Identification | Back Directory | [Name]
ATN-224 | [CAS]
649749-10-0 | [Synonyms]
ATN-224 WTX-101) Choline tetrathiomolybdate Bis(choline)tetrathioMolybdate ATN-224
(Choline tetrathiomolybdate CHOLINE TETRATHIOMOLYBDATE;WTX-101;WTX 101;WTX101 bis(sulfanylidene)molybdenum,2-hydroxyethyl(trimethyl)azanium,sulfanide | [Molecular Formula]
C10H28MoN2O2S4 | [MDL Number]
MFCD25976790 | [MOL File]
649749-10-0.mol | [Molecular Weight]
432.542 |
Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:20.0(Max Conc. mg/mL);46.24(Max Conc. mM) DMSO:PBS (pH 7.2):0.5(Max Conc. mg/mL);1.16(Max Conc. mM) | [form ]
A crystalline solid | [color ]
Pink to red | [Water Solubility ]
H2O: ≥0.1mg/mL, clear |
Hazard Information | Back Directory | [Description]
ATN-224 is a choline salt of tetrathiomolybdate and an inhibitor of superoxide dismutase 1 (SOD1; IC50s = 2.91 and 3.51 μM in human and mouse blood cells, respectively, in vitro).1 ATN-224 reduces the viability of cultured oxidative stress-resistant WEHI7.2 murine thymic lymphoma cells (EC50s = 5-6 nM) and human diffuse large B cell lymphoma cell lines (EC50s = 9.73-105.61 nM) independently of Bcl-2 and Bcl-xL.2,3 In vivo, ATN-224 (0.7 mg/kg) chelates copper to stabilize an antitumor viral vector, enhancing its efficacy against lung metastases in mice.4 It also inhibits angiogenesis in a mouse model (IC50s = 1.50-3 mg/kg via gavage).1 | [Uses]
ATN-224 is an oral Cu2+/Zn2+-superoxide dismutase 1 (SOD1) inhibitor. ATN-224 inhibits SOD1 activity in endothelial cells, an effect that is dose dependent with an IC50 of 17.5±3.7 nM. | [in vivo]
ATN-224 also significantly (P<0.05) inhibits angiogenesis in the Matrigel plug model in mice either when added directly to the plug or when given by oral gavage. Inhibition of angiogenesis when ATN-224 is given by oral gavage occurred before there is measurable depletion of copper in either plasma or copper from the Matrigel plug. This result shows that ATN-224 inhibits angiogenesis independently of copper depletion[1]. | [References]
[1] Juarez JC, et al. Copper binding by tetrathiomolybdate attenuates angiogenesis and tumor cell proliferation through the inhibition of superoxide dismutase 1. Clin Cancer Res. 2006 Aug 15;12(16):4974-82. DOI:10.1158/1078-0432.CCR-06-0171 [2] Lin J, et al. A non-comparative randomized phase II study of 2 doses of ATN-224, a copper/zinc superoxide dismutase inhibitor, in patients with biochemically recurrent hormone-na?ve prostate cancer. Urol Oncol. 2013 Jul;31(5):581-8. DOI:10.1016/j.urolonc.2011.04.009 |
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BOC Sciences
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DC Chemicals
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