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Icotinib

埃克替尼,BPI-2009H

Icotinib是EGFR抑制剂，对突变型EGFR(L858R)，EGFR(L861Q)，EGFR(T790M)和EGFR(T790M，L858R)的IC50为5 nM。

目录号
EY0756
EY0756
EY0756
纯度
99.52%
99.52%
99.52%
规格
1 mg
5 mg
10 mg
原价
600
1200
1800
售价
600
1200
1800
库存
现货
现货
现货
订购
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  • 生物活性

    Icotinib is a potent and specific EGFR inhibitor with IC50 of 5 nM, including the EGFR, EGFR(L858R), EGFR(L861Q), EGFR(T790M) and EGFR(T790M, L858R).

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    ~25 μM

  • 动物实验

    30, 60 和 120 mg/kg/day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] Tan F, et al. Lung Cancer, 2012, 76(2), 177-182.
    [2] Ye C, Wang J, Zheng S, Chai Y. Effective treatment with icotinib in lung adenocarcinoma with EGFR and ALK co-alterations and brain metastasis. Onco Targets Ther. 2016 Oct 26;9:6605-6608.
    [3] Tang N, Zhang Q, Fang S, Han X, Wang Z. Anti-tumor activity of high-dose EGFR tyrosine kinase inhibitor and sequential docetaxel in wild type EGFR non-small cell lung cancer cell nude mouse xenografts. Oncotarget. 2016 Nov 12.

    分子式
    C22H21N3O4    		 分子量
    391.42    		 CAS号
    610798-31-7    		 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
    >5 mg/mL

    体内溶解度
    30 mg/mL

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT02934256 Vestibular Schwannoma|Neurofibromatosis Type 2 Drug: Icotinib Li Peng|Betta Pharmaceuticals Co.,Ltd.|Beijing Tiantan Hospital Phase 2 2016-07-01 2017-02-07
    NCT01963195 NSCLC Drug: Icotinib Anhui Medical University Phase 2 2013-10-01 2013-10-15
    NCT02375022 Lung Cancer Drug: Endostar and icotinib Zhejiang University|Jiangsu Simcere Pharmaceutical Co., Ltd.|Beta Pharma, Inc. Phase 2 2015-03-01 2015-03-23
    NCT01514877 Lung Cancer|Metastatic Cancer Drug: Icotinib Zhejiang Cancer Hospital Phase 2 2012-01-01 2014-07-22
    NCT01690390 NSCLC Drug: Icotinib of routine dose|Drug: Icotinib of high dose Betta Pharmaceuticals Co.,Ltd. Phase 2 2012-09-01 2014-12-26
    NCT02737774 Lung Adenocarcinoma Drug: Icotinib|Drug: Pemetrexed/Carboplatin Henan Cancer Hospital Phase 2 2016-04-01 2016-04-09
    NCT02062515 Non-small Cell Lung Cancer Drug: icotinib Betta Pharmaceuticals Co.,Ltd. Phase 2 2014-02-01 2015-07-14
    NCT02328261 Nasopharyngeal Carcinoma Drug: Icotinib Betta Pharmaceuticals Co.,Ltd. Phase 2 2014-11-01 2014-12-26
    NCT02961270 Non-small Cell Lung Cancer Drug: Icotinib Chinese Academy of Medical Sciences Phase 2 2016-11-01 2016-11-10
    NCT01646450 Non-Small Cell Lung Cancer Drug: Icotinib Betta Pharmaceuticals Co.,Ltd. Phase 4 2012-07-01 2015-09-05
    NCT02044328 Non-small Cell Lung Cancer Drug: Icotinib Betta Pharmaceuticals Co.,Ltd. Phase 2 2014-01-01 2016-07-01
    NCT01720901 Non-small Cell Lung Cancer Drug: Icotinib Betta Pharmaceuticals Co.,Ltd. Phase 4 2013-02-01 2015-05-21
    NCT02820116 Non-small Cell Lung Cancer(NSCLC) Drug: Icotinib Beijing Haidian Hospital|Peking University People's Hospital|307 Hospital of PLA|309th Hospital of Chinese People's Liberation Army Phase 2 2016-05-01 2016-06-29
    NCT02486354 Non-small Cell Lung Cancer Drug: icotinib Betta Pharmaceuticals Co.,Ltd. Phase 3 2010-03-01 2015-06-28
    NCT01855854 Adenocarcinoma of the Gastroesophageal Junction|Esophageal Carcinoma Drug: Icotinib Betta Pharmaceuticals Co.,Ltd. Phase 2 2013-05-01 2015-07-14
    NCT02191059 Non Small Cell Lung Cancer Drug: Icotinib|Drug: Docetaxel Shandong Cancer Hospital and Institute Phase 2 2014-07-01 2014-07-30
    NCT01973725 Esophageal Squamous Cell Carcinoma Drug: Icotinib Hydrochloride Yuhong Li|Sun Yat-sen University Phase 2 2013-10-01 2016-11-18
    NCT02103257 EGFR Positive Non-small Cell Lung Cancer|Adenocarcinoma Drug: Sequential Icotinib Plus Chemotherapy|Drug: Icotinib Betta Pharmaceuticals Co.,Ltd. Phase 4 2014-03-01 2015-04-27
    NCT01926171 Non-small-cell Lung Cancer Drug: Icotinib plus WBRT Betta Pharmaceuticals Co.,Ltd. Phase 4 2013-06-01 2015-07-14
    NCT01516983 Non-small Cell Lung Cancer|Brain Metastases Drug: icotinib|Radiation: Whole brain radiotherapy Betta Pharmaceuticals Co.,Ltd. Phase 1|Phase 2 2011-12-01 2014-02-13
    NCT02215356 Non-small Cell Lung Cancer Drug: Icotinib with concurrent radiotherapy|Drug: Chemoradiotherapy Betta Pharmaceuticals Co.,Ltd. Phase 2 2014-08-01 2014-08-11

    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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