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Everolimus

依维莫司,RAD001

Everolimus (RAD001)是一种mTOR抑制剂，作用于FKBP12，IC50为1.6-2.4 nM。

目录号
EY0847
EY0847
EY0847
纯度
99.18%
99.18%
99.18%
规格
5 mg
10 mg
50 mg
原价
450
700
2,500.00_
售价
450
700
2,500.00_
库存
现货
现货
现货
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  • 生物活性

    Everolimus, also known as RAD001, is a potent and orally bio-available inhibitor of mammalian target of rapamycin (mTOR), a key component of active PI3K/Akt pathway in human cancers. It binds to intracellular receptor FKBP12 in the mTOR pathway with high affinity forming an everolimus-FKBP12 complex. The complex further binds to mTOR resulting in reducing the activity of the downstream effectors S6 ribsomal protein kinase (S6K1) and translational repressor protein eukaryotic elongation factor 4E-binding protein (4EBP). Besides its immunosuppressive activity for the prevention of organ transplant rejection, everolimus exhibits antineoplastic activity and is currently used to treat renal cell cancer and other tumors.

  • 体外研究

  • 体内研究

    30% Propylene glycol (dissolve first)+5% Tween 80+ddH2O

  • 激酶实验

  • 细胞实验

    0.001 μM -10 μM

  • 动物实验

    ≤2 mg/kg 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] Sedrani R, et al. Transplant Proc, 1998, 30(5), 2192-2194.
    [2] Weisblum, B. 1984. Br. Med. Bull. 40: 47-53.
    [3] Nashan, B. 2002. Ther Drug Monit. 24: 53-58.
    [4] Anandappa, G., et al. 2010. Cancer Manag Res. 2: 61-70.
    [5] Patsenker, E., et al. 2010. J Hepatol. [Epub ahead of print].

    分子式
    C53H83NO14    		 分子量
    958.22    		 CAS号
    159351-69-6    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    100 mg/mL    		 Water
    <1 mg/mL    		 Ethanol

    体内溶解度

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

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT00596557 Chronic Rejection of Cardiac Transplant Drug: everolimus Rabin Medical Center Phase 4 2008-02-01 2011-07-28
    NCT01046045 Chronic Allograft Dysfunction in Renal Transplantation Drug: everolimus Chinese University of Hong Kong Phase 4 2008-04-01 2015-06-19
    NCT01545817 Carcinoma, Renal Cell Drug: Pazopanib followed by everolimus Novartis Phase 2 2012-04-01 2017-01-11
    NCT02155920 Recurrent Childhood Ependymoma Drug: Everolimus University of Texas Southwestern Medical Center Phase 2 2015-02-01 2016-12-02
    NCT01997255 Sturge Weber Syndrome Drug: Everolimus Baylor College of Medicine|Novartis Pharmaceuticals Phase 2 2014-04-01 2016-05-04
    NCT00805129 Bladder Cancer|Metastatic Transitional Cell Carcinoma Drug: Everolimus Memorial Sloan Kettering Cancer Center|Novartis Pharmaceuticals Phase 2 2008-12-01 2017-01-04
    NCT01642732 Prostate Cancer Other: Everolimus, lupron, bicalutamide, and radiation University of Michigan Cancer Center|Novartis Pharmaceuticals Phase 1 2012-10-01 2015-12-08
    NCT01216839 Refractory or Relapsed RMS and Soft Tissue Sarcomas Drug: Everolimus Sidnei Epelman|Hospital Santa Marcelina Phase 2 2011-03-01 2013-03-25
    NCT01216826 Refractory or Relapsed Osteosarcoma Drug: Everolimus Sidnei Epelman|Hospital Santa Marcelina Phase 2 2011-03-01 2013-08-05
    NCT01063478 Non-Small Cell Lung Cancer Drug: RAD001 (in addition to standard radiation and chemotherapy) University of Chicago|Novartis Pharmaceuticals Phase 1 2010-02-01 2014-01-16
    NCT01780948 Difference of 12-hour AUC Drug: Atorvastatin 20 mg|Drug: Everolimus Chulalongkorn University|Ratchadapiseksompotch Research Fund 2012-09-01 2013-02-07
    NCT01430572 Advanced Cancers|Solid Tumors Drug: Pazopanib|Drug: Everolimus M.D. Anderson Cancer Center|GlaxoSmithKline|National Comprehensive Cancer Network Phase 1 2011-10-01 2017-02-08
    NCT00446368 Carcinoma, Renal Cell Drug: RAD001 The Methodist Hospital System|Novartis Phase 2 2005-05-01 2016-03-15
    NCT01107509 Carcinoma, Renal Cell Drug: everolimus St. Joseph's Healthcare Hamilton|McMaster University|Novartis Pharmaceuticals 2010-10-01 2016-10-12
    NCT00516412 Lymphoma Drug: everolimus|Genetic: molecular response by PCR Swiss Group for Clinical Cancer Research Phase 2 2007-08-01 2015-09-28
    NCT00933777 Unspecified Adult Solid Tumor, Protocol Specific|Non-Small Cell Lung Cancer Drug: Combination of sorafenib and everolimus University of Cologne Phase 1 2009-07-01 2016-05-24
    NCT00823459 Low-grade Glioma|Astrocytoma|Oligodendroglioma|Mixed Oligoastrocytoma Drug: RAD001 University of California, San Francisco Phase 2 2009-01-01 2016-02-16
    NCT01773460 Metastatic Breast Cancer Drug: Everolimus|Drug: Everolimus-placebo German Breast Group|Novartis Phase 3 2013-07-01 2016-02-09
    NCT00976248 Waldenstrom's Macroglobulinemia Drug: RAD001 Dana-Farber Cancer Institute|Brigham and Women's Hospital|Novartis Phase 2 2009-11-01 2016-12-14
    NCT01466231 Germ Cell Tumor Drug: Everolimus National Cancer Institute, Slovakia Phase 2 2011-11-01 2016-01-11
    NCT01793636 Metastatic Clear Cell Renal Carcinoma Drug: AZD2014|Drug: Everolimus Queen Mary University of London|AstraZeneca|Cancer Research UK Phase 2 2013-02-01 2014-06-23
    NCT02305810 Pancreatic Neuroendocrine Tumour Metastatic Drug: Everolimus 10 mg daily European Institute of Oncology Phase 2 2013-09-01 2016-08-09
    NCT01141309 Thyroid Cancer Drug: sorafenib with everolimus Memorial Sloan Kettering Cancer Center Phase 2 2010-06-01 2017-03-21
    NCT01178151 Peutz-Jeghers Syndrome|Neoplastic Processes|Neoplasm Metastasis Drug: Everolimus Academisch Medisch Centrum - Universiteit van Amsterdam (AMC-UvA)|Erasmus Medical Center Phase 2 2010-10-01 2015-04-21

    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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