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MLN9708

MLN 9708,MLN-9708 枸橼酸艾沙佐米; MLN9708

MLN9708在水溶液或血浆中立即水解为MLN2238，MLN2238是具有生物活性，MLN2238抑制20S proteasome（20S蛋白酶体）的胰凝乳蛋白酶等蛋白水解位点（β5），IC50/Ki为3.4 nM/0.93 nM，对β1作用效果稍弱，对β2几乎没有抑制活性。

目录号
EY0653
EY0653
EY0653
EY0653
纯度
99.22%
99.22%
99.22%
99.22%
规格
1 mg
5 mg
10 mg
50 mg
原价
235
482
678
1420
售价
235
482
678
1420
库存
现货
现货
现货
现货
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  • 生物活性

    MLN9708 immediately hydrolyzed to MLN2238, the biologically active form, on exposure to aqueous solutions or plasma. MLN2238 inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with IC50/Ki of 3.4 nM/0.93 nM in cell-free assays, less potent to β1 and little activity to β2. Phase 3.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    10nM 左右

  • 动物实验

    11 mg/kg静脉注射，每周两次，持续三周

  • 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] Kupperman E, et al. Cancer Res, 2010, 70(5), 1970-80.

    分子式
    C20H23BCl2N2O9    		 分子量
    517.12    		 CAS号
    1201902-80-8 1239908-20-3    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    105 mg/mL    		 Water
    <1 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
    NCT02168101 Multiple Myeloma Drug: MLN9708 SCRI Development Innovations, LLC|Millennium Pharmaceuticals, Inc. Phase 2 2014-09-01 2016-11-21
    NCT02042989 Advanced Cancers Drug: MLN9708|Drug: Vorinostat M.D. Anderson Cancer Center|Millennium Pharmaceuticals, Inc. Phase 1 2014-06-27 2017-03-16
    NCT02477215 Multiple Myeloma Drug: MLN9708|Drug: Dexamethasone|Drug: Bendamustine Parameswaran Hari|Medical College of Wisconsin Phase 1|Phase 2 2015-10-01 2016-08-22
    NCT02630030 Glioblastoma Drug: Ixazomib Citrate Emory University|Takeda Early Phase 1 2016-03-01 2016-10-24
    NCT02250300 Patients Undergoing Allogeneic Hematopoietic Stem Cell Transplantation Drug: MLN9708 Mehdi Hamadani|Medical College of Wisconsin Phase 1|Phase 2 2014-11-01 2016-09-19
    NCT02158975 Lymphoma, T-Cell Drug: MLN9708 University of Michigan Cancer Center Phase 2 2014-09-01 2016-12-15
    NCT02181413 Multiple Myeloma|Autologous Stem Cell Transplant Drug: Ixazomib Citrate|Drug: Placebo Millennium Pharmaceuticals, Inc. Phase 3 2014-07-01 2016-05-17
    NCT02030405 Adult Acute Megakaryoblastic Leukemia (M7)|Adult Acute Minimally Differentiated Myeloid Leukemia (M0)|Adult Acute Monoblastic Leukemia (M5a)|Adult Acute Monocytic Leukemia (M5b)|Adult Acute Myeloblastic Leukemia With Maturation (M2)|Adult Acute Myeloblastic Leukemia Without Maturation (M1)|Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities|Adult Acute Myeloid Leukemia With Del(5q)|Adult Acute Myeloid Leukemia With Inv(16)(p13;q22)|Adult Acute Myeloid Leukemia With t(16;16)(p13;q22)|Adult Acute Myeloid Leukemia With t(8;21)(q22;q22)|Adult Acute Myelomonocytic Leukemia (M4)|Adult Erythroleukemia (M6a)|Adult Pure Erythroid Leukemia (M6b)|Recurrent Adult Acute Myeloid Leukemia Drug: ixazomib Bruno C. Medeiros|National Cancer Institute (NCI)|Stanford University Phase 2 2014-03-01 2017-01-20
    NCT02384746 Breast Cancer Drug: Fulvestrant|Drug: MLN9708 Dartmouth-Hitchcock Medical Center Phase 1 2015-03-01 2016-10-25
    NCT01318902 Light-Chain Amyloidosis Drug: MLN9708 Millennium Pharmaceuticals, Inc.|Takeda Phase 1 2011-05-01 2017-03-09
    NCT02057640 Multiple Myeloma|Kahler Disease|Plasma-Cell Myeloma|Myelomatosis Drug: Panobinostat|Drug: Dexamethasone|Drug: MLN9708 Case Comprehensive Cancer Center Phase 1|Phase 2 2014-05-01 2016-09-28
    NCT02169791 Acute Leukemia|Chronic Leukemia|Myelodysplastic Syndrome|Lymphomas|Multiple Myeloma Drug: MLN9708 Northside Hospital, Inc.|Millennium Pharmaceuticals, Inc. Phase 2 2014-09-01 2016-12-12
    NCT02993094 Triple-Negative Breast Cancer Drug: Ixazomib|Drug: Carboplatin Arbeitsgemeinschaft medikamentoese Tumortherapie|Takeda Phase 1|Phase 2 2016-11-01 2016-12-12
    NCT01936532 Newly Diagnosed Multiple Myeloma Drug: MLN9708|Drug: Lenalidomide|Drug: Dexamethasone Nantes University Hospital Phase 2 2014-10-01 2015-10-06
    NCT01830816 Multiple Myeloma|Advanced Solid Tumors Drug: ixazomib (MLN9708) Millennium Pharmaceuticals, Inc.|Takeda Phase 1 2013-09-01 2017-01-12
    NCT02176486 Lupus Nephritis Drug: Ixazomib|Drug: Placebo Takeda Phase 1 2014-07-01 2017-02-06
    NCT02302846 Leukemia Drug: Ixazomib M.D. Anderson Cancer Center|Millennium: The Takeda Oncology Company Phase 2 2015-03-01 2016-07-26
    NCT02697383 Multiple Myeloma|High Risk Smoldering Multiple Myeloma Drug: Ixazomib (MLN9708)|Drug: Dexamethasone Memorial Sloan Kettering Cancer Center|Millennium Pharmaceuticals, Inc. Phase 1 2016-02-01 2016-11-07
    NCT01659658 Relapsed or Refractory Systemic Light Chain Amyloidosis Drug: IXAZOMIB|Drug: Dexamethasone|Drug: Melphalan|Drug: Cyclophosphamide|Drug: Thalidomide|Drug: Lenalidomide Millennium Pharmaceuticals, Inc.|Takeda Phase 3 2012-12-26 2017-03-22
    NCT01718743 Myeloma Drug: Lenalidomide|Drug: MLN9708|Radiation: Questionnaires M.D. Anderson Cancer Center|Millennium Pharmaceuticals, Inc. Phase 2 2012-12-01 2017-03-06

    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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