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。
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.
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。
[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
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。
相关化合物库
使用AMQUAR产品发表文献后请联系我们