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CAS No.: 1032754-93-0
Synonyms: GDC-0980;GNE 390;RG 7422
GDC-0980 is a potent, class I PI3K inhibitor for PI3Kα/β/δ/γ with IC50 of 5 nM/27 nM/7 nM/14 nM in cell-free assays
生物活性
靶点 | PI3Kα IC50:5nM | PI3Kβ IC50:27nM | PI3Kγ IC50:14nM | PI3Kδ IC50:7nM |
动物研究 | |
剂量 | Mice: 0.25 mg/kg - 10 mg/kg[2] (p.o.) |
给药途径 | p.o. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
---|---|---|---|---|---|
NCT01301716 | Solid Cancers | Phase 1 | Completed | - | United States, California ... more >> Los Angeles, California, United States, 90025 United States, Florida Tampa, Florida, United States, 33612 United States, Massachusetts Boston, Massachusetts, United States, 02114 Boston, Massachusetts, United States, 02215 Spain Madrid, Spain, 28050 Collapse << |
NCT01485861 | Prostate Cancer | Phase 1 Phase 2 | Active, not recruiting | July 31, 2019 | - |
NCT01332604 | Solid Cancers | Phase 1 | Completed | - | United States, California ... more >> Los Angeles, California, United States, 90095 United States, Colorado Aurora, Colorado, United States, 80045 United States, Minnesota Rochester, Minnesota, United States, 55905 Spain Barcelona, Spain, 08035 Collapse << |
实验方案
技术信息
CAS号 | 1032754-93-0 | 储存条件 |
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分子式 | C23H30N8O3S | 运输 | 蓝冰 | |||||||||||
分子量 | 498.60 | 别名 | GDC-0980;GNE 390;RG 7422 | |||||||||||
溶解度 |
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动物实验配方 |
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Cell Lines | Concentration | Assay Type | Time | Activity Description | Data Sources |
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human MCF7.1 cells | - | Proliferation assay | - | Antiproliferative activity against human MCF7.1 cells expressing HER2 gene after overnight incubation by CellTiter-Glo luminescence assay, IC50=0.255 μM | 21981714 |
human PC3 cells | - | Function assay | - | Inhibition of PIK3 gamma-mediated Akt phosphorylation at Ser473 in human PC3 cells by ELISA, IC50=0.036 μM | 21981714 |
human PC3 cells | - | Proliferation assay | - | Antiproliferative activity against human PC3 cells after overnight incubation by CellTiter-Glo luminescence assay, IC50=0.307 μM | 21981714 |
insect cells | - | Function assay | 30 mins | Inhibition of human recombinant mTOR expressed in insect cells assessed as phosphorylation of recombinant (GFP)-4-EBP1 measured after 30 mins by fluorescence polarization assay, Ki=0.017 μM | 21981714 |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
---|
NCT01301716 | Solid Cancers | Phase 1 | Completed | - | United States, California ... more >> Los Angeles, California, United States, 90025 United States, Florida Tampa, Florida, United States, 33612 United States, Massachusetts Boston, Massachusetts, United States, 02114 Boston, Massachusetts, United States, 02215 Spain Madrid, Spain, 28050 Collapse << |
NCT01485861 | Prostate Cancer | Phase 1 Phase 2 | Active, not recruiting | July 31, 2019 | - |
NCT01332604 | Solid Cancers | Phase 1 | Completed | - | United States, California ... more >> Los Angeles, California, United States, 90095 United States, Colorado Aurora, Colorado, United States, 80045 United States, Minnesota Rochester, Minnesota, United States, 55905 Spain Barcelona, Spain, 08035 Collapse << |
NCT01437566 | Breast Cancer | Phase 2 | Completed | - | - |
NCT01287091 | Healthy Volunteer | Phase 1 | Completed | - | United States, Texas ... more >> Investigational Site Austin, Texas, United States, 78744 Collapse << |
NCT01473316 | Healthy Volunteer | Phase 1 | Completed | - | United States, Texas ... more >> Austin, Texas, United States, 78744 Collapse << |
NCT00854152 | Non-Hodgkin's Lymphoma, Solid ... more >>Cancers Collapse << | Phase 1 | Completed | - | United States, Illinois ... more >> Chicago, Illinois, United States, 60637 United States, Massachusetts Boston, Massachusetts, United States, 02115 United States, New York New York, New York, United States, 10065 United States, Tennessee Nashville, Tennessee, United States, 37203 United Kingdom Sutton, United Kingdom, SM2 5PT Collapse << |
NCT01254526 | Breast Cancer | Phase 1 | Completed | - | United States, Massachusetts ... more >> Boston, Massachusetts, United States, 02115 United States, Tennessee Nashville, Tennessee, United States, 37203 Belgium Leuven, Belgium, 3000 Collapse << |
NCT01455493 | Endometrial Carcinoma | Phase 2 | Completed | - | - |
NCT00854126 | Non-Hodgkin's Lymphoma, Solid ... more >>Cancers Collapse << | Phase 1 | Completed | - | United States, Massachusetts ... more >> Boston, Massachusetts, United States, 02115 France Villejuif, France, 94805 United Kingdom Manchester, United Kingdom, M20 4BX Collapse << |
NCT01487239 | Healthy Volunteer | Phase 1 | Completed | - | United States, Wisconsin ... more >> Madison, Wisconsin, United States, 53704-2523 Collapse << |
NCT01442090 | Renal Cell Carcinoma | Phase 2 | Completed | - | United States, Florida ... more >> Fort Myers, Florida, United States, 33908 Saint Petersburg, Florida, United States, 33705 United States, Massachusetts Boston, Massachusetts, United States, 02215 United States, Nevada Las Vegas, Nevada, United States, 89148 United States, New York New York, New York, United States, 10065 United States, North Carolina Durham, North Carolina, United States, 27710 United States, Ohio Cleveland, Ohio, United States, 44195 United States, Tennessee Nashville, Tennessee, United States, 37203 France Bordeaux, France, 33075 Paris, France, 75908 Villejuif, France, 94800 Germany Berlin, Germany, 10117 Hannover, Germany, 30625 München, Germany, 81377 Spain Barcelona, Spain, 08003 Barcelona, Spain, 08035 Madrid, Spain, 28041 United Kingdom Leeds, United Kingdom, LS9 7TF London, United Kingdom, EC1A 7BE London, United Kingdom, SW3 6JJ Manchester, United Kingdom, M20 4BX Sutton, United Kingdom, SM2 5PT Collapse << |
靶点 | Description | IC50 |
---|---|---|
PI3Kα | IC50:5nM | |
PI3Kβ | IC50:27nM | |
PI3Kγ | IC50:14nM | |
PI3Kδ | IC50:7nM |
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