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INK 128

INK-128,INK128,MLN 0128,MLN-0128,MLN0128,

INK 128 (MLN0128)是一种有效的,选择性的mTOR抑制剂,IC50为1 nM;对I型PI3K亚型的作用效果低200倍以上,与Rapamycin相比,优先抑制mTORC1/2,且对促侵袭基因敏感。

目录号
EY1801
EY1801
EY1801
EY1801
EY1801
纯度
99.23%
99.23%
99.23%
99.23%
99.23%
规格
2 mg
5 mg
10 mg
50 mg
100 mg
原价
820
1210
1923
5960
9210
售价
820
1210
1923
5960
9210
库存
现货
现货
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    INK 128 (MLN0128) is a potent and selective mTOR inhibitor with IC50 of 1 nM in cell-free assays; >200-fold less potent to class I PI3K isoforms, superior in blocking mTORC1/2 and sensitive to pro-invasion genes (vs Rapamycin). Phase 1.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

  • 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 AKm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] Liu A, et al. Drug Discovery Today: Therapeutic Strategies. 2009, 6(2), 47-55.

    分子式
    C15H15N7O
    分子量
    309.33
    CAS号
    1224844-38-5
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    65 mg/mL
    Water
    <1 mg/mL
    Ethanol
    6 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
    NCT01058707 Advanced Solid Malignancies Drug: MLN0128 Millennium Pharmaceuticals, Inc.|Takeda Phase 1 2010-01-01 2017-01-03
    NCT02244463 Anaplastic Thyroid Cancer|Thyroid Cancer Drug: MLN0128 Dana-Farber Cancer Institute|Millennium Pharmaceuticals, Inc. Phase 2 2015-07-01 2016-09-09
    NCT02514824 Merkel Cell Carcinoma Drug: MLN0128 Dana-Farber Cancer Institute|Millennium Pharmaceuticals, Inc. Phase 1|Phase 2 2015-10-01 2016-12-29
    NCT02503722 Recurrent Non-Small Cell Lung Carcinoma|Stage IIIA Non-Small Cell Lung Cancer|Stage IIIB Non-Small Cell Lung Cancer|Stage IV Non-Small Cell Lung Cancer Other: Laboratory Biomarker Analysis|Drug: Osimertinib|Other: Pharmacological Study|Drug: Sapanisertib National Cancer Institute (NCI) Phase 1 2016-10-01 2017-03-14
    NCT01351350 Advanced Solid Malignancies|Hematologic Malignancies Drug: MLN0128 + paclitaxel|Drug: MLN0128 + paclitaxel + trastuzumab Millennium Pharmaceuticals, Inc. Phase 1 2011-03-01 2015-04-07
    NCT02719691 Metastatic Breast Cancer|Solid Tumors Drug: Alisertib|Drug: MLN0128 University of Colorado, Denver Phase 1 2016-05-01 2016-11-07
    NCT02197572 Advanced Solid Tumors Drug: MLN0128 Millennium Pharmaceuticals, Inc.|Takeda Phase 1 2014-09-01 2017-01-12
    NCT01118689 Relapsed Multiple Myeloma|Refractory Multiple Myeloma|Waldenstrom Macroglobulinemia Drug: MLN0128 Millennium Pharmaceuticals, Inc. Phase 1 2010-11-01 2013-07-31
    NCT02575339 Hepatocellular Carcinoma|Liver Cancer|HCC Drug: MLN0128|Drug: MLN0128 (RP2D)|Drug: Sorafenib Bert O'Neil, MD|Hoosier Cancer Research Network|Millennium Pharmaceuticals, Inc.|Big Ten Cancer Research Consortium Phase 1|Phase 2 2016-07-01 2017-01-19
    NCT02484430 Recurrent Adult Acute Lymphoblastic Leukemia Other: Laboratory Biomarker Analysis|Other: Pharmacological Study|Drug: Sapanisertib National Cancer Institute (NCI) Phase 2 2016-10-01 2017-03-23
    NCT02091531 Metastatic Castration-Resistant Prostate Cancer Drug: MLN0128 Memorial Sloan Kettering Cancer Center|Millennium Pharmaceuticals, Inc. Phase 2 2014-03-01 2016-11-21
    NCT02412722 Non-Hematologic Malignancy Drug: Milled MLN0128 API|Drug: Unmilled MLN0128 API|Drug: Paclitaxel Millennium Pharmaceuticals, Inc.|Takeda Phase 1 2015-03-01 2017-01-11
    NCT01899053 Advanced Nonhematologic Malignancies Drug: MLN0128|Drug: MLN1117 Millennium Pharmaceuticals, Inc.|Takeda Phase 1 2013-07-01 2016-11-08
    NCT02142803 Adult Glioblastoma|Endometrial Clear Cell Adenocarcinoma|Endometrial Serous Adenocarcinoma|Ovarian Clear Cell Cystadenocarcinoma|Ovarian Endometrioid Adenocarcinoma|Ovarian Mucinous Cystadenocarcinoma|Ovarian Serous Cystadenocarcinoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma|Recurrent Uterine Corpus Carcinoma|Solid Neoplasm|Stage IIIA Fallopian Tube Cancer|Stage IIIA Ovarian Cancer|Stage IIIA Primary Peritoneal Cancer|Stage IIIB Fallopian Tube Cancer|Stage IIIB Ovarian Cancer|Stage IIIB Primary Peritoneal Cancer|Stage IIIC Fallopian Tube Cancer|Stage IIIC Ovarian Cancer|Stage IIIC Primary Peritoneal Cancer|Stage IV Fallopian Tube Cancer|Stage IV Ovarian Cancer|Stage IV Primary Peritoneal Cancer Biological: Bevacizumab|Other: Laboratory Biomarker Analysis|Other: Pharmacological Study|Drug: Sapanisertib National Cancer Institute (NCI) Phase 1 2014-05-01 2017-01-31
    NCT02049957 Breast Cancer Drug: MLN0128|Drug: Fulvestrant|Drug: Exemestane Millennium Pharmaceuticals, Inc. Phase 1|Phase 2 2014-02-01 2016-02-22
    NCT02756364 Breast Neoplasms Drug: Fulvestrant|Drug: MLN0128 Millennium Pharmaceuticals, Inc.|Takeda Phase 2 2016-06-01 2016-12-15
    NCT02724020 Clear-cell Metastatic Renal Cell Carcinoma Drug: Everolimus|Drug: MLN0128|Drug: MLN1117 Millennium Pharmaceuticals, Inc.|Takeda Phase 2 2016-09-01 2016-11-02
    NCT02417701 Recurrent Squamous Cell Lung Carcinoma|Stage IV Squamous Cell Lung Carcinoma Other: Laboratory Biomarker Analysis|Other: Pharmacological Study|Drug: Sapanisertib National Cancer Institute (NCI) Phase 2 2016-10-01 2017-01-31
    NCT02725268 Endometrial Neoplasms Drug: Paclitaxel|Drug: MLN0128|Drug: MLN1117 Millennium Pharmaceuticals, Inc.|European Network of Translational Research in Ovarian Cancer - EUTROC|European Network of Individualized Treatment in Endometrial Cancer - ENITEC|Takeda Phase 2 2016-06-01 2016-11-02
    NCT02987959 Soft-tissue Sarcoma Drug: TAK-228 Fox Chase Cancer Center Phase 2 2017-02-21 2017-03-02

    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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