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CAS No.: 1206161-97-8
Synonyms: GLPG0634;PubChemSID 163643231
Filgotinib is a selective JAK1/2 inhibitor with IC50 values of 10/28nM, with less potency against JAK3 and TYK2 with IC50 values of 810 nM and 116 nM, respectively.
生物活性
靶点 | JAK1 IC50:10nM | JAK2 IC50:28nM | JAK3 IC50:810nM | Tyk2 IC50:116nM |
动物研究 | |||||||||||||||||||||||||||||||
剂量 | Mice: 50 mg/kg[1] (p.o.), 1.5 mg/kg[2] (p.o.) Rat: 0.1 mg/kg - 30 mg/kg[1] (p.o.) | ||||||||||||||||||||||||||||||
给药途径 | p.o. | ||||||||||||||||||||||||||||||
动物药代数据 |
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NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
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NCT01179581 | Healthy | Phase 1 | Completed | - | Belgium ... more >> SGS Stuivenberg Antwerp, Belgium Collapse << |
NCT01384422 | Rheumatoid Arthritis | Phase 2 | Completed | - | Moldova, Republic of ... more >> Innophar MO S.R.L. Chisinau, Moldova, Republic of, MD-2025 Collapse << |
NCT02885181 | - | - | Completed | - | - |
实验方案
技术信息
CAS号 | 1206161-97-8 | 储存条件 |
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分子式 | C21H23N5O3S | 运输 | 蓝冰 | |||||||||||||
分子量 | 425.50 | 别名 | GLPG0634;PubChemSID 163643231 | |||||||||||||
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 CD34+ cells | - | Function assay | 45 mins | Inhibition of JAK2 homodimer in human CD34+ cells spiked into human whole blood assessed as inhibition of EPO-induced STAT-5 phosphorylation preincubated for 45 mins followed by EPO addition measured after 15 mins by FACS analysis | 24417533 |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
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NCT01179581 | Healthy | Phase 1 | Completed | - | Belgium ... more >> SGS Stuivenberg Antwerp, Belgium Collapse << |
NCT01384422 | Rheumatoid Arthritis | Phase 2 | Completed | - | Moldova, Republic of ... more >> Innophar MO S.R.L. Chisinau, Moldova, Republic of, MD-2025 Collapse << |
NCT02885181 | - | - | Completed | - | - |
NCT01888874 | Rheumatoid Arthritis | Phase 2 | Completed | - | - |
NCT01894516 | Rheumatoid Arthritis | Phase 2 | Completed | - | - |
NCT02885181 | Rheumatoid Arthritis | Phase 2 | Completed | - | United States, Florida ... more >> Omega Research Consultants DeBary, Florida, United States, 32713 Sarasota Arthritis Research Center Sarasota, Florida, United States, 34239 United States, Georgia Medical Associates of North Georgia Canton, Georgia, United States, 30114 United States, Kentucky Center For Arthritis and Osteoporosis Elizabethtown, Kentucky, United States, 42701 United States, New Mexico Albuquerque Center For Rheumatology Albuquerque, New Mexico, United States, 87102 United States, Pennsylvania Altoona Center for Clinical Research Duncansville, Pennsylvania, United States, 16635 United States, Texas Accurate Clinical Management - Najam Houston, Texas, United States, 77084 Accurate Clinical Research Inc. Stafford, Texas, United States, 77477 Medical Center Research LLC Webster, Texas, United States, 77598 Bulgaria MHAT-Plovdiv AD Plovdiv, Bulgaria, 4000 Umhat Kaspela Plovdiv, Bulgaria, 4003 NMTH Tsar Boris III Sofia, Bulgaria, 1233 Czechia A-Shine s.r.o. Plzen, Czechia, 31200 Medical Plus, S.R.O. Uherske Hradiste, Czechia, 68601 Georgia LLC Arensia Exploratory Medicine T'bilisi, Georgia, 0112 Moldova, Republic of ARENSIA Exploratory Medicine Phase I Unit, Republican Clinical Hospital Chisinau, Moldova, Republic of, MD-2025 Poland ClinicMed Badurski i wspolnicy Spolka Jawna Bialystok, Poland, 15-879 Ukraine Kharkiv City Hospital 8 Kharkiv, Ukraine, 140176 Medical Center_Clinic of International Institute of clinical Studies Kyiv, Ukraine, 2068 Collapse << |
