DMXAA (Vadimezan)

DMXAA (Vadimezan)は一種のVDA(vascular disrupting agents)で、一種のDT-diaphorase競争性的な阻害剤で、無細胞試験でKi値が20 μMで、IC50値が62.5μMです。臨床3期。

価格 在庫  
USD 151 あり
USD 176 あり
USD 466 あり
USD 1222 あり

DMXAA (Vadimezan) 化学構造
分子量: 282.29




  • Compare VDA Inhibitors
  • 研究分野



製品説明 DMXAA (Vadimezan)は一種のVDA(vascular disrupting agents)で、一種のDT-diaphorase競争性的な阻害剤で、無細胞試験でKi値が20 μMで、IC50値が62.5μMです。臨床3期。
ターゲット DT-diaphorase DT-diaphorase
IC50 62.5 μM 20 μM (Ki) [1]
In vitro試験 In DLD-1 human colon carcinoma cells, DMXAA inhibits DT-diaphorase activity without significant effects on the activity of cytochrome b5 reductase and cytochrome P450 reductase. Combination of menadione and DMXAA leads to an increase in the antiproliferative activity of DLD-1 cells. [1] DMXAA, as an antiviral agent, inhibits VSV-induced cytotoxicity and influenza virus replication in RAW 264.7 macrophages. [2] A recent study shows that DMXAA has non-immune-mediated inhibitory effects against several kinase members of VEGFR (vascular endothelial growth factor receptor), such as VEGFR2 signalling in human umbilical vein endothelial cells. [3]
In vivo試験 DMXAA treatment significantly protects C57BL/6J mice infected i.n. with 200 p.f.u. mouse-adapted H1N1 influenza PR8 virus with 60% survival, while the control group only exhibited 20% survival. [2] DMXAA significantly delays tumor growth induced by chemical carcinogen, increases the time to tumor doubling and increases time from treatment to euthanasia. After the treatment of DMXAA, median tumor doubling time, median tumour tripling time and median time from treatment to euthanasia in tumor-bearing animals are increased by approximately 4.4-, 1.8- and 2.7-fold, respectively. [4]
臨床試験 DMXAA is currently in Phase II clinical trials in patients with non-small cell lung cancer.

プロトコル (参考用のみ)

キナーゼアッセイ: [1]

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

細胞アッセイ: [1]

細胞株 DLD-1 and H460 cells
濃度 0-2 mM
反応時間 96 hours
実験の流れ 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.

動物実験: [4]

動物モデル Chemical carcinogen (NMU) is injected into female Wistar rats.
製剤 DMXAA is dissolved in 5% sodium bicarbonate.
投薬量 ≤300 mg/kg
投与方法 Administered via i.p.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)



Download DMXAA (Vadimezan) SDF
分子量 282.29


CAS No. 117570-53-3
保管 3年-20℃
2年-80℃in solvent
別名 NSC 640488, ASA-404
溶解度 (25°C) * In vitro DMSO 7 mg/mL (24.79 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 2-(5,6-dimethyl-9-oxo-9H-xanthen-4-yl)acetic acid



電話番号: +1-832-582-8158 Ext:3月曜日〜金曜日 9:00 AM–5:00 PM (米国中部標準時)


* 必須

Related VDA 阻害剤

  • PX-478 2HCl

    PX-478 2HClは一種の経口活性をしている、選択性的なHIF-1α阻害剤です。臨床1期。

  • Defactinib (VS-6063, PF-04554878)

    Defactinib (VS-6063, PF-04554878)は一種の選択性的で、経口有効なFAK阻害剤です。臨床2期。

  • SU6656

    SU6656は一種の選択性的なSrc家族キナーゼ阻害剤で、Src、Yes、LynとFynに作用する時の IC50値が280 nM、20 nM、130 nMと170 nMにそれぞれ分かれることです。

  • Dasatinib Monohydrate

    Dasatinib Monohydrateは一種の新たで、有効な多ターゲット阻害剤で、Abl、Srcとc-Kitに作用する時のIC50値が1 nM以下、0.8 nMと79 nMにそれぞれ分かれることです。

  • Plinabulin (NPI-2358)

    Plinabulin (NPI-2358)は一種のVDAで、腫瘍細胞の中にチュブリン脱重合に作用する時のIC50値が9.8~18 nMです。臨床 1/2です。

    Features:Synthetic analog of NPI-2350 and greater potentcy than NPI-2350.

  • Verteporfin

    Verteporfinは一種の内皮細胞中のポリフィリン(porphyrin)からの有効な二代目光感作薬(photosensitizing agent)です。

  • Ibrutinib (PCI-32765)

    Ibrutinib (PCI-32765)は一種の有効で、高度選択性的なBTK( Brutons tyrosine kinase)阻害剤で、無細胞試験でIC50値が0.5 nMですが、Bmx、CSK、FGR、BRK及びHCKに適度に作用して、EGFR、Yes、ErbB2とJAK3等に作用する効果が弱いです。

  • Dasatinib

    Dasatinibは一種の新たで、有効な多ターゲット阻害剤で、無細胞試験でAbl、Srcとc-Kitに作用する時のIC50値が1 nM以下、0.8 nMと79 nMにそれぞれ分かれることです。

  • Saracatinib (AZD0530)

    Saracatinib (AZD0530)は一種の有効なSrc阻害剤で、無細胞試験でIC50値が2.7 nMです。Saracatinib (AZD0530)はc-Yes、Fyn、Lyn、Blk、FgrとLckにも活性をしていますが、AblとEGFR (L858RとL861Q)に作用する活性が低いです。臨床2/3期。

    Features:The 1st Src inhibitor to show inhibition of the Src pathway in human tumor tissue.


Tags: DMXAA (Vadimezan)を買う | DMXAA (Vadimezan)供給者 | DMXAA (Vadimezan)を購入する | DMXAA (Vadimezan)費用 | DMXAA (Vadimezan)生産者 | オーダーDMXAA (Vadimezan) | DMXAA (Vadimezan)代理店
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID