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Afatinib

阿法替尼,BIBW2992,BIBW-2992,BIBW 2992

Afatinib (BIBW2992)是一种不可逆EGFR/HER2抑制剂，对EGFR(wt)， EGFR(L858R)， EGFR(L858R/T790M)和HER2均有抑制作用，IC50分别为0.5 nM，0.4 nM，10 nM和14 nM；用于Gefitinib抗性的突变型EGFR (L858R-T790M )时，活性增强100倍。

目录号
EY1739
EY1739
EY1739
纯度
99.31%
99.31%
99.31%
规格
100 mg
250 mg
500 mg
原价
210
420
740
售价
210
420
740
库存
现货
现货
现货
订购
订购
订购
订购
订购
订购
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  • 生物活性

    Afatinib (BIBW2992), an irreversible inhibitor of the ErbB family of tyrosine kinases, downregulates ErbB signalling by binding to the kinase domains of epidermal growth factor receptor (EGFR)/ human epidermal growth factor receptor 2 (HER2) with IC50 of 0.5 nM and 14nM, respectively. Afatinib was shown to suppress EGF-induced phosphorylation of EGFR and cell proliferation in a variety of EGFR-overexpressing and HER2-expressing cell lines such as A431, NIH-3T3-HER2, NCI-N87 and BT-474.

  • 体外研究

  • 体内研究

    0.5% methylcellulose+0.2% Tween 80

  • 激酶实验

  • 细胞实验

    0-10 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 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] Li D, et al. Oncogene, 2008, 27(34), 4702-4711.

    分子式
    C24H25ClFN5O3    		 分子量
    485.94    		 CAS号
    439081-18-2    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    95 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    15 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
    NCT01427478 Head and Neck Squamous Cell Carcinoma Drug: AFATINIB|Drug: Placebo of AFATINIB Centre Leon Berard|Boehringer Ingelheim Phase 3 2011-09-01 2017-02-22
    NCT01415674 Carcinoma, Squamous Cell of Head and Neck Drug: Afatinib UNICANCER Phase 2 2012-01-01 2015-08-31
    NCT02423525 Brain Cancer Drug: Afatinib Santosh Kesari|Boehringer Ingelheim|John Wayne Cancer Institute Phase 1 2016-12-01 2017-03-03
    NCT03083678 Chordoma Drug: Afatinib Leiden University Medical Center|Chordoma Foundation|Boehringer Ingelheim Phase 2 2017-06-01 2017-03-13
    NCT01522768 Esophageal Cancer|Gastric Cancer Drug: Afatinib and Paclitaxel Memorial Sloan Kettering Cancer Center|Boehringer Ingelheim|University of Southern California|Dana-Farber Cancer Institute|United States Department of Defense Phase 2 2012-03-01 2017-02-14
    NCT02511847 Triple Negative Breast Cancer Drug: Afatinib National Taiwan University Hospital Phase 2 2015-08-01 2016-04-14
    NCT01953913 Carcinoma, Non-Small-Cell Lung Drug: Afatinib Boehringer Ingelheim Phase 3 2013-09-01 2017-03-21
    NCT01320280 Refractory Cancer Drug: BIBW 2992 (Afatinib) Universit盲tsklinikum Hamburg-Eppendorf|Boehringer Ingelheim Phase 2 2011-05-01 2013-04-07
    NCT01824823 Head and Neck Squamous Cell Carcinoma Drug: afatinib|Other: placebo ECOG-ACRIN Cancer Research Group|National Cancer Institute (NCI)|Eastern Cooperative Oncology Group Phase 2 2013-07-01 2016-03-04
    NCT02274012 HER-2 Positive Gastric Cancer|Gastrooesophageal Cancer|Esophageal Cancer Drug: Afatinib|Drug: Paclitaxel Columbia University|Boehringer Ingelheim Phase 2 2014-05-29 2017-03-10
    NCT02369484 NSCLC Drug: Afatinib European Thoracic Oncology Platform Phase 2 2015-06-01 2017-01-03
    NCT02514174 Carcinoma, Non-Small-Cell Lung|ErbB Receptors Drug: Afatinib Boehringer Ingelheim Phase 4 2015-08-01 2017-03-07
    NCT02491099 HER2/Neu+ Uterine Serous Carcinoma Drug: Afatinib Yale University|Boehringer Ingelheim Phase 2 2015-06-01 2016-12-01
    NCT02096718 Renal Insufficiency Drug: Afatinib healthy|Drug: Afatinib severe renally impaired|Drug: Afatinib moderate renally impaired Boehringer Ingelheim Phase 1 2014-05-01 2015-12-09
    NCT02625168 Lung Cancer Drug: Afatinib|Drug: Erlotinib The University of Hong Kong Phase 2 2013-01-01 2015-12-06
    NCT02122172 Distal Urethral Cancer|Proximal Urethral Cancer|Recurrent Bladder Cancer|Recurrent Urethral Cancer|Stage III Bladder Cancer|Stage III Urethral Cancer|Stage IV Bladder Cancer|Stage IV Urethral Cancer|Ureter Cancer Drug: afatinib dimaleate|Other: laboratory biomarker analysis University of Chicago|National Cancer Institute (NCI) Phase 2 2013-10-01 2017-03-06
    NCT02629523 Lung Neoplasms|EGFR Gene Mutation Drug: Afatinib Chonnam National University Hospital Phase 2 2016-06-01 2016-07-31
    NCT02208843 Carcinoma, Non-Small-Cell Lung Drug: Afatinib Boehringer Ingelheim Phase 4 2014-10-01 2017-03-08
    NCT01542437 Non-Small Cell Lung Cancer|EGFR|HER-2 Drug: BIBW 2992 Instituto Nacional de Cancerologia de Mexico Phase 2 2012-01-01 2017-03-01
    NCT02364609 Recurrent Non-Small Cell Lung Carcinoma|Stage IIIA Non-Small Cell Lung Cancer|Stage IIIB Non-Small Cell Lung Cancer|Stage IV Non-Small Cell Lung Cancer Drug: Afatinib Dimaleate|Biological: Pembrolizumab University of California, Davis|National Cancer Institute (NCI) Phase 1 2015-09-01 2016-08-30
    NCT01853826 Carcinoma, Non-Small-Cell Lung Drug: afatinib Boehringer Ingelheim Phase 3 2013-07-01 2016-10-03
    NCT01415011 Carcinoma, Non-Small-Cell Lung Drug: Afatinib (BIBW 2992) University College, London|Boehringer Ingelheim Phase 2 2012-12-01 2016-10-26
    NCT01538381 Carcinoma, Squamous Cell of Head and Neck Drug: Afatinib|Other: Observation European Organisation for Research and Treatment of Cancer - EORTC|Boehringer Ingelheim Phase 2 2012-07-01 2016-10-11
    NCT01531764 Carcinoma Breast Stage IV Drug: BIBW 2992 in combination with vinorelbine University of Magdeburg|Boehringer Ingelheim Phase 2 2012-07-01 2013-10-17

    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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