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Home > Produkt-Liste > Angiogenese > VDA-Inhibitor > DMXAA (Vadimezan) 117570-53-3

DMXAA (Vadimezan) 117570-53-3

Produktbeschreibung


Molekülmasse:
282.29 DMXAA (Vadimezan) ist eine vaskuläre Agenten (VDA) und kompetitiver Inhibitor der DT-Diaphorase mit Ki 20 μm und IC50 von 62,5 μM, bzw. stören. Phase 3.

Biologische Aktivität

In den DLD-1 menschlichen Doppelpunkt-Karzinom-Zellen hemmt DMXAA DT-Diaphorase Aktivität ohne erhebliche Auswirkungen auf die Aktivität der Cytochrom b5-Reduktase und Cytochrom P450-Reduktase. Kombination von Menadion und DMXAA führt zu einer Erhöhung der Antiproliferative Tätigkeit der DLD-1 Zellen. DMXAA, hemmt als Vermittler antivirale VSV-induzierte Zytotoxizität und Grippe-Virus-Replikation in RAW 264.7 Makrophagen. Eine aktuelle Studie zeigt, dass DMXAA immun-vermittelte hemmende Wirkung gegen mehrere Mitglieder der Kinase des VEGFR (vaskulären endothelialen Wachstumsfaktor-Rezeptor), z. B. VEGFR2 Signalisierung in menschlichen Nabelschnur vein endotheliale Zellen.

DMXAA Behandlung schützt deutlich C57BL/6J Mäuse infiziert i.n. mit 200 p.f.u. Maus angepasst H1N1 Influenza PR8-Virus mit 60 % überleben, während die Kontrollgruppe nur 20 % überleben ausgestellt. DMXAA erheblich verzögert Tumorwachstum durch chemische karzinogen induzierten, erhöht die Zeit, um den Tumor zu verdoppeln und erhöht die Zeit zwischen Behandlung und Euthanasie. Nach der Behandlung von DMXAA, Median Tumor Verdoppelung Zeit Median Tumor Trippeln Zeit und mediane Zeit aus der Behandlung gegen die Euthanasie bei Tumor-tragenden Tieren stieg um etwa 4,4-, 1,8 - und 2.7-fold, beziehungsweise.

Protokoll (nur für Referenzzwecke)

Kinaseprobe: [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

Zellenprobe: [1]

Cell lines DLD-1 and H460 cells
Concentrations 0-2 mM
Incubation Time 96 hours
Method 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.

Tierstudie: [4]

Animal Models Chemical carcinogen (NMU) is injected into female Wistar rats.
Formulation DMXAA is dissolved in 5% sodium bicarbonate.
Dosages ≤300 mg/kg
Administration Administered via i.p.
Solubility 30% PEG400/0.5% Tween80/5% propylene glycol, 30 mg/mL
* 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.

Umwandlung von anderes Modell-Tiere, die auf der Grundlage von BSA (Wert basierend auf Daten aus FDA-Leitlinienentwurf)

Species Baboon Dog Monkey Rabbit Guinea pig Rat Hamster Mouse
Weight (kg) 12 10 3 1.8 0.4 0.15 0.08 0.02
Body Surface Area (m2) 0.6 0.5 0.24 0.15 0.05 0.025 0.02 0.007
Km factor 20 20 12 12 8 6 5 3
Animal A (mg/kg) = Animal B (mg/kg) multiplied by Animal B Km
Animal A Km

Beispielsweise um die Dosis von Resveratrol verwendet für eine Maus (22,4 mg/kg) in einer Dosis, die basierend auf der BSA für eine Ratte zu ändern, Multiplizieren von 22,4 mg/kg mit der Km-Faktor für eine Maus, und teilen Sie dann durch die Km-Faktor für eine Ratte. Diese Berechnung ergibt sich eine Ratte Äquivalentdosis für Resveratrol von 11,2 mg/kg.

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

Chemische Informationen

Molecular Weight (MW) 282.29
Formula

C17H14O4

CAS No. 117570-53-3
Storage 3 years -20℃Powder
6 months-80℃in solvent (DMSO, water, etc.)
Synonyms NSC 640488, ASA-404
Solubility (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.
Chemical Name 2-(5,6-dimethyl-9-oxo-9H-xanthen-4-yl)acetic acid
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Produktgruppe : Angiogenese > VDA-Inhibitor

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