DMXAA (Vadimezan)

製品コードS1537 別名:NSC 640488, ASA-404

DMXAA (Vadimezan)化学構造


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。

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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。
DT-diaphorase [1]
(Cell-free assay)
DT-diaphorase [1]
(Cell-free assay)
20 μM(Ki) 20 μM(Ki)

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]

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human BJ cells NYi2TIFJS3m2b4TvfIlkyqCjc4PhfS=> NULjeXRROjRiaB?= M{CzV2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGJLKGOnbHzzJIFnfGW{IEK0JIhzeyCkeTDNWHQh[XO|YYmsJGNEPTB;NEiuPUDPxE1? MkTHNlQ2OTh{OUW=
HECPP cells M2ro[mZ2dmO2aX;uJIF{e2G7 NVzpbVYyOTBidXevcWw> NGLaSmZC[3SrdnH0bY9vKG:oIF7GMYtieHCjQjDpckBJTUOSUDDj[YxteyCjdDCxNEB2\y:vTB?= NVy3NJB5OTd4MU[xNVQ>


体内試験 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]


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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
細胞試験: [1]
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  • 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.
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  • 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.

溶解度 (25°C)

体外 DMSO 7 mg/mL (24.79 mM)
Water Insoluble
Ethanol Insoluble
体内 順序で溶剤を入れること:
30% PEG400+0.5% Tween80+5% propylene glycol
30 mg/mL

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)で起きる正常な現象ですから、ご安心ください。


分子量 282.29


CAS No. 117570-53-3
in solvent
別名 NSC 640488, ASA-404





マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)


  • マス




貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積


この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 輸入 輸出 )

  • C1



  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):




チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2


マス 濃度 ボリューム 分子量


NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01278758 Terminated Metastatic Cancer Novartis Pharmaceuticals|Novartis March 2010 Phase 1
NCT01290380 Terminated Solid Tumor Malignancies Novartis Pharmaceuticals|Novartis February 2010 Phase 1
NCT01057342 Completed Lung Cancer Swiss Group for Clinical Cancer Research January 2010 Phase 2
NCT01299415 Terminated Solid Tumors Novartis Pharmaceuticals|Novartis August 2009 Phase 1
NCT01285453 Completed Advanced or Recurrent Solid Tumors Novartis Pharmaceuticals|Novartis March 2009 Phase 1
NCT00111618 Completed Prostate Cancer Antisoma Research May 2005 Phase 2



Handling Instructions


  • * 必須



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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID