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CAS No.: 912999-49-6
Synonyms: AT13387
AT13387 is a selective potent Hsp90 inhibitor with IC50 of 18 nM in A375 cells, displays a long duration of anti-tumor activity.
生物活性
靶点 | HSP90 IC50:18nM |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
---|---|---|---|---|---|
NCT01685268 | Prostate Cancer | Phase 1 Phase 2 | Completed | - | - |
NCT02474173 | Estrogen Receptor Negative ... more >> HER2/Neu Negative Progesterone Receptor Negative Stage III Breast Cancer AJCC v7 Stage IIIA Breast Cancer AJCC v7 Stage IIIB Breast Cancer AJCC v7 Stage IIIC Breast Cancer AJCC v7 Stage IV Breast Cancer AJCC v6 and v7 Triple-Negative Breast Carcinoma Collapse << | Phase 1 | Recruiting | - | United States, Kentucky ... more >> University of Kentucky/Markey Cancer Center Recruiting Lexington, Kentucky, United States, 40536 Contact: Site Public Contact 859-257-3379 Principal Investigator: Mara D. Chambers United States, Ohio Ohio State University Comprehensive Cancer Center Recruiting Columbus, Ohio, United States, 43210 Contact: Site Public Contact 800-293-5066 Jamesline@osumc.edu Principal Investigator: Robert Wesolowski United States, Pennsylvania Thomas Jefferson University Hospital Recruiting Philadelphia, Pennsylvania, United States, 19107 Contact: Site Public Contact 215-955-6084 Principal Investigator: Saveri Bhattacharya University of Pittsburgh Cancer Institute (UPCI) Recruiting Pittsburgh, Pennsylvania, United States, 15232 Contact: Site Public Contact 412-647-8073 Principal Investigator: Adam M. Brufsky Collapse << |
NCT02381535 | Stage III Hypopharyngeal Squam... more >>ous Cell Carcinoma AJCC v7 Stage III Laryngeal Squamous Cell Carcinoma AJCC v6 and v7 Stage III Oral Cavity Squamous Cell Carcinoma AJCC v6 and v7 Stage III Oropharyngeal Squamous Cell Carcinoma AJCC v7 Stage IVA Hypopharyngeal Squamous Cell Carcinoma AJCC v7 Stage IVA Laryngeal Squamous Cell Carcinoma AJCC v7 Stage IVA Oral Cavity Squamous Cell Carcinoma AJCC v6 and v7 Stage IVA Oropharyngeal Squamous Cell Carcinoma AJCC v7 Stage IVB Hypopharyngeal Squamous Cell Carcinoma AJCC v7 Stage IVB Laryngeal Squamous Cell Carcinoma AJCC v7 Stage IVB Oral Cavity Squamous Cell Carcinoma AJCC v6 and v7 Stage IVB Oropharyngeal Squamous Cell Carcinoma AJCC v7 Collapse << | Phase 1 | Active, not recruiting | - | United States, Connecticut ... more >> Yale University New Haven, Connecticut, United States, 06520 Canada, Ontario University Health Network-Princess Margaret Hospital Toronto, Ontario, Canada, M5G 2M9 Collapse << |
实验方案
技术信息
CAS号 | 912999-49-6 | 储存条件 |
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分子式 | C24H31N3O3 | 运输 | 蓝冰 | |||||||||||
分子量 | 409.52 | 别名 | AT13387 | |||||||||||
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 A231 cells | - | Proliferation assay | 48 h | Antiproliferative activity against human A231 cells after 48 hrs by MTT assay, IC50=1.01 μM | 24763261 |
human HCT116 cells | - | Cytotoxic assay | - | Cytotoxicity against human HCT116 cells by Alamar blue assay, IC50=0.048 μM | 20662534 |
human HCT116 cells | - | Proliferation assay | 48 h | Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay, IC50=0.08 μM | 24763261 |
human HCT116 cells | 10 nM | Function assay | 18 h | Induction of apoptosis in human HCT116 cells assessed as upregulation of Hsp70 level at 10 nM after 18 hrs by immunoblotting | 20662534 |
human HCT116 cells | 30 nM | Function assay | 18 h | Induction of apoptosis in human HCT116 cells assessed as reduction of CDK4 level at 30 nM after 18 hrs by immunoblotting | 20662534 |
human HCT116 cells | 30 nM | Function assay | 18 h | Induction of apoptosis in human HCT116 cells assessed as reduction of Raf-1 level at 30 nM after 18 hrs by immunoblotting | 20662534 |
human MCF7 cells | - | Proliferation assay | 48 h | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50=0.28 μM | 24763261 |
human SKBR3 cells | - | Proliferation assay | 48 h | Antiproliferative activity against human SKBR3 cells after 48 hrs by MTT assay, IC50=0.14 μM | 24763261 |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
---|
NCT01685268 | Prostate Cancer | Phase 1 Phase 2 | Completed | - | - |
NCT02474173 | Estrogen Receptor Negative ... more >> HER2/Neu Negative Progesterone Receptor Negative Stage III Breast Cancer AJCC v7 Stage IIIA Breast Cancer AJCC v7 Stage IIIB Breast Cancer AJCC v7 Stage IIIC Breast Cancer AJCC v7 Stage IV Breast Cancer AJCC v6 and v7 Triple-Negative Breast Carcinoma Collapse << | Phase 1 | Recruiting | - | United States, Kentucky ... more >> University of Kentucky/Markey Cancer Center Recruiting Lexington, Kentucky, United States, 40536 Contact: Site Public Contact 859-257-3379 Principal Investigator: Mara D. Chambers United States, Ohio Ohio State University Comprehensive Cancer Center Recruiting Columbus, Ohio, United States, 43210 Contact: Site Public Contact 800-293-5066 Jamesline@osumc.edu Principal Investigator: Robert Wesolowski United States, Pennsylvania Thomas Jefferson University Hospital Recruiting Philadelphia, Pennsylvania, United States, 19107 Contact: Site Public Contact 215-955-6084 Principal Investigator: Saveri Bhattacharya University of Pittsburgh Cancer Institute (UPCI) Recruiting Pittsburgh, Pennsylvania, United States, 15232 Contact: Site Public Contact 412-647-8073 Principal Investigator: Adam M. Brufsky Collapse << |
NCT02381535 | Stage III Hypopharyngeal Squam... more >>ous Cell Carcinoma AJCC v7 Stage III Laryngeal Squamous Cell Carcinoma AJCC v6 and v7 Stage III Oral Cavity Squamous Cell Carcinoma AJCC v6 and v7 Stage III Oropharyngeal Squamous Cell Carcinoma AJCC v7 Stage IVA Hypopharyngeal Squamous Cell Carcinoma AJCC v7 Stage IVA Laryngeal Squamous Cell Carcinoma AJCC v7 Stage IVA Oral Cavity Squamous Cell Carcinoma AJCC v6 and v7 Stage IVA Oropharyngeal Squamous Cell Carcinoma AJCC v7 Stage IVB Hypopharyngeal Squamous Cell Carcinoma AJCC v7 Stage IVB Laryngeal Squamous Cell Carcinoma AJCC v7 Stage IVB Oral Cavity Squamous Cell Carcinoma AJCC v6 and v7 Stage IVB Oropharyngeal Squamous Cell Carcinoma AJCC v7 Collapse << | Phase 1 | Active, not recruiting | - | United States, Connecticut ... more >> Yale University New Haven, Connecticut, United States, 06520 Canada, Ontario University Health Network-Princess Margaret Hospital Toronto, Ontario, Canada, M5G 2M9 Collapse << |
NCT02535338 | EGFR Activating Mutation ... more >> EGFR Exon 20 Insertion Mutation Recurrent Non-Small Cell Lung Carcinoma Stage IV Non-Small Cell Lung Cancer AJCC v7 Collapse << | Phase 1 Phase 2 | Active, not recruiting | - | United States, California ... more >> City of Hope Comprehensive Cancer Center Duarte, California, United States, 91010 Los Angeles County-USC Medical Center Los Angeles, California, United States, 90033 USC / Norris Comprehensive Cancer Center Los Angeles, California, United States, 90033 Keck Medical Center of USC Pasadena Pasadena, California, United States, 91105 University of California Davis Comprehensive Cancer Center Sacramento, California, United States, 95817 City of Hope South Pasadena South Pasadena, California, United States, 91030 Collapse << |
