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Sunitinib

苏尼替尼,Sutent,SU11248,SU 11248,SU-11248,

Sunitinib 是多靶点RTK抑制剂，对VEGFR2(Flk-1)和PDGFRβ的IC50分别为80nM和2nM。

目录号
EY0485
EY0485
EY0485
纯度
99.18%
99.18%
99.18%
规格
100 mg
200 mg
500 mg
原价
620
930
1400
售价
620
930
1400
库存
现货
现货
现货
订购
订购
订购
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  • 生物活性

    Sunitinib is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    溶解于DMSO，~10 μM

  • 动物实验

    ~80 mg/kg 口服，每天一次

  • 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] Sun L, et al. J Med Chem, 2003, 46(7), 1116-1119.
    [2] O'Farrell AM, et al. SU11248 is a novel FLT3 tyrosine kinase inhibitor with potent activity in vitro and in vivo. Blood. 2003 May 1;101(9):3597-605.
    [3] Bauerschlag DO, et al. Sunitinib (SU11248) inhibits growth of human ovarian cancer in xenografted mice. Anticancer Res. 2010 Sep;30(9):3355-60.

    分子式
    C22H27FN4O2    		 分子量
    398.47    		 CAS号
    557795-19-4    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    40 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    1 mg/mL

    体内溶解度

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

    NCT00794950 Urinary Tract Urothelial Carcinoma Drug: Sunitinib University of Michigan Phase 2 2009-01-01 2016-10-07
    NCT01499121 Clear Cell, Metastatic Renal Cell Carcinoma Drug: Sunitinib Sunnybrook Health Sciences Centre|Pfizer Phase 2 2012-05-01 2016-05-30
    NCT01498835 Soft Tissue Sarcoma Drug: Sunitinib Heidelberg University|German Research Foundation Phase 1 2012-02-01 2015-05-27
    NCT00886132 Adenoid Cystic Carcinoma|Salivary Gland Cancer Drug: Sunitinib University Health Network, Toronto Phase 2 2007-01-01 2015-07-22
    NCT02626754 Renal Cell Carcinoma Drug: Sunitinib malate vghtpe user|Taipei Veterans General Hospital, Taiwan Phase 2 2015-08-01 2016-06-20
    NCT00864721 Non Small Cell Lung Cancer Drug: Sutent US Oncology Research|Pfizer Phase 2 2009-02-01 2014-05-19
    NCT00912912 Genitourinary Disease Drug: Sunitinib Malate M.D. Anderson Cancer Center|Pfizer Phase 2 2009-05-01 2016-03-17
    NCT00422344 Renal Cell Carcinoma|Kidney Cancer Drug: RAD001, Sunitinib Memorial Sloan Kettering Cancer Center|Novartis Phase 1 2006-10-01 2010-02-25
    NCT00768144 Ovarian Cancer|Fallopian Tube Cancer|Peritoneal Cancer Drug: Sunitinib Dana-Farber Cancer Institute|Beth Israel Deaconess Medical Center|Brigham and Women's Hospital|Massachusetts General Hospital Phase 2 2008-09-01 2016-06-13
    NCT02398552 Metastatic Renal Cell Carcinoma Drug: Sunitinib Beijing Cancer Hospital Phase 2 2015-03-01 2016-02-27
    NCT00668811 Papillary Thyroid Cancer|Follicular Thyroid Cancer|Differentiated Thyroid Cancer Drug: SU011248, Sutent Washington Hospital Center|Pfizer Phase 2 2008-04-01 2016-03-24
    NCT00864864 Glioblastoma|Brain Tumor Drug: Sunitinib Massachusetts General Hospital|Brigham and Women's Hospital|Dana-Farber Cancer Institute|Pfizer Early Phase 1 2007-05-01 2016-07-06
    NCT00961571 Metastatic Colorectal Cancer Drug: sunitinib and capecitabine Georgetown University|Pfizer Phase 2 2009-08-01 2014-02-04
    NCT00672594 Prostate Cancer|Prostatectomy Drug: Sunitinib Malate Duke University|Pfizer Phase 2 2006-07-01 2014-07-31
    NCT02713763 Pancreatic Neuroendocrine Tumour Metastatic Drug: Sunitinib Grupo Espanol de Tumores Neuroendocrinos Phase 2 2016-04-01 2016-03-18
    NCT00606008 Anaplastic Astrocytoma|Glioblastoma Drug: Sunitinib Malate H. Lee Moffitt Cancer Center and Research Institute|Pfizer Phase 2 2007-03-01 2012-11-13
    NCT01286896 Malignant Solid Tumour Drug: Sunitinib The Netherlands Cancer Institute|Pfizer Phase 1 2011-03-01 2011-10-07
    NCT02058901 Solid Tumors Drug: Sunitinib VU University Medical Center Phase 1 2013-07-01 2017-03-17
    NCT00663559 Carcinoma Renal Cells Drug: Sunitinib Spanish Oncology Genito-Urinary Group Phase 2 2008-02-01 2014-12-17
    NCT01082809 Advanced Biliary Tract Adenocarcinoma Drug: Sunitinib Samsung Medical Center Phase 2 2009-03-01 2014-05-13
    NCT01073644 Metastatic Renal Cell Carcinoma Drug: Sunitinib malate Pfizer Phase 4 2010-02-01 2013-07-03

    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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