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Alectinib

艾乐替尼,AF-802,RG-7853,AF 802,RG 7853,AF802,RG7853

Alectinib (CH5424802)是一种有效的ALK抑制剂,IC50为1.9 nM,对L1196M突变型敏感,作用于ALK比PF-02341066, NVP-TAE684和PHA-E429选择性高。

目录号
EY1275
EY1275
EY1275
纯度
99.25%
99.25%
99.25%
规格
5 mg
10 mg
50 mg
原价
500
800
2000
售价
500
800
2000
库存
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    Alectinib is a highly selective, orally active and potent ALK inhibitor with IC50 of 1.9 nM.

  • 体外研究

  • 体内研究

    30% PEG400+0.5% Tween80+5% propylene glycol

  • 激酶实验

  • 细胞实验

    0-1 μM

  • 动物实验

    20 mg/kg 口服处理

  • 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 AKm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] Sakamoto H, et al. Cancer Cell. 2011, 19(5), 679-690.

    分子式
    C30H34N4O2
    分子量
    482.62
    CAS号
    1256580-46-7
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    0.5 mg/mL with gentle warming
    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
    NCT02521051 Non-Small Cell Lung Cancer (NSCLC) Drug: Alectinib|Drug: Bevacizumab Massachusetts General Hospital|Genentech, Inc. Phase 1|Phase 2 2015-10-01 2016-09-12
    NCT02075840 Non-Small Cell Lung Cancer Drug: Alectinib|Drug: Crizotinib Hoffmann-La Roche Phase 3 2014-08-01 2017-02-23
    NCT02838420 Anaplastic Lymphoma Kinase-positive Non-small Cell Lung Cancer Drug: Alectinib|Drug: Crizotinib Hoffmann-La Roche Phase 3 2016-08-01 2016-11-01
    NCT02621047 Hepatic Impairment Drug: Alectinib Hoffmann-La Roche Phase 1 2015-12-01 2017-02-21
    NCT01984229 Healthy Volunteer Drug: Alectinib|Drug: Posaconazole Hoffmann-La Roche Phase 1 2013-12-01 2016-08-16
    NCT02023125 Healthy Volunteer Drug: Alectinib|Drug: Esomeprazole|Other: High Fat and Calorie Meal|Other: Standard Meal Hoffmann-La Roche Phase 1 2013-12-01 2016-08-16
    NCT02604342 Non-small Cell Lung Cancer Drug: Alectinib|Drug: Docetaxel|Drug: Pemetrexed Hoffmann-La Roche Phase 3 2015-11-03 2017-03-14
    NCT02271139 Non-Small Cell Lung Cancer Drug: Alectinib Genentech, Inc. null 2017-03-07
    NCT02013219 Non-Small Cell Lung Cancer Drug: Alectinib|Drug: Atezolizumab [TECENTRIQ]|Drug: Erlotinib Hoffmann-La Roche Phase 1 2014-04-03 2017-03-17
    NCT01871805 Non-Small Cell Lung Cancer Drug: RO5424802|Drug: RO5424802 Hoffmann-La Roche Phase 2 2013-09-01 2016-07-01
    NCT01981005 Healthy Volunteer Drug: RO5424802 Hoffmann-La Roche Phase 1 2013-11-01 2016-11-01
    NCT01940510 Healthy Volunteer Drug: RO5424802|Drug: rifampin Hoffmann-La Roche Phase 1 2013-10-01 2016-11-01
    NCT02074553 Healthy Volunteer Drug: Part 1 (Fasted): Treatment A|Drug: Part 1 (Fasted): Treatment B|Drug: Part 1 (Fasted): Treatment C|Drug: Part 1 (Fasted): Treatment D|Drug: Part 2 (Fed): Treatment A|Drug: Part 2 (Fed): Treatment B|Drug: Part 2 (Fed): Treatment C|Drug: Part 2 (Fed): Treatment D Hoffmann-La Roche Phase 1 2014-02-01 2016-08-25
    NCT01588028 ALK-Rearranged Non-Small Cell Lung Cancer Drug: CH5424802 Hoffmann-La Roche Phase 1 2012-04-01 2014-10-16
    NCT01801111 Non-Squamous Non-Small Cell Lung Cancer Drug: erlotinib [Tarceva]|Drug: RO5452802 Hoffmann-La Roche Phase 2 2013-06-01 2016-04-11
    NCT02450903 Non-Small-Cell Lung Cancer Drug: LDK378 Novartis Pharmaceuticals|Novartis Phase 2 2015-08-01 2017-02-05
    NCT02314481 Non-small Cell Lung Cancer Drug: MPDL3280A|Drug: Vemurafenib|Drug: Alectinib|Drug: Trastuzumab emtansine University College, London|Hoffmann-La Roche Phase 2 2017-01-01 2016-03-08
    NCT02706626 Non-Small Cell Lung Cancer Drug: brigatinib Criterium, Inc.|University of Colorado, Denver|Duke University|Ariad Pharmaceuticals Phase 2 2017-03-09 2017-03-10
    NCT03087448 Non-small Cell Lung Cancer Drug: Ceritinib|Drug: Trametinib University of California, San Francisco|Novartis Pharmaceuticals|University of California, Davis|University of California, Los Angeles|University of California, San Diego|University of California, Irvine Phase 1|Phase 2 2017-03-01 2017-03-16
    NCT01634763 Tumors Characterized by Genetic Alterations in Anaplastic Lymphoma Kinase (ALK) Drug: LDK378 Novartis Pharmaceuticals|Novartis Phase 1 2012-06-01 2016-07-25

    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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