NCT02898207 | Estrogen Receptor Negative ... more >> HER2/Neu Negative High Grade Fallopian Tube Serous Adenocarcinoma High Grade Ovarian Serous Adenocarcinoma Metastatic Malignant Solid Neoplasm Primary Peritoneal High Grade Serous Adenocarcinoma Progesterone Receptor Negative Recurrent Breast Carcinoma Recurrent Fallopian Tube Carcinoma Recurrent Ovarian Carcinoma Recurrent Primary Peritoneal Carcinoma Triple-Negative Breast Carcinoma Unresectable Malignant Solid Neoplasm Collapse << | Phase 1 | Recruiting | June 1, 2020 | United States, Arizona ... more >> Mayo Clinic Hospital Recruiting Phoenix, Arizona, United States, 85054 Contact: Site Public Contact 855-776-0015 Principal Investigator: Andrea E. Wahner Hendrickson Mayo Clinic in Arizona Recruiting Scottsdale, Arizona, United States, 85259 Contact: Site Public Contact 855-776-0015 Principal Investigator: Andrea E. Wahner Hendrickson United States, Florida Mayo Clinic in Florida Recruiting Jacksonville, Florida, United States, 32224-9980 Contact: Site Public Contact 855-776-0015 Principal Investigator: Andrea E. Wahner Hendrickson United States, Massachusetts Massachusetts General Hospital Cancer Center Recruiting Boston, Massachusetts, United States, 02114 Contact: Site Public Contact 877-726-5130 Principal Investigator: Panagiotis A. Konstantinopoulos Brigham and Women's Hospital Recruiting Boston, Massachusetts, United States, 02115 Contact: Site Public Contact 888-823-5923 ctsucontact@westat.com Principal Investigator: Panagiotis A. Konstantinopoulos Beth Israel Deaconess Medical Center Recruiting Boston, Massachusetts, United States, 02215 Contact: Site Public Contact 617-667-9925 Principal Investigator: Panagiotis A. Konstantinopoulos Dana-Farber Cancer Institute Recruiting Boston, Massachusetts, United States, 02215 Contact: Site Public Contact 877-442-3324 Principal Investigator: Panagiotis A. Konstantinopoulos United States, Minnesota Mayo Clinic Recruiting Rochester, Minnesota, United States, 55905 Contact: Site Public Contact 855-776-0015 Principal Investigator: Andrea E. Wahner Hendrickson Collapse << |
NCT02097225 | BRAF V600E Mutation Present ... more >> BRAF V600K Mutation Present Metastatic Malignant Solid Neoplasm Metastatic Melanoma Stage III Cutaneous Melanoma AJCC v7 Stage IIIA Cutaneous Melanoma AJCC v7 Stage IIIB Cutaneous Melanoma AJCC v7 Stage IIIC Cutaneous Melanoma AJCC v7 Stage IV Cutaneous Melanoma AJCC v6 and v7 Unresectable Solid Neoplasm Collapse << | Phase 1 | Recruiting | - | United States, Massachusetts ... more >> Massachusetts General Hospital Cancer Center Recruiting Boston, Massachusetts, United States, 02114 Contact: Ryan J. Sullivan 617-724-4000 rsullivan7@partners.org Principal Investigator: Ryan J. Sullivan Dana-Farber Cancer Institute Suspended Boston, Massachusetts, United States, 02215 Collapse << |
NCT02572453 | ALK Positive ... more >>BCL6 Positive Recurrent Anaplastic Large Cell Lymphoma Recurrent Diffuse Large B-Cell Lymphoma Recurrent Mantle Cell Lymphoma Refractory Anaplastic Large Cell Lymphoma Refractory Diffuse Large B-Cell Lymphoma Refractory Mantle Cell Lymphoma Collapse << | Phase 2 | Recruiting | - | United States, California ... more >> Los Angeles County-USC Medical Center Suspended Los Angeles, California, United States, 90033 USC / Norris Comprehensive Cancer Center Suspended Los Angeles, California, United States, 90033 USC Norris Oncology/Hematology-Newport Beach Suspended Newport Beach, California, United States, 92663 Keck Medical Center of USC Pasadena Suspended Pasadena, California, United States, 91105 United States, Kentucky University of Kentucky/Markey Cancer Center Recruiting Lexington, Kentucky, United States, 40536 Contact: Site Public Contact 859-257-3379 Principal Investigator: Hayder Saeed United States, Maryland Johns Hopkins University/Sidney Kimmel Cancer Center Recruiting Baltimore, Maryland, United States, 21287 Contact: Site Public Contact 410-955-8804 jhcccro@jhmi.edu Principal Investigator: Nina D. Wagner-Johnston United States, Massachusetts Brigham and Women's Hospital Recruiting Boston, Massachusetts, United States, 02115 Contact: Site Public