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Erlotinib HCl

盐酸埃罗替尼,盐酸厄洛替尼,盐酸厄罗替尼,盐酸伊诺替尼,CP358774,NSC 718781,OSI-744 HCl

Erlotinib HCl (OSI-744)是一种EGFR抑制剂，IC50为2 nM，对EGFR的选择性比c-Src或v-Abl高1000倍以上。

目录号
EY0933
EY0933
EY0933
纯度
99.38%
99.38%
99.38%
规格
50 mg
100 mg
500 mg
原价
200
380
800
售价
200
380
800
库存
现货
现货
现货
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  • 生物活性

    Selective inhibition of EGFR tyrosine kinase by erlotinib hydrochloride leads to the disruption of cancer growth and development which include cell migration, proliferation, angiogenesis, and apoptosis. For instance, erlotinib hydrochloride was shown to induce cell apoptosis and G0/G1 cell cycle arrest in hepatocellular cancer cells, Bxpc-3 and PANC-1 cells, thereby enhancing chemosensitivity towards cytostatics。In addition, this product is widely researched and used for the treatment of human advanced non-small cell lung cancer (NSCLC). In pancreatic cancer, erlotinib hydrochloride was also reported to exhibit an anti-tumour effect.

  • 体外研究

  • 体内研究

    15% Captisol

  • 激酶实验

  • 细胞实验

    0.01 μM-10 μM

  • 动物实验

    50 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] Moyer JD, et al. Cancer Res. 1997, 57(21), 4838-4848.
    [2] Ali, S., et al. 2008. Mol. Cancer Ther. 7: 1708-1719.
    [3] Chen, J., et al. 2007. Cancer Chemother. Pharmacol. 59: 651-659.
    [4] Burris, H. and Rocha-Lima, C. 2008. Oncologist. 13: 289-298.

    分子式
    C22H24ClN3O4    		 分子量
    429.9    		 CAS号
    183319-69-9    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    3 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
    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
    NCT00045487 Kidney Cancer Drug: OSI-774 The University of Texas Health Science Center at San Antonio|National Cancer Institute (NCI) Phase 2 2002-06-01 2013-12-09
    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
    NCT00072631 Advanced Non Small Cell Lung Cancer|Failed Prior Chemotherapy Drug: Tarceva (Trademark) (erlotinib HCl, OSI-774) OSI Pharmaceuticals|Astellas Pharma Inc Phase 2 2003-08-01 2015-06-12
    NCT00369512 Cancer Drug: Erlotinib University of Alabama at Birmingham|Genentech, Inc.|OSI Pharmaceuticals Phase 2 2006-08-01 2013-08-06
    NCT00954226 Head And Neck Cancer Drug: Erlotinib M.D. Anderson Cancer Center|OSI Pharmaceuticals Phase 1 2009-08-01 2016-07-13
    NCT00841035 Pancreatic Cancer Drug: erlotinib University of Alabama at Birmingham|OSI Pharmaceuticals Phase 2 2009-02-01 2014-09-29
    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
    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
    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
    NCT00739063 Breast Cancer Drug: Tarceva M.D. Anderson Cancer Center|OSI Pharmaceuticals Phase 2 2008-07-01 2012-02-10
    NCT00144976 Head and Neck Neoplasms Drug: Tarceva Institut Claudius Regaud|Roche Pharma AG 2003-10-01 2015-03-26
    NCT02140333 NSCLC|EGFR Mutation Drug: Erlotinib The First Affiliated Hospital of Guangzhou Medical University Phase 3 2013-08-01 2015-02-11
    NCT00272038 Prostate Cancer Drug: Tarceva Oncology Specialists, S.C. Phase 2 2005-12-01 2013-08-12
    NCT00536861 Non-Small Cell Lung Cancer|Brain Metastases Drug: erlotinib VU University Medical Center Phase 1 2006-05-01 2008-05-27
    NCT00125372 Carcinoma, Non-small-cell Lung Drug: erlotinib (Tarceva) and bexarotene (Targretin) Dartmouth-Hitchcock Medical Center|Ligand Pharmaceuticals|Genentech, Inc. 2005-12-01 2014-07-14
    NCT00301418 Glioblastoma Multiforme|Anaplastic Astrocytoma Drug: Erlotinib Northwell Health|Genentech, Inc. Phase 1|Phase 2 2006-03-01 2016-01-12

    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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