Home > EGFR & EGFR & EGFR & > Gefitinib

Gefitinib

吉非替尼,吉菲替尼,格非替尼,ZD1839

Gefitinib (ZD1839)是一种EGFR酪氨酸激酶和Akt磷酸化抑制剂，作用于NR6wtEGFR和NR6W细胞中的Tyr1173， Tyr992， Tyr1173和Tyr992时，IC50分别为37 nM， 37nM， 26 nM和57 nM。

目录号
EY0917
EY0917
EY0917
EY0917
纯度
99.33%
99.33%
99.33%
99.33%
规格
10 mg
50 mg
100 mg
500 mg
原价
180
300
500
920
售价
180
300
500
920
库存
现货
现货
现货
现货
订购
订购
订购
订购
订购
订购
具体折扣请咨询客服

  • 生物活性

    Gefitinib is an epidermal growth factor receptor (EGFR)-tyrosine kinase inhibitor and has been shown to increase phosphorylation of c-Jun NH2-terminal kinase (JNK) and p38 mitogen-activated protein kinase (MAPK) in HaCaT cells. Selective inhibitor of EGFR tyrosine kinase (IC50 = 23 - 79 nM). Shows minimal activity against ErbB2, KDR, c-flt, PKC, MEK and ERK-2. Blocks EGFR autophosphorylation and inhibits tumor growth in mice bearing a range of human xenografts. Studies suggest that gefitinib can enhance keratinocyte apoptosis via an EGFR-independent JNK-activation pathway. Research indicates that gefitinib can induce apoptosis in several cell lines including, HaCaT cells, KG-1, P39, and primary CD34+ myeloblasts.

  • 体外研究

  • 体内研究

    0.5% methylcellulose+0.2% Tween 80

  • 激酶实验

  • 细胞实验

    0 μM -2 μM

  • 动物实验

    75 mg/kg 饲喂处理

  • 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] Pedersen MW, et al. Br J Cancer. 2005, 93(8), 915-923.
    [2] Galetti, M., et al. 2010. Biochem. Pharmacol. 80: 179-187.
    [3] Lu, P.H., et al. 2010. Br J Dermatol.
    [4] Okamoto, K. et al. 2010. Cancer Res. 70(24): 10402-10410.

    分子式
    C22H24ClFN4O3    		 分子量
    446.9    		 CAS号
    184475-35-2    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    89 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    4 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
    NCT00824746 Carcinoma, Non-Small-Cell Lung Drug: Gefitinib retreatment Chonnam National University Hospital|AstraZeneca Phase 2 2009-01-01 2013-01-22
    NCT00809237 Non-small Cell Lung Cancer Drug: Gefitinib, Hydroxychloroquine National University Hospital, Singapore|Massachusetts General Hospital|AstraZeneca Phase 1|Phase 2 2008-11-01 2013-12-08
    NCT01510990 Non-small Cell Lung Cancer Drug: Gefitinib Asan Medical Center|AstraZeneca Phase 2 2012-04-01 2013-01-26
    NCT00372515 Non-Small Cell Lung Cancer Drug: Gefitinib David M. Jackman, MD|AstraZeneca|Massachusetts General Hospital|Dana-Farber Cancer Institute Phase 1 2006-06-01 2014-10-20
    NCT00212108 Nasopharyngeal Carcinoma Drug: celecoxib, gefitinib National University Hospital, Singapore|National Healthcare Group, Singapore Phase 1|Phase 2 2003-11-01 2012-03-29
    NCT00986284 Non Small Cell Lung Cancer Drug: gefitinib Tianjin Medical University Cancer Institute and Hospital Phase 2 2009-09-01 2015-12-21
    NCT01833572 Non-small-cell Lung Cancer Drug: Gefitinib Fudan University Phase 2 2013-05-01 2013-05-27
    NCT02282267 Lung Adenocarcinoma Drug: Gefitinib Beijing Cancer Hospital 2014-10-01 2017-02-22
    NCT02804776 Non-small Cell Lung Cancer Drug: Gefitinib National Cancer Centre, Singapore Phase 2 2015-02-01 2016-06-14
    NCT01530334 Lung Cancer Drug: Gefitinib 250mg AstraZeneca Phase 2 2012-07-01 2016-01-26
    NCT01933347 Non Small Cell Lung Cancer Drug: Gefitinib Guangdong Association of Clinical Trials Phase 2 2014-04-07 2017-02-23
    NCT00770588 Non-small Cell Lung Cancer (NSCLC) Drug: Gefitinib|Drug: Placebo AstraZeneca Phase 4 2008-09-01 2016-01-15
    NCT00071994 Adult Primary Hepatocellular Carcinoma|Advanced Adult Primary Liver Cancer|Localized Unresectable Adult Primary Liver Cancer|Recurrent Adult Primary Liver Cancer Drug: gefitinib|Other: laboratory biomarker analysis National Cancer Institute (NCI) Phase 2 2004-02-01 2013-02-26
    NCT01965275 Self Efficacy|Drug Toxicity Drug: Erlotinib or Gefitinib Anhui Medical University Phase 2 2013-10-01 2015-06-27
    NCT00519077 Head and Neck Neoplasms Drug: Gefitinib University of Chicago|AstraZeneca Phase 2 2005-03-01 2016-06-02
    NCT01498562 Non Small Cell Lung Cancer (NSCLC) Drug: Gefitinib and Nimotuzumab|Drug: Gefitinib Yonsei University Phase 2 2011-12-01 2014-11-26
    NCT00614809 Non-Small Cell Lung Cancer|Brain Metastasis Drug: gefitinib Guangdong Provincial People's Hospital Phase 2 2007-12-01 2008-02-13
    NCT01485809 Squamous Cell Carcinoma of Bronchus Drug: Gefitinib Seoul Veterans Hospital Phase 2 2011-10-01 2011-12-05
    NCT02824458 EGFR Tyrosine Kinase Inhibitors Plus VEGFR Inhibitors Drug: Apatinib|Drug: Gefitinib|Drug: Placebo Sun Yat-sen University Phase 3 2016-06-01 2016-07-06

    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。

  • 相关化合物库

  • 使用AMQUAR产品发表文献后请联系我们

相关推荐

X
  • 联系人 ：
  • 收件地址 ：
  • 电话号码 ：
  • 单位名称 ：
  • 产品货号 ：
  • 产品规格 ：
  • 发票抬头以及单位税号 ：