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ATN-224

ATN-224 (Bis(choline)tetrathiomolybdate) 抑制内皮细胞中的 SOD1 活性，这种作用呈剂量依赖性，IC50 为 17.5±3.7 nM。 ATN-224 是一种口服 Cu2+/Zn2+-超氧化物歧化酶 1 (SOD1) 抑制剂。

CAS号

649749-10-0

分子式

C10H28MoN2O2S4

主要靶点

Others

仅限科研使用

Cat No : CM06352

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Synonyms

四硫钼酸二胆碱|Bis(choline)tetrathiomolybdate

验证数据展示

  • CAS No.: 649749-10-0

    ATN-224
    CAS#: 649749-10-0

产品信息

ATN-224 inhibits SOD1 activity in endothelial cells, an effect that is dose dependent with an IC50 of 17.5±3.7 nM. ATN-224 is an oral Cu2+/Zn2+-superoxide dismutase 1 (SOD1) inhibitor.

CAS号 649749-10-0
分子式 C10H28MoN2O2S4
主要靶点 Others
主要通路 其他
分子量 432.56
纯度 99.45%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 四硫钼酸二胆碱|Bis(choline)tetrathiomolybdate

靶点活性

SOD1, in endothelial cells:17.5±3.7 nM

体内活性

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. 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. This result shows that ATN-224 inhibits angiogenesis independently of copper depletion[1].

体外活性

ATN-224 is an orally-available inorganic small molecule that inhibits the copper/zinc-dependent enzyme, superoxide dismutase 1 (Cu/Zn-SOD1), in endothelial and tumor cells[2] amd it is able to inhibit SOD1 activity in endothelial cells, an effect that is dose dependent with an IC50 of 17.5±3.7 nM. ATN-224 inhibits FGF-2-induced ERK1/2 phosphorylation in a dose-dependent and time-dependent manner with an IC50 between 1.25 and 2.5 μM, consistent with the IC50 for the inhibition of proliferation[1], and it inhibits the proliferation of both HUVEC (IC50=1.4±0.3 μM; n=5) and it is also able to inhibit the activity of purified bovine SOD1 with an IC50 of 0.33±0.03 μM after 24 hours of incubation. ATN-224 has a specific and high affinity for copper ions (108 mol/L-1) and shows no binding to calcium, iron, magnesium, zinc, or manganese ions at concentrations up to 1 mM as determined by isothermal titration calorimetry. The SOD1 inhibition by ATN-224 is time dependent, reaching maximal inhibition at ~16 hours. ATN-224 seems to inhibit SOD1 by depleting the enzyme of copper.

溶解度

DMSO:50 mg/mL (115.59 mM),Sonification is recommended.

参考文献

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.
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-naïve prostate cancer. Urol Oncol. 2013 Jul;31(5):581-8.

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