NCT03100942 | Sjogren's Syndrome | Phase 2 | Active, not recruiting | December 2019 | - |
NCT01668641 | Rheumatoid Arthritis | Phase 2 | Completed | - | Hungary ... more >> Budai Irgalamsrendi Korhaz, II. Reumatologia Osztaly Budapest, Hungary Orszagos Reumatologiai es Fizioterapias Intezet, I. Reumatologia Osztaly Budapest, Hungary Markhot Ferenc Korhaz, Reumatologiai Osztaly Eger, Hungary Pest Megyei Flor Ferenc Korhaz, Reumatologiai es Fizioterapias Osztaly Kistarcsa, Hungary Moldova, Republic of IMSP Institutel de Cardiologie Chisinau, Moldova, Republic of Russian Federation State Healthcare Institution of city Moscow 'City Clinical Hospital #7' Moscow, Russian Federation State Healthcare Institution 'Ryazan Regional Cardiology Dispensary' Ryazan, Russian Federation Saint-Petersburg State Healthcare Institution 'City Hospital #26' Saint-Petersburg, Russian Federation Saint-Petersburg State Healthcare Institution 'City Mariinskiy Hospital' Saint-Petersburg, Russian Federation Municipal Clinical Healthcare Institution 'Medical-Sanitary Unit of Novoyaroslavskiy Oil Refinery' Yaroslavl, Russian Federation Ukraine Chernivtsi Regional Clinical Hospital Chernivtsi, Ukraine State Institution 'Institute of Urgent and Recovery Surgery n.a. V.K. Gusaka' of AMS of Ukraine Donetsk, Ukraine Communal Institution of Healthcare Kharkiv, Ukraine Institution of Therapy of AMS of Ukraine Kharkiv, Ukraine State Institution 'Institute of Microbiology and Immunology of AMS of Ukraine' Kharkiv, Ukraine State Institution 'Republican Clinical Hospital of MoH of Ukraine' Kiev, Ukraine Lutsk City Clinical Hospital Lutsk, Ukraine Vinnytsa Regional Clinical Hospital Vinnytsa, Ukraine Zaporizhzhia Regional Clinical Hospital Zaporizhzhia, Ukraine Collapse << |
NCT01419990 | Healthy | Phase 1 | Completed | - | Belgium ... more >> SGS Stuivenberg Antwerp, Belgium, 2060 Collapse << |
NCT02886728 | Rheumatoid Arthritis | Phase 3 | Active, not recruiting | May 2019 | - |
NCT02889796 | Rheumatoid Arthritis | Phase 3 | Active, not recruiting | April 2019 | - |
NCT03201445 | Ulcerative Colitis | Phase 2 | Recruiting | October 2024 | - |
NCT01820806 | Healthy | Phase 1 | Completed | - | United Kingdom ... more >> Quotient Clinical Nottingham, United Kingdom, NG11 6JS Collapse << |
NCT02084199 | Renal Impairment | Phase 1 | Completed | - | Germany ... more >> CRS Clinical Research Services Kiel GmbH Kiel, Germany Collapse << |
NCT03134222 | Cutaneous Lupus Erythematosus | Phase 2 | Recruiting | January 2020 | United States, California ... more >> Wallace Rheumatic Studies Center Recruiting Beverly Hills, California, United States, 90211 Contact: Daniel Wallace 310-360-9197 St. Joseph Heritage Healthcare Recruiting Fullerton, California, United States, 92835 Contact: Shirley Pang 714-626-8650 Dermatology Research Associates Recruiting Los Angeles, California, United States, 90045 Contact: Howard Sofen 310-337-7171 Desert Medical Advances Active, not recruiting Palm Desert, California, United States, 92260 Medderm Associates Recruiting San Diego, California, United States, 92103 Contact: Michelle Pelle 619-542-0013 Robin K. Dore MD Inc. Recruiting Tustin, California, United States, 92780 Contact: Robin Dore 714-505-5500 Inland Rheumatology Clinical Trials Recruiting Upland, California, United States, 91786 Contact: Eric Lee 909-296-8700 United States, Colorado Denver Arthritis Clinic Withdrawn Denver, Colorado, United States, 80230 United States, Florida Clinical