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Erlotinib

埃罗替尼,厄洛替尼,厄罗替尼,伊诺替尼,CP358774,NSC-718781

Erlotinib (厄洛替尼; OSI-744; NSC 718781; R1415) 是EGFR抑制剂，IC50为2 nM，比对人c-Src和v-Abl的抑制性高1000倍以上。

目录号
EY1725
EY1725
EY1725
纯度
99.15%
99.15%
99.15%
规格
50 mg
100 mg
500 mg
原价
220
400
600
售价
220
400
600
库存
现货
现货
现货
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  • 生物活性

    Erlotinib (CP-358,774, OSI-774, Ro 50-8231), is a reversible, ATP-competitive, highly selective, quinazoline inhibitor of purified human EGFR tyrosine kinase (IC50=2 nM) and reduces EGFR autophosphorylation in intact tumor cells (IC50=20 nM). Erlotinib inhibits the proliferation of DiFi human colon tumor cells at submicromolar concentration and blocks cell cycle progression at G1 phase.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    30 nM-20 μM

  • 动物实验

    50 mg/kg 口服给药

  • 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] Moyer JD, et al. Cancer Res. 1997, 57(21), 4838-4848.

    分子式
    C22H23N3O4    		 分子量
    393.44    		 CAS号
    183321-74-6    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    70 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    10 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
    NCT01085838 Myelodysplastic Syndrome Drug: Erlotinib Groupe Francophone des Myelodysplasies|Roche Pharma AG Phase 1|Phase 2 2010-07-01 2016-11-07
    NCT00997334 Non-small Cell Lung Cancer Drug: erlotinib David M. Jackman, MD|Beth Israel Deaconess Medical Center|Brigham and Women's Hospital|Genentech, Inc.|Dana-Farber Cancer Institute Phase 2 2009-12-01 2015-01-12
    NCT00966472 Squamous Cell Carcinoma|Non-Small Cell Lung Cancer Drug: Erlotinib + Rosuvastatin Ottawa Hospital Research Institute|Ozmosis Research Inc. Phase 1 2009-03-01 2015-04-21
    NCT00497224 Cancer|Pancreas Drug: Erlotinib University Health Network, Toronto|OSI Pharmaceuticals Phase 2 2006-11-01 2013-07-08
    NCT01247922 Ependymoma Drug: Erlotinib OSI Pharmaceuticals|Astellas Pharma Inc Phase 2 2011-05-01 2015-12-07
    NCT00954226 Head And Neck Cancer Drug: Erlotinib M.D. Anderson Cancer Center|OSI Pharmaceuticals Phase 1 2009-08-01 2016-07-13
    NCT00369512 Cancer Drug: Erlotinib University of Alabama at Birmingham|Genentech, Inc.|OSI Pharmaceuticals Phase 2 2006-08-01 2013-08-06
    NCT01116336 Cancer of Head and Neck|Neoplasms, Head and Neck Drug: Erlotinib|Dietary Supplement: Green Tea Polyphenon E Emory University|Astellas Pharma Inc|Polyphenon Pharma|National Cancer Institute (NCI) Phase 1 2010-03-01 2016-12-22
    NCT00841035 Pancreatic Cancer Drug: erlotinib University of Alabama at Birmingham|OSI Pharmaceuticals Phase 2 2009-02-01 2014-09-29
    NCT01487265 Non Small Cell Lung Cancer Drug: BKM120 and Erlotinib SCRI Development Innovations, LLC|Novartis Phase 2 2014-03-01 2017-02-13
    NCT02080078 Non-small Cell Lung Cancer|Advanced Solid Malignancies Drug: Theophylline|Drug: Erlotinib AHS Cancer Control Alberta|Cross Cancer Institute Phase 1 2014-09-01 2015-12-31
    NCT00749892 Transitional Cell Carcinoma Drug: Erlotinib Hydrochloride M.D. Anderson Cancer Center|Genentech, Inc. Phase 2 2008-06-01 2016-11-10
    NCT02140333 NSCLC|EGFR Mutation Drug: Erlotinib The First Affiliated Hospital of Guangzhou Medical University Phase 3 2013-08-01 2015-02-11
    NCT01967095 EGFR-Mutant Lung Cancer Drug: erlotinib Memorial Sloan Kettering Cancer Center|Astellas Pharma US, Inc. Phase 1 2013-10-01 2016-11-23
    NCT01069757 Non-small-cell Lung Cancer Drug: ARQ 197 and Erlotinib Kyowa Hakko Kirin Co., Ltd Phase 1 2010-02-01 2017-03-14
    NCT00462995 Non Small Cell Lung Cancer Drug: Erlotinib|Drug: Erlotinib University Health Network, Toronto|Hoffmann-La Roche Phase 2 2006-05-01 2015-05-26
    NCT00536861 Non-Small Cell Lung Cancer|Brain Metastases Drug: erlotinib VU University Medical Center Phase 1 2006-05-01 2008-05-27
    NCT00281021 Carcinoma, Non-Small Cell Lung Drug: Erlotinib plus Digoxin James Graham Brown Cancer Center|University of Louisville Phase 2 2006-02-01 2014-11-06
    NCT01471964 Non-small Cell Lung Cancer Metastatic|Non-small Cell Lung Cancer Recurrent Drug: MLN8237 and Erlotinib Fox Chase Cancer Center|Millennium Pharmaceuticals, Inc. Phase 1|Phase 2 2011-10-20 2017-01-24
    NCT00509431 Brain and Central Nervous System Tumors Drug: Erlotinib + Sirolimus Jonsson Comprehensive Cancer Center|National Cancer Institute (NCI) Phase 1 2006-08-01 2016-02-05
    NCT00654420 Carcinoma, Non-small-cell Lung Drug: Dalotuzumab|Drug: Erlotinib Merck Sharp & Dohme Corp. Phase 2 2008-03-01 2016-10-28
    NCT00476476 Squamous Cell Carcinoma Drug: Erlotinib Dana-Farber Cancer Institute|Genentech, Inc.|Beth Israel Deaconess Medical Center|Brigham and Women's Hospital|Women and Infants Hospital of Rhode Island Phase 2 2006-12-01 2015-04-13
    NCT00977548 Myelodysplastic Syndrome Drug: Erlotinib H. Lee Moffitt Cancer Center and Research Institute|Genentech, Inc. Phase 2 2009-09-01 2013-09-13

    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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