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CAS No.: 908112-43-6
Synonyms: PF-04928473
SNX-2112 is a potent synthetic heat shock protein 90 (HSP90) inhibitor with an IC50 of 0.92 μM for K562 cells.
生物活性
靶点 | HSP90 IC50:0.92μM |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
---|---|---|---|---|---|
NCT02973399 | Cancer | Phase 1 | Active, not recruiting | February 2019 | United States, New York ... more >> Weill Cornell Medical College New York, New York, United States, 10065 United States, Ohio Wexner Medical Center, Ohio State University Columbus, Ohio, United States, 43210 Collapse << |
NCT02914327 | Cancer | Phase 1 | Withdrawn(Lack of enrollment) | - | United States, Ohio ... more >> Wexner Medical Center, Ohio State University Columbus, Ohio, United States, 43210 Collapse << |
NCT02612285 | - | - | Terminated(Recruitment very sl... more >>ow - study could not be enrolled) Collapse << | - | - |
实验方案
技术信息
CAS号 | 908112-43-6 | 储存条件 |
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分子式 | C23H27F3N4O3 | 运输 | 蓝冰 | |||||||||||
分子量 | 464.48 | 别名 | PF-04928473 | |||||||||||
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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A375 cells | - | Function assay | 24 h | Inhibition of Hsp90 in human A375 cells assessed as pS6 degradation after 24 hrs by high content screening, IC50=0.001 μM | 19552433 |
AU565 cells | - | Function assay | 24 h | Inhibition of Hsp90 in human AU565 cells assessed as pERK degradation after 24 hrs by high content screening, IC50=0.041 μM | 19552433 |
HCT15 cells | - | Proliferation assay | 72-144 h | Antiproliferative activity against human HCT15 cells after 72 to 144 hrs by cyquant DNA dye method, IC50=0.052 μM | 19552433 |
HT-29 cells | - | Proliferation assay | 72-144 h | Antiproliferative activity against human HT-29 cells after 72 to 144 hrs by cyquant DNA dye method, IC50=0.003 μM | 19552433 |
human SK-MEL-5 cells | - | Proliferation assay | 72-144 h | Antiproliferative activity against human SK-MEL-5 cells after 72 to 144 hrs by cyquant DNA dye method, IC50=0.006 μM | 19552433 |
human SW620 cells | - | Proliferation assay | 72-144 h | Antiproliferative activity against human SW620 cells after 72 to 144 hrs by cyquant DNA dye method, IC50=0.003 μM | 19552433 |
K562 cells | - | Proliferation assay | 72-144 h | Antiproliferative activity against human K562 cells after 72 to 144 hrs by cyquant DNA dye method, IC50=0.006 μM | 19552433 |
LNCAP cells | - | Proliferation assay | 72-144 h | Antiproliferative activity against human LNCAP cells after 72 to 144 hrs by cyquant DNA dye method, IC50=0.003 μM | 19552433 |
MCF7 cells | - | Function assay | - | Inhibition of HSP90alpha in human MCF7 cells assessed as degradation of Her-2, EC50=0.019 μM | 22938030 |
MDA-MB-231 cells | - | Proliferation assay | 72-144 h | Antiproliferative activity against human MDA-MB-231 cells after 72 to 144 hrs by cyquant DNA dye method, IC50=0.006 μM | 19552433 |
MRC5 cells | - | Cytotoxicity assay | 48 h | Cytotoxicity against human MRC5 cells after 48 hrs by MTT assay, CC50=21.34 μM | 22704890 |
NCI-H460 cells | - | Proliferation assay | 72-144 h | Antiproliferative activity against human NCI-H460 cells after 72 to 144 hrs by cyquant DNA dye method, IC50=0.018 μM | 19552433 |
PC3 cells | - | Proliferation assay | 72-144 h | Antiproliferative activity against human PC3 cells after 72 to 144 hrs by cyquant DNA dye method, IC50=0.017 μM | 19552433 |
sf9 cells | - | Function assay | 3 h | Binding affinity to human N-terminal polyHis-tagged HSP90beta (D9 to E236) expressed in insect sf9 cells after 3 hrs by fluorescence polarization assay, Ki=0.006 μM | 24332488 |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
---|
NCT02973399 | Cancer | Phase 1 | Active, not recruiting | February 2019 | United States, New York ... more >> Weill Cornell Medical College New York, New York, United States, 10065 United States, Ohio Wexner Medical Center, Ohio State University Columbus, Ohio, United States, 43210 Collapse << |
NCT02914327 | Cancer | Phase 1 | Withdrawn(Lack of enrollment) | - | United States, Ohio ... more >> Wexner Medical Center, Ohio State University Columbus, Ohio, United States, 43210 Collapse << |
NCT02612285 | - | - | Terminated(Recruitment very sl... more >>ow - study could not be enrolled) Collapse << | - | - |
NCT02612285 | Cancer | Phase 2 | Terminated(Recruitment very sl... more >>ow - study could not be enrolled) Collapse << | - | United States, Arizona ... more >> HonorHealth Research Institute Scottsdale, Arizona, United States, 85258 United States, Georgia Augusta University Augusta, Georgia, United States, 30912 United States, Michigan Karmanos Cancer Institute Detroit, Michigan, United States, 48201 United States, Ohio Gabrail Cancer Center Research Canton, Ohio, United States, 44718 Wexner Medical Center, Ohio State University Columbus, Ohio, United States, 43210 Collapse << |
靶点 | Description | IC50 |
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HSP90 | IC50:0.92μM |
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