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Triciribine

曲西立滨,曲西瑞宾,NSC 154020,VD-0002,vqd-002,API-2

Triciribine是一种DNA合成抑制剂，也抑制Akt和HIV-1，IC50分别为130 nM和20 nM；对PI3K/PDK1没有抑制作用；作用于缺乏腺苷激酶的细胞，活性降低5000倍。

目录号
EY1498
EY1498
EY1498
纯度
99.31%
99.31%
99.31%
规格
1 mg
5 mg
50 mg
原价
300
700
3000
售价
300
700
3000
库存
现货
现货
现货
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  • 生物活性

    Triciribine(API-2; NSC 154020) is a DNA synthesis inhibitor, also inhibits Akt and HIV-1 with IC50 of 130 nM and 20 nM, respectively; does not inhibit PI3K/PDK1; 5000-fold less active in cells lacking adenosine kinase.

  • 体外研究

  • 体内研究

    1% DMSO+30% polyethylene glycol+1% Tween 80

  • 激酶实验

  • 细胞实验

    0-500 μM

  • 动物实验

    1 mg/kg/天腹腔注射，一天一次.

  • 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] Gursel DB, et al, Nero Oncol, 2011, 13(6), 610-621.
    [2] Porcari, A.R., et al. 2000. J. Med. Chem. 43: 2438-2448.
    [3] Yang et al (2004) Akt/protein kinase B signaling inhibitor-2, a selective small molecule inhibitor of Akt signaling with antitumour activity in cancer cells overexpressing Akt. Cancer Res. 64 4394.
    [4] Ptak et al (1998) Phosphorylation of triciribine is necessary for activity against HIV type 1. AIDS Res.Hum.Retroviruses. 14 1315.
    [5] Wotring et al (1990) Dual mechanisms of inhibition of DNA synthesis by triciribine. Cancer Res. 50 4891.

    分子式
    C13H16N6O4    		 分子量
    320.3    		 CAS号
    35943-35-2    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    100 mM    		 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
    NCT00642031 Hematologic Malignancies|Leukemia Drug: Triciribine Prescient Therapeutics, Ltd.|VioQuest Pharmaceuticals Phase 1 2006-08-01 2016-08-06
    NCT00363454 Cancer Drug: Triciribine Phosphate Monohydrate Prescient Therapeutics, Ltd.|VioQuest Pharmaceuticals Phase 1 2006-04-01 2016-08-06
    NCT01719874 Influenza Biological: TCN-032|Biological: Placebo (saline) Theraclone Sciences, Inc. Phase 2 2012-08-01 2012-10-30
    NCT01690468 Ovarian Cancer Drug: Triciribine|Drug: Carboplatin Prescient Therapeutics, Ltd. Phase 1|Phase 2 2014-09-01 2016-09-07
    NCT02930109 Acute Leukemia Drug: PTX-200|Drug: Cytarabine Prescient Therapeutics, Ltd. Phase 1|Phase 2 2016-09-01 2016-10-07
    NCT01390025 Influenza, Human Biological: TCN-032|Biological: Placebo Theraclone Sciences, Inc. Phase 1 2011-09-01 2012-03-30
    NCT01697293 Breast Adenocarcinoma|Estrogen Receptor Positive|HER2/Neu Negative|Recurrent Breast Carcinoma|Stage IIB Breast Cancer|Stage IIIA Breast Cancer|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer|Stage IV Breast Cancer Drug: Cyclophosphamide|Drug: Doxorubicin Hydrochloride|Other: Laboratory Biomarker Analysis|Drug: Paclitaxel|Procedure: Therapeutic Conventional Surgery|Drug: Triciribine Phosphate Albert Einstein College of Medicine, Inc.|National Cancer Institute (NCI) Phase 1|Phase 2 2012-01-01 2016-01-13
    NCT01594437 Cytomegalovirus Infections Biological: TCN-202|Biological: Placebo Theraclone Sciences, Inc. Phase 1 2012-05-01 2014-03-19
    NCT00747565 Cataract Device: Tecnis ZM900 Multifocal Intraocular Lens|Device: CeeOn 911A monofocal IOL Abbott Medical Optics 2004-11-01 2013-02-27
    NCT02860013 Heart Failure Device: Telemedicine Aalborg University 2016-08-01 2016-08-04
    NCT01984840 Pulmonary Disease, Chronic Obstructive Device: Telemedicine Aalborg University 2013-04-01 2016-06-16
    NCT01863290 Hypertension|Substance Abuse|Asthma|Depression Other: Primary care redesign Yale University 2013-05-01 2016-08-23
    NCT01098812 Cataract Device: Tecnis ZCB00 IOL (control)|Device: Toric Intraocular lens Abbott Medical Optics Phase 3 2010-03-01 2013-06-28
    NCT02332005 Diabetic Peripheral Neuropathy Drug: diepalrestat choline|Drug: Placebo NeuromaxBionevia Phase 2|Phase 3 2014-11-01 2016-04-04

    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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