Research of West Florida, Inc. Recruiting Clearwater, Florida, United States, 33765 Contact: Robert Levin 727-466-0078 Omega Research Consultants LLC Recruiting DeBary, Florida, United States, 32713 Contact: Sanjiv Kapil 386-668-4202 Rheumatology Associates of Central Florida, P.A. Recruiting Orlando, Florida, United States, 32806 Contact: Pamela Freeman 407-859-4540 ext 124 Lovelace Scientific Resources, Inc. Recruiting Sarasota, Florida, United States, 34233 Contact: Elmer Arne 941-485-8314 United States, Illinois Northwestern University Recruiting Chicago, Illinois, United States, 60611 Contact: Anne Laumann 312-503-5944 United States, Michigan Beals Institute PC Withdrawn Lansing, Michigan, United States, 48917 United States, North Carolina DJL Clinical Research, PLLC Recruiting Charlotte, North Carolina, United States, 28210 Contact: Emily Jane Herron Box 704-247-9179 Duke University Medical Center Recruiting Durham, North Carolina, United States, 27710 Contact: Jennifer Rogers 919-681-7405 PMG Wilmington Recruiting Wilmington, North Carolina, United States, 28401 Contact: Ronald George 910-815-6108 Wake Forest University Health Sciences Recruiting Winston-Salem, North Carolina, United States, 27104 Contact: William Huang 336-716-3775 United States, Pennsylvania Penn State Hershey Medical Center Recruiting Hershey, Pennsylvania, United States, 17033 Contact: Galen Foulke 717-531-1513 University of Pennsylvania Recruiting Philadelphia, Pennsylvania, United States, 19104 Contact: Victoria Werth 215-615-2940 United States, South Carolina Low Country Rheumatology Recruiting Summerville, South Carolina, United States, 29486 Contact: William Edwards 843-572-1818 United States, Texas Metroplex Clinical Research Center Recruiting Dallas, Texas, United States, 75231 Contact: Roy Fleischmann 214-879-6737 Canada Office of Dr. Michael Robern Recruiting Ottawa, Canada, K2G 6E2 Contact: Michael Robern 613-688-0545 University Health Network (UHN) - Toronto Western Hospital Recruiting Toronto, Canada, M5T 2S8 Contact: Zahi Touma (416) 603-5248 K.Papp Clinical Research Recruiting Waterloo, Canada, N2J 1C4 Contact: Kim Papp 519-579-9535 Collapse << |
NCT01798979 | Healthy | Phase 1 | Completed | - | United States, Wisconsin ... more >> Covance Clinical Research Unit Madison, Wisconsin, United States, 53704 Collapse << |
NCT01665924 | Healthy | Phase 1 | Completed | - | Belgium ... more >> SGS LSS Clinical Pharmacology Unit Antwerp Antwerp, Belgium, 2060 Collapse << |
NCT02048618 | Crohn's Disease | Phase 2 | Completed | - | - |
NCT03285711 | Lupus Membranous Nephropathy | Phase 2 | Recruiting | April 2021 | United States, Alabama ... more >> University of Alabama at Birmingham (UAB) Recruiting Birmingham, Alabama, United States, 35294 United States, California University of California San Diego (UCSD) Recruiting La Jolla, California, United States, 92037 Stanford University Recruiting Palo Alto, California, United States, 94304 United States, Florida University of Florida Recruiting Gainesville, Florida, United States, 32610 University Of Florida, Jacksonville Recruiting Jacksonville, Florida, United States, 32207 United States, Georgia Emory University School of Medicine Recruiting Atlanta, Georgia, United States, 30303 Georgia Nephrology Research Institute Recruiting Lawrenceville, Georgia, United States, 30046 United States, Michigan University of Michigan Recruiting Ann Arbor, Michigan, United States, 48109 United States, North Carolina University of North Carolina at Chapel Hill / UNC School of Medicine Recruiting Chapel Hill, North Carolina, United