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Apatinib

阿帕替尼,YN968D1,YN 968D1,YN-968D1

Apatinib是一种口服生物有效性的VEGFR2选择性抑制剂,IC50为1 nM。

目录号
EY1242
EY1242
纯度
99.54%
99.54%
规格
5 mg
25 mg
原价
880
1800
售价
880
1800
库存
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    Apatinib (YN968D1)is a potent inhibior of the VEGF signaling pathway with the IC50 value of 1nM for VEGFR-2 in in vitro enzyme experiments.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

    50, 100, 200 mg/kg 口服

  • 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] Tian S, et al. Cancer Sci, 2011, 102(7), 1374-1380.

    分子式
    C25H27N5O4S
    分子量
    493.58
    CAS号
    811803-05-1(1218779-75-9)
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    20 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
    NCT02836821 Neoplasms Drug: Apatinib Mesylate Tablets|Drug: Rifampicin Capsules Jiangsu HengRui Medicine Co., Ltd. Phase 1 2016-05-01 2017-02-23
    NCT02995187 Small Cell Lung Cancer Drug: Apatinib Mesylate tablet Chinese Academy of Medical Sciences Phase 2 2016-12-01 2016-12-14
    NCT02829385 Colorectal Neoplasms Drug: Apatinib and XELOX combined treatment group Shoucheng Ma|LanZhou University Phase 2 2016-06-01 2016-07-11
    NCT02544737 Esophageal Cancer|Metastatic Esophageal Cancer|Apatinib Drug: Apatinib Hangzhou Cancer Hospital Phase 2 2015-09-01 2016-08-25
    NCT02772029 Hepatocellular Carcinoma Drug: Apatinib Mesylate Tablets The First Affiliated Hospital of Zhengzhou University Phase 1|Phase 2 2016-05-01 2016-05-12
    NCT02515435 Non-Small Cell Lung Cancer Drug: apatinib single agent Tongji University Phase 2 2015-01-01 2015-07-31
    NCT02540824 Non-small Cell Lung Cancer Drug: Apatinib single agent arm Tongji University Phase 2 2015-01-01 2015-09-03
    NCT02726854 Pancreatic Neoplasms Drug: Apatinib First Affiliated Hospital Xi'an Jiaotong University Phase 2 2016-04-01 2016-11-30
    NCT03046979 Hepatocellular Carcinoma Drug: Apatinib Tianjin Medical University Cancer Institute and Hospital Phase 2 2016-12-01 2017-02-06
    NCT02836171 Neoplasms Drug: Apatinib Mesylate Tablets|Drug: Itraconazole Capsules Jiangsu HengRui Medicine Co., Ltd. Phase 1 2016-07-01 2017-02-23
    NCT03083041 Carcinoma, Non-Small-Cell Lung Biological: SHR-1210|Drug: Apatinib Jiangsu HengRui Medicine Co., Ltd. Phase 2 2017-03-01 2017-03-13
    NCT02989259 Head and Neck Neoplasms Drug: Apatinib Cancer Institute and Hospital, Chinese Academy of Medical Sciences Phase 2 2016-12-01 2016-12-11
    NCT02485015 Stomach Neoplasms Biological: Cytokine-Induced Killer Cells|Drug: Apatinib The First People's Hospital of Changzhou Phase 2 2015-06-01 2016-02-18
    NCT02493582 Adenocarcinoma of Lung Biological: Cytokine-Induced Killer Cells|Drug: Apatinib The First People's Hospital of Changzhou Phase 2 2015-07-01 2016-02-04
    NCT01653561 Breast Neoplasms Drug: Apatinib Fudan University|Jiangsu HengRui Medicine Co., Ltd. Phase 2 2011-11-01 2013-12-02
    NCT02878057 Breast Cancer Drug: Apatinib Beijing Cancer Hospital|Hebei Medical University Fourth Hospital|Peking University First Hospital|Peking University Third Hospital|Shanxi Province Cancer Hospital Phase 2 2016-05-01 2016-08-24
    NCT03007446 Gastric Cancer Drug: Apatinib|Drug: Oxaliplatin|Drug: S-1 Chinese PLA General Hospital Phase 2 2016-11-01 2016-12-29
    NCT02537171 Gastric Cancer Drug: apatinib The Affiliated Hospital of the Chinese Academy of Military Medical Sciences Phase 3 2015-07-01 2016-08-01
    NCT02711007 Osteosarcoma|Metastasis Drug: apatinib GUO WEI|Peking University People's Hospital Phase 2|Phase 3 2016-03-01 2016-03-16
    NCT02774200 Metastatic Renal Cell Carcinoma Drug: Apatinib Tianjin Medical University Cancer Institute and Hospital Phase 2 2016-05-01 2016-05-12

    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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