Investigative Site Jette, Belgium Novartis Investigative Site Lambert, Belgium Novartis Investigative Site Wilrijk, Belgium 收起 <<
NCT01071928	Urothelial Carcinoma	Phase 2	Withdrawn(Lack of efficacy of ... 展开 >>experimental treatment) 收起 <<	-	-
NCT00674102	Non-small Cell Lung Cancer	Phase 1	Completed	-	Japan ... 展开 >> Novartis Investigative Site Aichi, Japan Novartis Investigative Site Osaka, Japan Novartis Investigative Site Shizuoka, Japan Novartis Investigative Site Tokyo, Japan 收起 <<
NCT01278849	Histologically-proven and Radi... 展开 >>ologically-confirmed Solid Tumors 收起 <<	Phase 1	Terminated	-	Italy ... 展开 >> Novartis Investigative Site Ancona, AN, Italy, 60126 Novartis Investigative Site Milano, Italy, 2104 New Zealand Novarts Investigative Site Auckland, New Zealand Novartis Investigative Site Wellington, New Zealand 收起 <<
NCT01285453	Advanced or Recurrent Solid Tu... 展开 >>mors 收起 <<	Phase 1	Completed	-	Japan ... 展开 >> Novartis Investigative Site Aichi, Japan Novartis Investigative Site Osaka, Japan 收起 <<
NCT01299701	Advanced Solid Tumors	Phase 1	Terminated	-	New Zealand ... 展开 >> Novartis Investigative Site Grafton, Auckland, New Zealand 收起 <<
NCT01290380	Solid Tumor Malignancies	Phase 1	Terminated	-	United States, Texas ... 展开 >> The University of Texas Science Center at Houston Houston, Texas, United States, 77030 United States, Wisconsin University of Wisconsin & Paul P. Carbone Comprehensive Cancer Center Madison, Wisconsin, United States, 53792 收起 <<
NCT01299415	Solid Tumors	Phase 1	Terminated	-	United States, Indiana ... 展开 >> Univ. of Indiana School of Medicine/Simon Cancer Center Indianapolis, Indiana, United States, 46202 United States, Minnesota Masonic Cancer Center/ Clinical Trials Office Minneapolis, Minnesota, United States, 55455 United States, Missouri Washington University School of Medicine/Siteman Cancer Center St. Louis, Missouri, United States, 63110 United States, Texas Cancer Therapy & Research Center San Antonio, Texas, United States, 78229 收起 <<
NCT00856336	Refractory Tumors	Phase 1	Completed	-	-
NCT00832494	Non-Small Cell Lung Cancer	Phase 1 Phase 2	Completed	-	-
NCT01278758	Metastatic Cancer	Phase 1	Terminated	-	United States, Indiana ... 展开 >> Indiana University Melvin and Bren Simon Cancer Center, Hematology/Oncology Dept. Indiannapolis, Indiana, United States, 46202 United States, Maryland Hematology /Oncology Associates Rockville, Maryland, United States, 20850 United States, Michigan Joseph Ford Cancer Center/Clinical Trials Office, Henry Ford Health System Detroit, Michigan, United States, 48202 United States, Washington Seattle Cancer Care Alliance Seattle, Washington, United States, 98109-1023 收起 <<
NCT00863733	Solid Tumors	Phase 1	Completed	-	-
NCT00738387	Non-Small Cell Lung Cancer	Phase 3	Terminated	-	-

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

Vadimezan 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Vadimezan 质控信息

Vadimezan 生物活性

Vadimezan 细胞研究

Vadimezan 动物研究

Vadimezan 临床研究

Vadimezan 参考文献

Vadimezan 实验方案

Vadimezan 技术信息

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

Vadimezan 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Vadimezan 质控信息

Vadimezan 生物活性

Vadimezan 细胞研究

Vadimezan 动物研究

Vadimezan 临床研究

Vadimezan 参考文献

Vadimezan 实验方案

Vadimezan 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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