GLPBio

ATN-224

Catalog No.: GC18537Purity:>98.00%Synonyms: Bis-Choline Tetrathiomolybdate
COASDSData Sheet
ATN-224, the bis-choline salt of tetrathiomolybdate (TM), is a superoxide dismutase inhibitor and specific, high-affinity copper binder that suppresses CuZn superoxide dismutase 1 (SOD1) activity in blood and endothelial cells, leading to antiangiogenic and antitumour effects.

Die Produkte sind ausschließlich für Forschungszwecke bestimmt. Nicht zur Anwendung am Menschen. Wir verkaufen nicht an Patienten.

ATN-224
Cas No.: 649749-10-0
10mM (in 1mL DMSO)In Stock
$54.00
1
2mgIn Stock
$32.00
1
5mgIn Stock
$49.00
1
10mgIn Stock
$78.00
1
50mgIn Stock
$252.00
1
100mgIn Stock
$403.00
1
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com

Zitate (Citations)

Für dieses Produkt sind derzeit keine Zitate verfügbar. Nachfolgend finden Sie ausgewählte Publikationen, die GlpBio-Produkte zitieren.
  • Nature cover
    Nature
    641, 529–536 (2025)
  • Nature cover
    Nature
    628, 630–638 (2024)
  • Nature cover
    Nature
    632, 686–694 (2024)
  • Nature cover
    Nature
    618, 1017–1023 (2023)
  • Nature cover
    Nature
    610, 366–372 (2022)
  • Cell cover
    Cell
    187(9):2288-2304 (2024)
  • Cell cover
    Cell
    183(7):1867-1883 (2020)
  • Science cover
    Science
    388(6745) (2025)
  • Science cover
    Science
    387(6739) (2025)
  • Science cover
    Science
    387(6734) (2025)
  • Cell Research cover
    Cell Research
    35, 97–116 (2025)
  • Cell Research cover
    Cell Research
    34, 683–706 (2024)
  • Cell Research cover
    Cell Research
    33, 273–287 (2023)
  • Cell Research cover
    Cell Research
    33, 546–561 (2023)
  • Cell Research cover
    Cell Research
    33, 904–922 (2023)
  • Cell Research cover
    Cell Research
    31, 1291–1307 (2021)

Beschreibung (Description)

ATN-224, the bis-choline salt of tetrathiomolybdate (TM), is a superoxide dismutase inhibitor and specific, high-affinity copper binder that suppresses CuZn superoxide dismutase 1 (SOD1) activity in blood and endothelial cells, leading to antiangiogenic and antitumour effects[1-3]. ATN-224 inhibited Fibroblast growth factor-2 (FGF-2)-induced extracellular signal-regulated kinases 1 and 2 (ERK1/2) phosphorylation in a dose-dependent (0, 0.625, 1.25, 2.5, 5, 10μM) and time-dependent (0, 1, 2, 4, 6, 8, 16, 24, 48h) manner with an IC50 between 1.25 and 2.5μM[4].

In vitro, treatment of WEHI7.2 and its variants, namely, hydrogen-peroxide-resistant 200R cells and Bcl-2-overexpressing Hb12 cells, with 0-10nM ATN-224 for 48h decreased the number of viable cells in a concentration-dependent manner, yielding EC50 values of 3.17±0.27, 5.84±0.34, and 5.25±0.32nM, respectively. Concurrently, ATN-224 markedly elevated caspase-3 activity and propidium iodide (PI) uptake in all three cell lines[5]. Treatment of SUDHL-10 cells with 32.71±2.04nM ATN-224 caused a significant drop in mitochondrial membrane potential (ΔΨm) within 12h and a pronounced reduction in Mcl-1 protein levels by 48h[6].

In vivo, in Matrigel plug model female BALB/c nude mice, 500µL 94µM ATN-224, delivered subcutaneously within the Matrigel plug significantly inhibited angiogenesis[4]. In nude mice bearing CAL27 squamous cell carcinoma (SCC) xenografts, daily oral gavage of 0.7mg ATN-224 combined with intratumoral Phosphate-Buffered Saline (PBS) or RAMBO on days 7 and 16 resulted in a significantly smaller average tumor volume in the RAMBO group by day 21 after ATN-224 treatment initiation[7].

References:
[1] Trapp V, Lee K, Doñate F, et al. Redox-related antimelanoma activity of ATN-224. Melanoma Res. 2009;19(6):350-360.
[2] Lowndes SA, Sheldon HV, Cai S, et al. Copper chelator ATN-224 inhibits endothelial function by multiple mechanisms. Microvasc Res. 2009;77(3):314-326.
[3] Doñate F, Juarez JC, Burnett ME, et al. Identification of biomarkers for the antiangiogenic and antitumour activity of the superoxide dismutase 1 (SOD1) inhibitor tetrathiomolybdate (ATN-224). Br J Cancer. 2008;98(4):776-783.
[4] Juarez JC, Betancourt O Jr, Pirie-Shepherd SR, et al. Copper binding by tetrathiomolybdate attenuates angiogenesis and tumor cell proliferation through the inhibition of superoxide dismutase 1. Clin Cancer Res. 2006;12(16):4974-4982.
[5] Lee K, Briehl MM, Mazar AP, et al. The copper chelator ATN-224 induces peroxynitrite-dependent cell death in hematological malignancies. Free Radic Biol Med. 2013;60:157-167.
[6] Lee K, Hart MR, Briehl MM, et al. The copper chelator ATN-224 induces caspase-independent cell death in diffuse large B-cell lymphoma. Int J Oncol. 2014;45(1):439-447.
[7] Yoo JY, Yu JG, Kaka A, et al. ATN-224 enhances antitumor efficacy of oncolytic herpes virus against both local and metastatic head and neck squamous cell carcinoma. Mol Ther Oncolytics. 2015;2:15008.

