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Temsirolimus

替西罗莫司,坦罗莫司,坦西莫司,CCI-779,NSC 683864

Temsirolimus (CCI-779) is a specific mTOR inhibitor with IC50 of 1.76 μM。

目录号
EY0969
EY0969
EY0969
EY0969
纯度
99.26%
99.26%
99.26%
99.26%
规格
1 mg
5 mg
10 mg
50 mg
原价
249
580
885
1900
售价
249
580
885
1900
库存
现货
现货
现货
现货
订购
订购
订购
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  • 生物活性

    Temsirolimus is a specific mTOR inhibitor with IC50 of 1.76 μM. Temsirolimus is a potent inhibitor of proliferation and induces apoptosis in primary human lymphoblastic leukemia (ALL) cells. Temsirolimus treatment at nanomolar concentrations (10 nM to <5 μM) displays a modest and selective antiproliferative activity via FKBP12-dependent mechanism, but can completely inhibit the proliferation of a broad panel of tumor cells at low micromolar concentrations (5-15 μM), involving FKBP12-independent suppression of mTOR (FRAP) signaling.

  • 体外研究

  • 体内研究

    30% PEG400+0.5% Tween80+5% propylene glycol

  • 激酶实验

  • 细胞实验

    ~20 μM

  • 动物实验

    20 mg/kg每天注射，每周5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] Shor B, et al. Cancer Res, 2008, 68(8), 2934-2943.
    [2] Raymond, E., et al. 2004. J. Clin. Oncol. 22: 2336-2347.
    [3] Galanis, E., et al. 2005. J. Clin. Oncol. 23:5294-5304.

    分子式
    C56H87NO16    		 分子量
    1030.29    		 CAS号
    162635-04-3    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    75 mg/mL    		 Water
    1 mg/mL    		 Ethanol
    75 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
    NCT01072890 Solid Tumors Drug: Temsirolimus, Pazopanib University of California, Davis|GlaxoSmithKline|Pfizer Phase 1 2010-02-01 2012-03-26
    NCT00942747 Recurrent or Refractory Primary CNS Lymphoma Drug: temsirolimus Charite University, Berlin, Germany|Pfizer Phase 2 2009-07-01 2013-04-15
    NCT00838955 Hodgkin's Lymphoma Drug: Temsirolimus Loyola University|Wyeth is now a wholly owned subsidiary of Pfizer Phase 2 2009-01-01 2012-10-29
    NCT01050985 Advanced Solid Tumors Drug: Temsirolimus and capecitabine Georgetown University|Wyeth is now a wholly owned subsidiary of Pfizer Phase 1 2010-07-01 2014-02-12
    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
    NCT00823459 Low-grade Glioma|Astrocytoma|Oligodendroglioma|Mixed Oligoastrocytoma Drug: RAD001 University of California, San Francisco Phase 2 2009-01-01 2016-02-16
    NCT00838539 Neoplasms|Malignant Carcinoma Drug: Neratinib|Drug: Temsirolimus Puma Biotechnology, Inc. Phase 1 2009-04-01 2016-11-22
    NCT01049841 Pediatric Solid Tumors Drug: perifosine + temsirolimus Memorial Sloan Kettering Cancer Center|University of Wisconsin, Madison|Duke University|NATL COMP CA NETWORK|Pfizer|AEterna Zentaris Phase 1 2010-01-01 2017-03-09
    NCT00563147 Renal Cell Carcinoma Drug: tivozanib (AV-951) plus temsirolimus AVEO Pharmaceuticals, Inc. Phase 1 2007-11-01 2011-09-30
    NCT00796796 Carcinoma, Non-Small-Cell Lung Drug: Temsirolimus|Radiation: Radiation therapy Washington University School of Medicine Phase 1 2009-03-01 2013-07-09
    NCT01025453 Thyroid Cancer Drug: Temsirolimus and Sorafenib Memorial Sloan Kettering Cancer Center|National Comprehensive Cancer Network|Pfizer Phase 2 2009-12-01 2017-01-04
    NCT01529593 Advanced Cancers Drug: Temsirolimus|Drug: Metformin M.D. Anderson Cancer Center Phase 1 2012-03-01 2016-10-31
    NCT01016769 Squamous Cell Cancer|Head and Neck Cancer Drug: Temsirolimus + Weekly Paclitaxel + Carboplatin Memorial Sloan Kettering Cancer Center|NATL COMP CA NETWORK|Pfizer Phase 1|Phase 2 2009-11-01 2016-04-25
    NCT02389309 Solid Tumors Drug: Dasatinib|Drug: Cyclophosphamide|Drug: Temsirolimus M.D. Anderson Cancer Center Phase 1 2015-10-05 2017-03-07
    NCT00919035 Prostate Cancer Drug: torisel Oncology Specialists, S.C.|Wyeth is now a wholly owned subsidiary of Pfizer Phase 2 2009-06-01 2014-06-19
    NCT01204450 Brain and Central Nervous System Tumors|Neuroblastoma|Sarcoma|Unspecified Childhood Solid Tumor, Protocol Specific Drug: Temsirolimus|Drug: Valproic Acid UNC Lineberger Comprehensive Cancer Center|National Cancer Institute (NCI) Phase 1 2009-11-01 2016-12-22
    NCT01420601 Renal Cell Carcinoma Drug: Temsirolimus Pfizer 2011-09-01 2016-05-27
    NCT00446368 Carcinoma, Renal Cell Drug: RAD001 The Methodist Hospital System|Novartis Phase 2 2005-05-01 2016-03-15
    NCT02093598 Carcinoma, Endometrioid|mTOR Protein Drug: Temsirolimus MedSIR Phase 2 2012-05-01 2015-04-13
    NCT01210482 Renal Cell Carcinoma Drug: Temsirolimus Pfizer 2010-08-01 2016-05-27
    NCT01122615 Renal Cell Cancer|Kidney Cancer Drug: Sunitinib|Drug: Temsirolimus M.D. Anderson Cancer Center|Pfizer Phase 1 2010-05-01 2015-11-16
    NCT01281917 Non-Hodgkins Lymphoma Drug: Velcade|Drug: Temsirolimus University of Wisconsin, Madison|Millennium Pharmaceuticals, Inc.|Pfizer|National Cancer Institute (NCI) Phase 2 2011-02-01 2015-06-03
    NCT01851408 Melanoma|Recurrent Melanoma|Stage III Melanoma|Stage IV Melanoma Drug: sorafenib tosylate|Drug: temsirolimus National Cancer Institute (NCI)|M.D. Anderson Cancer Center Phase 2 2006-04-01 2015-04-14

    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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