Contact 888-823-5923 ctsucontact@westat.com Principal Investigator: Caron A. Jacobson Dana-Farber Cancer Institute Recruiting Boston, Massachusetts, United States, 02215 Contact: Site Public Contact 877-442-3324 Principal Investigator: Caron A. Jacobson United States, Nebraska Nebraska Medicine-Bellevue Recruiting Bellevue, Nebraska, United States, 68123 Contact: Site Public Contact 402-559-6941 unmcrsa@unmc.edu Principal Investigator: Philip J. Bierman Nebraska Medicine-Village Pointe Recruiting Omaha, Nebraska, United States, 68118 Contact: Site Public Contact 402-559-5600 Principal Investigator: Philip J. Bierman University of Nebraska Medical Center Recruiting Omaha, Nebraska, United States, 68198 Contact: Site Public Contact 402-559-6941 unmcrsa@unmc.edu Principal Investigator: Philip J. Bierman United States, New Hampshire Dartmouth Hitchcock Medical Center Recruiting Lebanon, New Hampshire, United States, 03756 Contact: Site Public Contact 800-639-6918 cancer.research.nurse@dartmouth.edu Principal Investigator: Frederick Lansigan United States, New Jersey Rutgers Cancer Institute of New Jersey-Robert Wood Johnson University Hospital Recruiting New Brunswick, New Jersey, United States, 08903 Contact: Site Public Contact 732-235-8675 Principal Investigator: Kevin A. David Rutgers Cancer Institute of New Jersey Recruiting New Brunswick, New Jersey, United States, 08903 Contact: Site Public Contact 732-235-8675 Principal Investigator: Kevin A. David United States, Ohio Ohio State University Comprehensive Cancer Center Recruiting Columbus, Ohio, United States, 43210 Contact: Site Public Contact 800-293-5066 Jamesline@osumc.edu Principal Investigator: Jonathan E. Brammer United States, Pennsylvania University of Pennsylvania/Abramson Cancer Center Active, not recruiting Philadelphia, Pennsylvania, United States, 19104 University of Pittsburgh Cancer Institute (UPCI) Recruiting Pittsburgh, Pennsylvania, United States, 15232 Contact: Site Public Contact 412-647-8073 Principal Investigator: Kathleen A. Dorritie United States, Utah Huntsman Cancer Institute/University of Utah Recruiting Salt Lake City, Utah, United States, 84112 Contact: Site Public Contact 888-424-2100 cancerinfo@hci.utah.edu Principal Investigator: Deborah M. Stephens Collapse << |
NCT02503709 | Advanced Malignant Solid Neopl... more >>asm Metastatic Malignant Solid Neoplasm Unresectable Solid Neoplasm Collapse << | Phase 1 | Recruiting | - | United States, District of Col... more >>umbia MedStar Georgetown University Hospital Recruiting Washington, District of Columbia, United States, 20007 Contact: Site Public Contact 202-444-2223 Principal Investigator: Stephen V. Liu United States, Maryland National Cancer Institute Developmental Therapeutics Clinic Recruiting Bethesda, Maryland, United States, 20892 Contact: Site Public Contact 800-411-1222 Principal Investigator: A P. Chen National Institutes of Health Clinical Center Recruiting Bethesda, Maryland, United States, 20892 Contact: Site Public Contact 800-411-1222 Principal Investigator: A P. Chen United States, Massachusetts Massachusetts General Hospital Cancer Center Recruiting Boston, Massachusetts, United States, 02114 Contact: Site Public Contact 877-726-5130 Principal Investigator: Khanh T. Do Dana-Farber Cancer Institute Recruiting Boston, Massachusetts, United States, 02215 Contact: Site Public Contact 877-442-3324 Principal Investigator: Khanh T. Do United States, Ohio Ohio State University Comprehensive Cancer Center Recruiting Columbus, Ohio, United States, 43210 Contact: Site Public Contact 800-293-5066 Jamesline@osumc.edu Principal Investigator: John L. Hays Collapse << |
靶点 | Description | IC50 |
---|---|---|
HSP90 | IC50:18nM |
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