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Crizotinib

克里唑替尼,克唑替尼,可唑替尼,PF-02341066

Crizotinib (PF-02341066)是一种有效的c-Met抑制剂，作用于人的c-Met激酶时，Ki为4 nM。

目录号
EY1172
EY1172
EY1172
纯度
99.11%
99.11%
99.11%
规格
5 mg
10 mg
50 mg
原价
260
400
600
售价
260
400
600
库存
现货
现货
现货
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  • 生物活性

    Crizotinib has shown to inhibit wild-type c-Met phosphorylation with a mean IC50 value of 11 nmol/L in multiple human endothelial and carcinoma cell lines. Crizotinib has been demonstrated to inhibit cell growth and induce apoptosis in human GTL-16 gastric carcinoma cells. Additionally, crizotinib could inhibit cell migration and invasion induced by HGF in human NCI-H441 lung cancer cells. Moreover, crizotinib has revealed to block cell scattering of MDCK.

  • 体外研究

  • 体内研究

    5% DMSO+30% PEG 300+dd H2O

  • 激酶实验

  • 细胞实验

    0 nM-256 nM

  • 动物实验

    12.5 mg/kg/day, 25 mg/kg/day, 和50 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] Zou HY, et al. Cancer Res. 2007, 67(9), 4408-4417.
    [2] Cui et al (2011) Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). J.Med.Chem. 54 6342.
    [3] Christensen et al (2007) Cytoreductive antitumor activity of PF-2341066, a novel inhibitor of anaplastic lymphoma kinase and c-Met, in experimental models of anaplastic large-cell lymphoma. Mol.Cancer Ther. 6 3314.

    分子式
    C21H22Cl2FN5O    		 分子量
    450.34    		 CAS号
    877399-52-5    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    10 mM    		 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
    NCT02034981 Hematologic Cancers|Solid Tumors|Metastatic Cancer Drug: Crizotinib UNICANCER|National Cancer Institute, France|Fondation ARC|Pfizer Phase 2 2013-08-01 2016-02-16
    NCT02223819 Uveal Melanoma Drug: Crizotinib Columbia University|Pfizer Phase 2 2015-03-01 2016-12-15
    NCT02499614 Carcinoma, Non-Small-Cell Lung Drug: Crizotinib Fondazione Ricerca Traslazionale Phase 2 2014-12-01 2015-07-14
    NCT01945021 Non Small Cell Lung Cancer|ROS1 Proto Oncogene|Crizotinib Drug: Crizotinib OxOnc Development LP|Pfizer Phase 2 2013-09-01 2016-07-28
    NCT01744652 Advanced Cancers Drug: Crizotinib|Drug: Dasatinib M.D. Anderson Cancer Center|Pfizer Phase 1 2013-03-01 2016-09-26
    NCT02183870 Lung Cancer|Adenocarcinoma|NSCLC Drug: Crizotinib University of Cologne|Spanish Lung Cancer Group|Pfizer Phase 2 2014-05-01 2015-12-07
    NCT03088930 Lung Cancer, Nonsmall Cell Drug: Crizotinib University of Colorado, Denver|Pfizer Phase 2 2017-05-01 2017-03-17
    NCT02207504 Castration-resistant Prostate Cancer Drug: Crizotinib|Drug: Enzalutamide Dana-Farber Cancer Institute|Astellas Pharma Inc|Pfizer Phase 1 2014-08-01 2017-01-29
    NCT01121588 Neoplasms Malignant Drug: Crizotinib Pfizer Phase 1 2011-03-01 2017-02-27
    NCT01712217 Non-small Cell Lung Cancer(NSCLC) Drug: AT13387|Drug: Crizotinib Astex Pharmaceuticals Phase 1|Phase 2 2012-10-01 2017-03-14
    NCT01549574 Healthy Drug: crizotinib|Drug: esomeprazole Pfizer Phase 1 2012-05-01 2012-06-01
    NCT02737501 Non-small Cell Lung Cancer|Lung Cancer|Advanced Malignancies|Carcinoma Drug: Brigatinib|Drug: Xalkori (crizotinib) Ariad Pharmaceuticals Phase 3 2016-04-01 2017-03-06
    NCT02487316 Systemic Anaplastic Large-Cell Lymphoma Drug: crizotinib Jun Zhu|Peking University First Hospital|Peking University People's Hospital|Peking University Third Hospital|Peking Union Medical College Hospital|Beijing Hospital|Chinese PLA General Hospital|First Hospitals affiliated to the China PLA General Hospital|Air Force General Hospital of the PLA|Cancer Institute and Hospital, Chinese Academy of Medical Sciences|Anhui Provincial Hospital|Zhejiang University|Peking University Phase 4 2015-07-01 2016-12-28
    NCT02435108 c-MET Positive Gastric Cancer Drug: crizotinib Samsung Medical Center Phase 2 2014-05-15 2017-02-16
    NCT02419287 Anaplastic Large Cell Lymphoma, ALK-Positive Drug: crizotinib University of Milano Bicocca Phase 2 2015-04-01 2016-10-27
    NCT01531361 Advanced Cancers Drug: Vemurafenib|Drug: Sorafenib|Drug: Crizotinib M.D. Anderson Cancer Center Phase 1 2012-02-01 2016-12-27
    NCT01419041 Renal Impairment Drug: crizotinib|Drug: crizotinib Pfizer Phase 1 2011-11-01 2012-09-28
    NCT01125904 Healthy Drug: crizotinib Pfizer Phase 1 2010-06-01 2010-07-21

    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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