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Dacomitinib

达克替尼,PF299804,PF-299804,PF 299804,PF 299,PF-299,PF299,

Dacomitinib 是一种有效的，不可逆的pan-ErbB抑制剂，最有效作用于EGFR，IC50为6 nM，高效作用于携带EGFR或ERBB2突变型(抗Gefitinib)和携带EGFR T790M突变型的NSCLCs。

目录号
EY1733
EY1733
EY1733
纯度
99.41%
99.41%
99.41%
规格
5 mg
10 mg
50 mg
原价
550
1000
3000
售价
550
1000
3000
库存
现货
现货
现货
订购
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  • 生物活性

    Dacomitinib (PF299804, PF299) is a potent, irreversible pan-ErbB inhibitor, mostly to EGFR with IC50 of 6 nM in a cell-free assay, effective against NSCLCs with EGFR or ERBB2 mutations (resistant to gefitinib) as well as those harboring the EGFR T790M mutation. Phase 2.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    0-20 nM

  • 动物实验

    10 mg/kg 口服强饲给药

  • 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] Engelman JA, et al, Cancer Res, 2007, 67(24), 11924-11932.

    分子式
    C24H25ClFN5O2    		 分子量
    469.94    		 CAS号
    1110813-31-4    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    20 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
    NCT02268747 Skin Squamous Cell Cancer Drug: Dacomitinib Fondazione IRCCS Istituto Nazionale dei Tumori, Milano Phase 2 2014-11-01 2016-07-01
    NCT01728233 Penile Neoplasms|Carcinoma, Squamous Cell Drug: Dacomitinib Fondazione IRCCS Istituto Nazionale dei Tumori, Milano|Pfizer Phase 2 2013-06-15 2017-03-08
    NCT01737008 Squamous Cell Carcinoma of the Head and Neck Drug: dacomitinib|Radiation: Radiotherapy|Drug: Cisplatin University Health Network, Toronto Phase 1 2013-01-01 2016-06-09
    NCT01796327 Healthy Volunteers Drug: dacomitinib oral|Drug: dacomitinib intravenous Pfizer Phase 1 2013-04-01 2015-10-06
    NCT01918761 Non Small Cell Lung Cancer Drug: Dacomitinib, Pemetrexed Central European Cooperative Oncology Group Phase 1 2013-08-01 2016-02-17
    NCT02097433 Healthy Drug: Dacomitinib Pfizer Phase 1 2014-07-01 2014-10-02
    NCT02047747 Brain Cancer Drug: Dacomitinib David Piccioni, M.D., Ph.D|Pfizer|University of California, San Diego Phase 2 2014-02-01 2016-08-08
    NCT01152853 Advanced Gastric Cancer|HER2 Drug: PF00299804 Seoul National University Hospital|Pfizer Phase 2 2010-07-01 2015-11-17
    NCT01774721 EGFR Positive Non-small Cell Lung Cancer Drug: Dacomitinib (PF-00299804)|Drug: Gefitinib SFJ Pharmaceuticals, Inc.|Pfizer Phase 3 2013-04-01 2016-10-12
    NCT01571388 Healthy|Otherwise Healthy Volunteers With Mild or Moderate Hepatic Dysfunction Drug: dacomitinib|Drug: dacomitinib|Drug: dacomitinib Pfizer Phase 1 2012-04-01 2013-12-16
    NCT01520870 Glioblastoma|Brain Tumor, Recurrent Drug: PF-299804 (Dacomitinib) Grupo Espaol de Investigacin en Neurooncologa|Pfizer Phase 2 2012-02-01 2016-08-10
    NCT01858389 Non-small Cell Lung Cancer Drug: Dacomitinib|Drug: Dacomitinib Pfizer Phase 2 2013-07-01 2016-01-15
    NCT02382796 NSCLC Drug: Dacomitinib Pfizer Phase 2 2015-07-01 2017-02-15
    NCT00818441 Carcinoma, Non-small Cell Drug: Dacomitinib (PF-00299804)|Drug: Dacomitinib (PF-00299804) Pfizer Phase 2 2009-03-01 2016-04-25
    NCT02039336 Colorectal Cancer Drug: Dacomitinib|Drug: PD-0325901|Drug: Irinotecan|Drug: Docetaxel|Drug: Capecitabine The Netherlands Cancer Institute|Pfizer Phase 1|Phase 2 2014-01-01 2016-11-10
    NCT01702506 Healthy Volunteers Drug: dacomitinib fasted|Drug: dacomitinib fed|Drug: dacomitinib+antacid Pfizer Phase 1 2012-10-01 2013-12-16
    NCT01465802 Non Small Cell Lung Cancer (NSCLC) Drug: Dacomitinib|Drug: Dacomitinib|Drug: Doxycycline|Drug: Probiotic|Drug: Alclometasone cream Pfizer Phase 2 2011-12-01 2016-07-07
    NCT01449201 Head Neck Cancer Squamous Cell Metastatic|Head Neck Cancer Squamous Cell Recurrent Drug: PF-00299804 Yonsei University Phase 2 2011-10-01 2014-09-28
    NCT01360554 Non-Small Cell Lung Cancer (NSCLC) Drug: Dacomitinib (PF-00299804)|Drug: Active Comparator (erlotinib)|Drug: Placebo erlotinib|Drug: Placebo PF00299804 Pfizer Phase 3 2011-06-01 2016-01-04
    NCT01112527 Glioblastoma|GBM|Glioblastoma Multiforme Drug: PF-00299804 Massachusetts General Hospital|Dana-Farber Cancer Institute|Brigham and Women's Hospital|Henry Ford Hospital|Pfizer Phase 2 2010-04-01 2016-12-09

    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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