States, 27599-7155 PMG Research Inc. Recruiting Wilmington, North Carolina, United States, 28401 United States, Pennsylvania Temple University Recruiting Philadelphia, Pennsylvania, United States, 19140 United States, South Carolina Medical University of South Carolina, University Hospital Recruiting Charleston, South Carolina, United States, 92037 United States, Texas Metroplex Clinical Research Recruiting Dallas, Texas, United States, 75231 Arthritis & Osteoporosis Center of South Texas Withdrawn San Antonio, Texas, United States, 78332 United States, Washington University of Washington Recruiting Seattle, Washington, United States, 98195 Collapse << |
NCT01915667 | Healthy | Phase 1 | Completed | - | Belgium ... more >> SGS LSS Clinical Pharmacology Unit Antwerp Antwerp, Belgium Collapse << |
NCT03101670 | Psoriatic Arthritis | Phase 2 | Completed | - | Belgium ... more >> ULB Hopital Erasme, Service de Rheumatology Brussels, Belgium Bulgaria UMHAT "Kaspela", EOOD Plovdiv, Bulgaria MHAT - Ruse, AD Ruse, Bulgaria UMHAT "SofiaMed", OOD, Block 1 Sofia, Bulgaria UMHAT "Sv. Ivan Rilski", EAD Sofia, Bulgaria Czechia CCBR Czech, a.s Pardubice, Czechia MEDICAL PLUS s.r.o. Uherské Hradiště, Czechia Estonia Center for Clinical and Basic Research Tallinn, Estonia North Estonia Medical Centre Foundation Tallinn, Estonia OÜ Innomedica Tallinn, Estonia Poland Twoja Przychodnia-Centrum Medyczne Nowa Sol Nowa Sól, Poland Ai Centrum Medyczne sp. z o.o. sp.k. Poznań, Poland Niepubliczny Zaklad Opieki Zdrowotnej "Nasz Lekarz" Praktyka Grupowa Lekarzy Rodzinnych z, Przychodnia Specjalistyczna Toruń, Poland Centrum Medyczne AMED, Warszawa Targowek Warsaw, Poland Spain Hospital Universitario de Fuenlabrada, Servicio de Reumatologia Fuenlabrada, Spain Hospital Infanta Luisa, Servicio de Reumatologia Sevilla, Spain Ukraine CI of Healthcare Kharkiv CCH #8 Dept of Rheumatology Kharkiv MA of PGE of MOHU, Ch of Cardiology and Funct Diagnostics Kharkiv, Ukraine CNI Consultative and Diagnostic Center of Pecherskyi District of Kyiv, Department of Therapy Kiev, Ukraine SI NSС M.D. Strazhesko Institute of Cardiology of NAMSU, Unit of Non-coronary HD&Rh Kiev, Ukraine CH of State Border Service of Ukraine (Military Base 2522) Dept of Therapy, D.Halytskyi Lviv NMU, Ch of Family Medicine & Dermatology, Venereology L'viv, Ukraine M.V. Sklifosovskyi Poltava RCH Dept of Rheumatology HSEIU UMSA, Ch of Family Medicine and Therapy Poltava, Ukraine CI of TRC Ternopil', Ukraine M.I. Pyrogov VRCH Dept of Rheumatology M.I. Pyrogov VNMU, Ch of IM #1 Vinnytsya, Ukraine MCIC MC LLC Health Clinic, Unit of Cardiology and Rheumatology Vinnytsya, Ukraine SRI of Invalid Rehabilitation (EST Complex) of Vinnytsia M.I.Pyrogov NMU MOHU, Un of Therapy and CRh Dept of Therapy Vinnytsya, Ukraine Collapse << |
NCT02162355 | Healthy | Phase 1 | Completed | - | United Kingdom ... more >> Hammersmith Medicines Research (HMR) London, United Kingdom Collapse << |
NCT03207815 | Noninfectious Uveitis | Phase 2 | Recruiting | July 2022 | - |
NCT02873936 | Rheumatoid Arthritis | Phase 3 | Completed | - | - |
NCT03046056 | Small Bowel Crohn's Disease | Phase 2 | Recruiting | March 2020 | - |
NCT02914522 | Ulcerative Colitis | Phase 3 | Recruiting | December 2019 | - |
NCT03077412 | Fistulizing Crohn's Disease | Phase 2 | Recruiting | April 2020 | - |
NCT03417778 | Rheumatoid Arthritis ... more >> Ulcerative Colitis Crohn's Disease Collapse << | Phase 1 | Completed | - | United States, Florida ... more >> Clinical Pharmacology of Miami Miami, Florida, United States, 33014 United States, Texas American Research Corporation at the Texas Liver Institute San Antonio, Texas, United States, 78215 Germany APEX GmbH Munich, Germany, 81241 New Zealand Auckland Clinical Studies Ltd. Grafton, Auckland, New Zealand, 1010 Collapse << |
