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Nilotinib

尼洛替尼,尼罗替尼,AMN-107

Nilotinib (尼洛替尼; AMN-107) 是Bcr-Abl抑制剂，IC50小于30 nM。

目录号
EY1239
EY1239
EY1239
纯度
99.39%
99.39%
99.39%
规格
25 mg
50 mg
100 mg
原价
300
500
800
售价
300
500
800
库存
现货
现货
现货
订购
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  • 生物活性

    Nilotinib (AMN107) is a small molecule Bcr-Abl kinase inhibitor with IC50 less than 30 nM.

  • 体外研究

  • 体内研究

    0.5% methylcellulose+0.2% Tween 80

  • 激酶实验

  • 细胞实验

    1 μM -10 μM

  • 动物实验

    100 mg/kg 口服饲喂

  • 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] Weisberg E, et al. Blood. 2007, 109(5), 2112-2120.
    [2] Golemovic, M., et al. 2005. Clin. Cancer Res. 11: 4941-4947.
    [3] Kantarjian, H., et al. 2006. N. Engl. J. Med. 354: 2542-2551.
    [4] McFarland, K.L., et al. 2009. Cancer Control. 16: 132-140.

    分子式
    C28H22F3N7O    		 分子量
    529.52    		 CAS号
    641571-10-0    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    50 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
    NCT02736149 Pulmonary Arterial Hypertension Drug: ubenimex Eiger BioPharmaceuticals Phase 2 2016-12-01 2017-03-02
    NCT02700529 Lymphedema Drug: ubenimex|Other: placebo Eiger BioPharmaceuticals Phase 2 2016-06-01 2017-03-02
    NCT02664558 Pulmonary Arterial Hypertension Drug: ubenimex|Other: placebo Eiger BioPharmaceuticals Phase 2 2016-04-01 2017-02-06
    NCT01944176 COPD Drug: simvastatin, placebo Mahidol University Phase 3 2013-09-01 2016-03-15
    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT02086487 Myeloid Leukemia, Chronic Drug: Nilotinib 300 mg. King Abdullah International Medical Research Center|Novartis Phase 4 2013-03-01 2017-03-06
    NCT02954978 Parkinson Disease|Parkinsons Disease With Dementia Drug: Placebo Oral Capsule|Drug: Nilotinib 150mg oral capsule [Tasigna]|Drug: Nilotinib 300mg oral capsule [Tasigna] Georgetown University Phase 2 2017-01-01 2017-03-15
    NCT01562847 Chronic Myeloid Leukemia Drug: Nilotinib Seoul St. Mary's Hospital|Novartis Phase 2 2011-07-01 2014-01-10
    NCT00980018 Chronic Myelogenous Leukemia Drug: Nilotinib Novartis Pharmaceuticals|Novartis Phase 4 2009-12-01 2015-04-14
    NCT01316250 Chronic Myelogenous Leukemia Drug: Nilotinib American University of Beirut Medical Center 2010-08-01 2016-07-23
    NCT01698905 Chronic Myeloid Leukemia Drug: nilotinib Novartis Pharmaceuticals|Novartis Phase 2 2012-12-01 2016-11-27
    NCT00976612 Gastrointestinal Stromal Tumors Drug: Nilotinib Asan Medical Center 2009-01-01 2013-07-03
    NCT01856283 Leukemia, Myeloid, Chronic-Phase Drug: Nilotinib 300mg BID Niguarda Hospital Phase 2 2013-03-01 2016-09-20
    NCT01131325 CML|Philadelphia Chromosome Positive (Ph+)|Chronic Myelogenous Leukemia Chronic Phase(CML-CP) Patients With Low Imatinib Trough Levels Drug: nilotinib Novartis Pharmaceuticals|Novartis Phase 4 2010-10-01 2015-10-06
    NCT01810718 Chronic Graft Versus Host Disease Drug: nilotinib Gruppo Italiano Trapianto di Midollo Osseo Phase 1 2011-11-01 2016-07-05
    NCT01690065 Chronic Myeloid Leukemia in Myeloid Blast Crisis|Untreated Adult Acute Myeloid Leukemia Drug: Nilotinib+AD induction Ulsan University Hospital|The Korean Society of Hematology CML working party Phase 2 2012-09-01 2016-05-10
    NCT02947893 Alzheimer's Disease Drug: Placebo Capsule(s) Once a Day by Mouth|Drug: Nilotinib Capsule(s) Once a Day by Mouth Georgetown University Phase 2 2017-01-01 2017-01-17
    NCT01395121 Mucosal Lentiginous Melanoma|Acral Lentiginous Malignant Melanoma Drug: nilotinib Institute of Cancer Research, United Kingdom|Royal Marsden NHS Foundation Trust Phase 2 2009-12-01 2012-05-18
    NCT00788775 Mucosal Lentiginous Melanoma|Acral Melanoma|Melanoma Drug: Nilotinib Dana-Farber Cancer Institute|Brigham and Women's Hospital|Beth Israel Deaconess Medical Center|Massachusetts General Hospital|Novartis Phase 2 2009-01-01 2016-10-16
    NCT01089595 GIST|Metastatic Disease Drug: Nilotinib|Drug: Nilotinib with Imatinib Fox Chase Cancer Center|Novartis Phase 2 2009-02-01 2017-01-25

    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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