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Tetrathiomolybdate

ATN 224,ATN-224,Bis(choline)tetrathiomolybdate,ATN224,

ATN-224为铜螯合剂，抑制细胞内的SOD1活性（IC50为17.5 nM）。

目录号
EY2012
EY2012
纯度
99.23%
99.23%
规格
2 mg
5 mg
原价
1590
3250
售价
1590
3250
库存
现货
现货
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  • 生物活性

    ATN-224 inhibits superoxide dismutase 1 (SOD1) in tumor and endothelial cells.  The inhibition of SOD1  leads to an increase in the steady-state levels of superoxide anions, resulting in the inhibition of extracellular signal-regulated kinase phosphorylation without apparent induction of apoptosis. ATN-224 can induce cell death in oxidative stress-resistant cells and cells overexpressing Bcl-2 by modulating the cellular redox environment and causing mitochondrial dysfunction. ATN-224 also targets the mitochondria, decreasing both cytochrome c oxidase (CcOX) activity and mitochondrial membrane potential. Treatment of HUVEC with ATN-224 caused increased superoxide levels, phospho-ERK signalling, nuclear NRF1 expression, HO-1 expression and induction of the anti-apoptotic proteins P21, BCL2 and BCLXL.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

  • 不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数


    例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

  • 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] Lee K, et al. The copper chelator ATN-224 induces peroxynitrite-dependent cell death in hematological malignancies. Free Radic Biol Med. 2013 Jul;60:157-67.
    [3] 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.

    分子式
    C10H28MoN2O2S4    		 分子量
    432.56    		 CAS号
    649749-10-0    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    >40 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    <1 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT00150995 Prostate Cancer Drug: Tetrathiomolybdate University of Michigan Cancer Center Phase 2 2001-05-01 2015-01-20
    NCT00195091 Breast Cancer Drug: Tetrathiomolybdate Weill Medical College of Cornell University Phase 2 2003-12-01 2017-01-25
    NCT00189176 Idiopathic Pulmonary Fibrosis Drug: Tetrathiomolybdate University of Michigan|Coalition for Pulmonary Fibrosis Phase 1|Phase 2 2003-03-01 2013-02-05
    NCT01837329 Non-Small Cell Lung Cancer Drug: Tetrathiomolybdate University of Rochester Phase 1 2013-11-01 2016-10-03
    NCT00805805 Primary Biliary Cirrhosis Drug: Tetrathiomolybdate|Other: Placebo University of Michigan|FDA Office of Orphan Products Development Phase 3 2006-04-01 2013-01-25
    NCT00113542 Psoriasis Drug: Tetrathiomolybdate (TM) University of Michigan Phase 2 2004-06-01 2015-05-20
    NCT00352742 Multiple Myeloma Drug: ATN-224 + bortezomib Attenuon Phase 1|Phase 2 2006-06-01 2008-10-27
    NCT00405574 Prostate Cancer Drug: ATN-224 Attenuon|Prostate Cancer Clinical Trials Consortium Phase 2 2006-11-01 2008-01-28
    NCT00176800 Esophageal Carcinoma Drug: Tetrathiomolybdate (TM)|Procedure: Radiation|Procedure: Surgery University of Michigan Cancer Center Phase 2 2001-11-01 2016-07-12
    NCT00383851 Melanoma Drug: ATN-224|Drug: Temozolomide Attenuon Phase 2 2006-09-01 2007-12-04
    NCT00560495 Lung Cancer Drug: ammonium tetrathiomolybdate|Other: immunoenzyme technique|Other: laboratory biomarker analysis|Radiation: Tc 99m sestamibi|Radiation: radiation therapy Roswell Park Cancer Institute|National Cancer Institute (NCI) Phase 1 2007-05-01 2012-02-08
    NCT00006332 Carcinoma, Hepatocellular Drug: Tetrathiomolybdate National Center for Research Resources (NCRR) Phase 2 2005-06-23
    NCT00004339 Wilson Disease Drug: tetrathiomolybdate|Drug: trientine National Center for Research Resources (NCRR)|University of Michigan Phase 3 1994-01-01 2006-05-08
    NCT00176774 Colorectal Carcinoma Drug: Irinotecan|Drug: 5-Fluorouracil|Drug: Leucovorin|Drug: Tetrathiomolybdate University of Michigan Cancer Center Phase 2 2001-02-01 2012-02-05
    NCT00674557 Breast Cancer Drug: SOD1 inhibitor ATN-224|Drug: exemestane|Genetic: protein expression analysis|Genetic: proteomic profiling|Other: laboratory biomarker analysis|Other: pharmacological study Cancer Research UK|National Cancer Institute (NCI) Phase 2 2008-06-01 2013-07-09

    注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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