Home > Proteasome & > Bortezomib

Bortezomib

硼替佐米,保特佐米,包特左米,PS341,LDP341,MLM341,PS-341,LDP-341,MLM-341,PS 341,LDP 341,MLM 341

Bortezomib (PS-341)是一种有效的蛋白酶抑制剂，Ki为0.6 nM。

目录号
EY1256
EY1256
EY1256
EY1256
纯度
99.32%
99.32%
99.32%
99.32%
规格
5 mg
10 mg
50 mg
100 mg
原价
400
550
1500
2600
售价
400
550
1500
2600
库存
现货
现货
现货
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  • 生物活性

    Bortezomib (originally codenamed PS-341) is the first therapeutic proteasome inhibitor to the tested in humans. It is approved in the U.S. for treating relapsed multiple myeloma and mantle cell lymphoma. The drug is an N-protected dipeptide and can be written as Pyz-Phe-boroLeu, which stands for pyrazinoic acid, phenylalanine and Leucine with a boronic acid instead of a carboxylic acid. Peptides are written N-terminus to C-terminus, and this convention is used here even though the "C-terminus" is a boronic acid instead of a carboxylic acid. While multiple mechanisms are likely to be involved, proteasome inhibition may prevent degradation of pro-apoptotic factors, permitting activation of programmed cell death in neoplastic cells dependent upon suppression of pro-apoptotic pathways. Recently, it was found that bortezomib caused a rapid and dramatic change in the levels of intracellular peptides that are produced by the proteasome. Some intracellular peptides have been shown to be biologically active, and so the effect of bortezomib on the levels of intracellular peptides may contribute to the biological and/or side effects of the drug.

  • 体外研究

  • 体内研究

    0.5% methylcellulose+0.2% Tween 80

  • 激酶实验

  • 细胞实验

    ~10 μM

  • 动物实验

    1mg/kg i.v.，一周两次，使用4周，然后一周一次

  • 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] Adams J, et al. Cancer Res, 1999, 59(11), 2615-2622.
    [2] Hirai, M., et al. 2010. Blood. [Epub ahead of print].
    [3] Jones, M.D., et al. 2010. Clin. Cancer Res. 16: 4978-4989.
    [4] Alimena, G., et al. 2010. Leuk Res. [Epub ahead of print].
    [5] Nawrocki, S.T., et al. 2005. Cancer Res. 65: 11510-11519.

    分子式
    C19H25BN4O4    		 分子量
    384.24    		 CAS号
    179324-69-7    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    200 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    200 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
    NCT00408928 Graft-versus-Host Disease Drug: Bortezomib Sidney Kimmel Cancer Center at Thomas Jefferson University|Thomas Jefferson University Phase 2 2005-11-01 2016-10-19
    NCT01929980 Allogeneic Stem Cell Transplantation|Refractory Autoimmune Cytopenia(s) Drug: Bortezomib Children's Hospital Medical Center, Cincinnati Phase 2 2012-07-01 2016-10-18
    NCT00644696 Neuroblastoma Drug: Irinotecan and Bortezomib University of Michigan Cancer Center|Millennium Pharmaceuticals, Inc. Phase 1 2008-04-01 2016-06-02
    NCT01163786 Bronchiolitis Obliterans Drug: Bortezomib Northwestern University|Robert H. Lurie Cancer Center Phase 2 2010-07-01 2017-03-01
    NCT01090921 Multiple Myeloma Drug: Bortezomib Boston VA Research Institute, Inc.|Millennium Pharmaceuticals, Inc. Phase 2 2007-05-01 2016-02-01
    NCT01801436 Multiple Myeloma Drug: Bortezomib Johnson & Johnson Taiwan Ltd Phase 3 2006-12-01 2013-03-28
    NCT00657553 Multiple Myeloma Drug: Bortezomib University of Arkansas Phase 3 2008-02-01 2011-06-13
    NCT01672229 Graft Versus Host Disease Drug: Bortezomib University of California, Davis|Millennium Pharmaceuticals, Inc. Phase 1 2012-07-01 2017-01-19
    NCT03013114 Immune Thrombocytopenia Drug: Bortezomib Shandong University Phase 2 2017-01-01 2017-01-05
    NCT02268890 Multiple Myeloma Drug: Bortezomib Johnson & Johnson Taiwan Ltd Phase 4 2014-12-01 2016-07-08
    NCT01158105 Chronic Graft-versus-host Disease Drug: Bortezomib Baylor Research Institute|Millennium Pharmaceuticals, Inc. Phase 2 2010-06-01 2016-01-15
    NCT01328236 Plasma Cell Leukemia|Multiple Myeloma Drug: Bortezomib|Drug: Liposome doxorubicin|Drug: Dexamethasone Clinical Service, China|Harbin Institute of Hematology and Oncology|Shanghai Changzheng Hospital|Chinese PLA General Hospital|307 Hospital of PLA|Wuhan Union Hospital, China|Beijing Chao Yang Hospital|Henan Provincial Hospital|Peking University Third Hospital Phase 2 2010-09-01 2011-09-21
    NCT01517724 Multiple Myeloma Drug: Bortezomib University College, London Phase 2 2009-12-01 2016-05-17
    NCT00153933 Refractory Multiple Myeloma|Relapsed Multiple Myeloma|Multiple Myeloma Drug: Bortezomib|Drug: CC-5013 Dana-Farber Cancer Institute|Beth Israel Deaconess Medical Center|Brigham and Women's Hospital|H. Lee Moffitt Cancer Center and Research Institute Phase 1 2004-08-01 2016-01-21
    NCT00093704 Lymphoma|Lymphoproliferative Disorder Drug: bortezomib + ganciclovir Jonsson Comprehensive Cancer Center|National Cancer Institute (NCI) Phase 1 2005-03-01 2015-10-01
    NCT00815919 Chronic Graft Versus Host Disease Drug: bortezomib|Drug: Prednisone Dana-Farber Cancer Institute|Millennium Pharmaceuticals, Inc. Phase 2 2008-12-01 2015-06-29
    NCT00789256 Acute Myelogenous Leukemia|Myelodysplastic Syndromes Drug: Melphalan|Drug: Bortezomib|Drug: Melphalan and bortezomib Dartmouth-Hitchcock Medical Center|Millennium Pharmaceuticals, Inc. 2004-09-01 2013-05-29
    NCT00153920 Multiple Myeloma Drug: bortezomib Dana-Farber Cancer Institute|Beth Israel Deaconess Medical Center|Massachusetts General Hospital|Brigham and Women's Hospital|Roswell Park Cancer Institute|Emory University|Memorial Sloan Kettering Cancer Center|Millennium Pharmaceuticals, Inc. Phase 2 2003-12-01 2016-01-21
    NCT01695330 Multiple Myeloma Drug: Subcutaneous bortezomib Oncotherapeutics|Millennium Pharmaceuticals, Inc. Phase 2 2012-05-01 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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