Protokoll (Protocol)

Cell experiment [1]:

Cell lines

Murine thymic lymphoma WEHI7.2 cells (include 200R and Hb12 cells)

Preparation Method

The Murine thymic lymphoma WEHI7.2 variants include WEHI7.2 cells selected for resistance to hydrogen peroxide (200R) and WEHI7.2 cells overexpressing Bcl-2 (Hb12 cells). For 1 week before each experiment, 200R cells were cultured in medium without H2O2. The number of viable treated cells, relative to control cells, was measured after 48h of ATN-224 treatment in murine cell lines. Absorbance was read at 490nm using a plate reader. The MTS assay was used to determine the estimated EC50 for ATN-224. Viable cell number was also determined by propidium iodide, a membrane-impermeant dye that intercalates with DNA in dying cells, which was measured using a flow cytometer. Ten thousand cells were analyzed per sample. Numbers less than 5% different were considered within the error of the machine after calibration for this assay.

Reaction Conditions

0-10nM; 48h

Applications

In the WEHI7.2 and WEHI7.2 variant cells, nanomolar concentrations of ATN-224 decreased the number of viable cells in a concentration-dependent manner. The EC50 values for the WEHI7.2, Hb12, and 200R cells were 3.17±0.27, 5.84±0.34, and 5.25±0.32nM, respectively. ATN-224 treatment in the WEHI7.2 and WEHI7.2 variant cells resulted in significant increases in caspase 3 activity and propidium iodide (PI) uptake.
Animal experiment [2]:

Animal models

Female BALB/c nude mice

Preparation Method

Cold Matrigel (500μL) was mixed with 800ng/mL FGF-2 or 300ng/mL VEGF and heparin (50μg/mL). Negative control plugs did not contain the proangiogenic factors. The Matrigel mixture was injected s.c. into 4- to 8-week-old female BALB/c nude mice. In some experiments, either ATN-224 (94μmol/L) or water was added directly to the Matrigel plug in the treated and negative control groups, respectively. Animals were sacrificed, and the plugs were recovered 5 days after plug injection. The plugs were then minced and homogenized with a tissue homogenizer, and hemoglobin levels in the plugs were determined using Drabkin's solution.

Dosage form

500μL, 94μmol/L; injected s.c.

Applications

ATN-224 significantly inhibited angiogenesis in the Matrigel plug model in mice, when added directly to the plug.

References:
[1] Lee K, Briehl MM, Mazar AP, et al. The copper chelator ATN-224 induces peroxynitrite-dependent cell death in hematological malignancies. Free Radic Biol Med. 2013;60:157-167.
[2] Juarez JC, Betancourt O Jr, Pirie-Shepherd SR, et al. Copper binding by tetrathiomolybdate attenuates angiogenesis and tumor cell proliferation through the inhibition of superoxide dismutase 1. Clin Cancer Res. 2006;12(16):4974-4982.

Produktdokumente (Product Documents)

Purity:>98.00%Appearance:A solid
COASDSData Sheet

Chemische Eigenschaften (Chemical Properties)

CAS-Nr.
649749-10-0
Synonyme
Bis-Choline Tetrathiomolybdate
Chemischer Name
2-hydroxy-N,N,N-trimethyl-ethanaminium, tetrathioxomolybdate
SMILES
C[N+](C)(C)CCO.C[N+](C)(C)CCO.S=[Mo-2](=S)(=S)=S
Summenformel
C5H14NO.1/2MoS4
Molekulargewicht
432.5
Löslichkeit
DMSO: 20 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml
Lagerung
Store at -20°C
Allgemeine Hinweise
Wählen Sie anhand der Löslichkeitsdaten des Produkts ein geeignetes Lösungsmittel. Aliquotieren Sie die Stammlösung nach der Herstellung, um wiederholte Gefrier-Auftau-Zyklen zu vermeiden.
Verwenden Sie Stammlösungen bei Lagerung bei -80°C innerhalb von 6 Monaten bzw. bei -20°C innerhalb von 1 Monat.
Zur Verbesserung der Löslichkeit das Röhrchen auf 37°C erwärmen und für eine angemessene Dauer beschallen.
Versandbedingungen
Evaluierungsmuster werden mit Kühlakkus versandt. Andere verfügbare Größen werden bei Raumtemperatur oder auf Anfrage mit Kühlakkus versandt.

Rechner (Calculators)Molarität / Verdünnung / Molekulargewicht / Einheitenumrechnung / In-vivo-Formulierung / Löslichkeit

g/mol

Reviews

Review for ATN-224

Rating: 5
  • 5 Star100%
  • 4 Star0%
  • 3 Star0%
  • 2 Star0%
  • 1 Star0%