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Sunitinib Malate

苹果酸舒尼替尼,苹果酸苏尼替尼

Sunitinib Malate是一种多靶点受体酪氨酸激酶(RTK)抑制剂，作用于VEGFR1， VEGFR2， VEGFR3， PDGFRβ， FLT3，和CSF-1R时，IC50分别为15 nM， 38 nM， 30 nM， 55 nM， 21 nM，和35 nM。

目录号
EY0865
EY0865
EY0865
纯度
99.43%
99.43%
99.43%
规格
50 mg
100 mg
500 mg
原价
400
500
1300
售价
400
500
1300
库存
现货
现货
现货
订购
订购
订购
订购
订购
订购
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  • 生物活性

    Sunitinib malate, also called sunitinib, is a novel, oral, multi-targeted , small molecule oxindole tyrosine kinase inhibitor which inhibits multiple receptor tyrosine kinases including platelet-derived growth factor receptor , vascular endothelial growth factor receptor 1, 2 and 3, c-KIT, FLT3 kinase, colony-stimulating factor 1 receptor and RET kinase. The IC50 of sunitinib is approximately 10-20 ng/ml to NB cell lines, which is within the clinically relevant human trough serum concentration (50-100 ng/ml).

  • 体外研究

  • 体内研究

    0.5% CMC, pH3.5

  • 激酶实验

  • 细胞实验

    ~10 μM

  • 动物实验

    ~80 mg/kg 口服处理，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] Sistla, A., et al.: Drug Dev. Ind. Pharm., 30, 19 (2004)
    [3] Mendel, D.B., et al.: Clin. Cancer Res., 9, 327 (2003)
    [4] Sakamoto, K.M., et al.: Curr. Opin. Invest. Drugs, 5. 1329 (2004)

    分子式
    C22H27FN4O2.C4H6O5    		 分子量
    532.56    		 CAS号
    341031-54-7    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    >10 mg/mL    		 Water
    >25 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
    NCT00912912 Genitourinary Disease Drug: Sunitinib Malate M.D. Anderson Cancer Center|Pfizer Phase 2 2009-05-01 2016-03-17
    NCT00672594 Prostate Cancer|Prostatectomy Drug: Sunitinib Malate Duke University|Pfizer Phase 2 2006-07-01 2014-07-31
    NCT00864721 Non Small Cell Lung Cancer Drug: Sutent US Oncology Research|Pfizer Phase 2 2009-02-01 2014-05-19
    NCT00794950 Urinary Tract Urothelial Carcinoma Drug: Sunitinib University of Michigan Phase 2 2009-01-01 2016-10-07
    NCT01073644 Metastatic Renal Cell Carcinoma Drug: Sunitinib malate Pfizer Phase 4 2010-02-01 2013-07-03
    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
    NCT00465179 Renal Cell Cancer|Kidney Cancer Drug: Sunitinib Malate M.D. Anderson Cancer Center|Pfizer Phase 2 2007-03-01 2016-05-04
    NCT00480935 Renal Cell Carcinoma Drug: Sunitinib Malate (Sutent) University Health Network, Toronto|Pfizer Phase 2 2007-10-01 2015-12-07
    NCT00400569 Liposarcoma|Leiomyosarcoma|Fibrosarcoma|Malignant Fibrous Histiocytoma Drug: Sunitinib Malate (SU011248) H. Lee Moffitt Cancer Center and Research Institute|Pfizer Phase 2 2006-11-01 2012-07-25
    NCT00673816 Von Hippel-Lindau Syndrome Drug: Sunitinib Malate National Eye Institute (NEI)|National Institutes of Health Clinical Center (CC) Phase 1|Phase 2 2008-05-01 2011-11-14
    NCT00330564 Von Hippel-Lindau Syndrome|Renal Cell Carcinoma|Hemangioblastoma Drug: SU011248 M.D. Anderson Cancer Center|Pfizer Phase 2 2006-05-01 2012-02-23
    NCT02626754 Renal Cell Carcinoma Drug: Sunitinib malate vghtpe user|Taipei Veterans General Hospital, Taiwan Phase 2 2015-08-01 2016-06-20
    NCT00606008 Anaplastic Astrocytoma|Glioblastoma Drug: Sunitinib Malate H. Lee Moffitt Cancer Center and Research Institute|Pfizer Phase 2 2007-03-01 2012-11-13
    NCT00338884 Carcinoma, Renal Cell Drug: Sunitinib malate Pfizer Phase 2 2006-09-01 2012-08-22
    NCT00873210 Advanced or Metastatic Renal Cell Carcinoma|Renal Cancer Drug: Sutent Pfizer 2009-05-01 2012-11-07
    NCT00478426 Endometrial Adenocarcinoma|Endometrial Endometrioid Adenocarcinoma|Endometrial Serous Adenocarcinoma|Recurrent Uterine Corpus Carcinoma|Stage IVA Uterine Corpus Cancer|Stage IVB Uterine Corpus Cancer|Uterine Carcinosarcoma|Uterine Corpus Carcinosarcoma Drug: Sunitinib Malate National Cancer Institute (NCI) Phase 2 2007-04-01 2017-01-31
    NCT00706706 Carcinoma, Renal Cell Drug: Sunitinib Malate (SU011248) Pfizer Phase 4 2008-07-01 2013-01-14
    NCT00495625 Liver Cancer Drug: Sunitinib Malate H. Lee Moffitt Cancer Center and Research Institute|Pfizer Phase 2 2006-10-01 2012-03-22
    NCT00361309 Hepatocellular Carcinoma|Liver Cancer Drug: SU011248 Massachusetts General Hospital|Beth Israel Deaconess Medical Center|Brigham and Women's Hospital|Dana-Farber Cancer Institute Phase 2 2006-04-01 2014-03-16
    NCT00434109 Neuroendocrine Tumor|Islet Cell Tumor Drug: Sunitinib malate|Procedure: Hepatic Artery Embolizations H. Lee Moffitt Cancer Center and Research Institute|Pfizer Phase 2 2006-11-01 2012-09-07
    NCT00389974 Cervical Adenocarcinoma|Cervical Adenosquamous Cell Carcinoma|Cervical Squamous Cell Carcinoma|Recurrent Cervical Cancer|Stage IVB Cervical Cancer Drug: sunitinib malate National Cancer Institute (NCI) Phase 2 2007-01-01 2015-02-04
    NCT00716625 Carcinoma, Renal Cell Drug: sunitinib malate Pfizer 2008-06-01 2016-11-17

    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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