NCT02914535 | Ulcerative Colitis | Phase 3 | Enrolling by invitation | October 2022 | - |
NCT03117270 | Ankylosing Spondylitis | Phase 2 | Completed | - | Belgium ... more >> ULB Hopital Erasme, Service de Rheumatology Brussels, Belgium Bulgaria Eurohospital Plovdiv, Bulgaria UMHAT Kaspela EOOD Plovdiv, Bulgaria Medical Center "Teodora", EOOD Ruse, Bulgaria Akademik Ivan Geshov, UMHAT "Sv. Ivan Rilski", EAD Sofia, Bulgaria Clinic of Rheumatology, UMHAT "Sv. Ivan Rilski", EAD Sofia, Bulgaria UMHAT "SofiaMed", OOD, Block 1 Sofia, Bulgaria Medical Center "Nov Rehabilitatsionen Tsentar", EOOD Stara Zagora, Bulgaria Czechia Revmatologicka ambulance Ostrava, Czechia CCBR Czech, a.s Pardubice, Czechia MEDICAL PLUS s.r.o. Uherské Hradiště, Czechia Estonia OÜ Innomedica Tallinn, Estonia Poland Centrum Medyczne SILESIANA Sp z oo Bytom, Poland Twoja Przychodnia-Centrum Medyczne Nowa Sol Nowa Sól, Poland Ai Centrum Medyczne sp. z o.o. sp.k. Poznań, Poland Niepubliczny Zaklad Opieki Zdrowotnej "Nasz Lekarz" Praktyka Grupowa Lekarzy Rodzinnych z, Przychodnia Specjalistyczna Toruń, Poland Centrum Medyczne AMED, Warszawa Targowek Warsaw, Poland Spain Corporacio Sanitaria Parc Tauli, Servicio de Reumatologia Santiago de Compostela, Spain Hospital Infanta Luisa, Servicio de Reumatologia Sevilla, Spain Hospital Universitario Virgen Macarena, Dept. of Rheumatology Sevilla, Spain Ukraine CI of Healthcare Kharkiv CCH #8 Dept of Rheumatology Kharkiv MA of PGE of MOHU, Ch of Cardiology and Funct Diagnostics Kharkiv, Ukraine CNI Consultative and Diagnostic Center of Pecherskyi District of Kyiv, Department of Therapy Kiev, Ukraine SI NSС M.D. Strazhesko Institute of Cardiology of NAMSU, Unit of Non-coronary HD&Rh Kiev, Ukraine CH of State Border Service of Ukraine (Military Base 2522) Dept of Therapy, D.Halytskyi Lviv NMU, Ch of Family Medicine & Dermatology, Venereology L'viv, Ukraine M.V. Sklifosovskyi Poltava RCH Dept of Rheumatology HSEIU UMSA, Ch of Family Medicine and Therapy Poltava, Ukraine CI of TRC Ternopil', Ukraine A.Novak Transcarpathian Regional Clinical Hospital, Dept of Rheumatology Uzhgorod, Ukraine M.I. Pyrogov VRCH Dept of Rheumatology M.I. Pyrogov VNMU, Ch of IM #1 Vinnytsia, Ukraine SRI of Invalid Rehabilitation (EST Complex) of Vinnytsia M.I.Pyrogov NMU MOHU, Un of Therapy and CRh Dept of Therapy Vinnytsia, Ukraine MCIC MC LLC Health Clinic, Unit of Cardiology and Rheumatology Vinnytsya, Ukraine Collapse << |
NCT02065700 | Rheumatoid Arthritis | Phase 2 | Active, not recruiting | May 2023 | - |
NCT03025308 | RheumatoId Arthritis | Phase 3 | Enrolling by invitation | May 2022 | - |
NCT02914561 | Crohn's Disease | Phase 3 | Recruiting | December 2019 | - |
NCT02914600 | Crohn's Disease | Phase 3 | Enrolling by invitation | October 2022 | - |
NCT03320876 | Psoriatic Arthritis | Phase 2 | Active, not recruiting | February 2021 | Belgium ... more >> ULB Hopital Erasme, Service de Rheumatology Brussels, Belgium Bulgaria UMHAT "Kaspela", EOOD Plovdiv, Bulgaria MHAT - Ruse, AD Ruse, Bulgaria UMHAT "SofiaMed", OOD, Block 1 Sofia, Bulgaria UMHAT "Sv. Ivan Rilski", EAD Sofia, Bulgaria Czechia CCBR Czech, a.s Pardubice, Czechia MEDICAL PLUS s.r.o. Uherské Hradiště, Czechia Estonia Center for Clinical and Basic Research Tallinn, Estonia North Estonia Medical Centre Foundation Tallinn, Estonia OÜ Innomedica Tallinn, Estonia Poland Twoja Przychodnia-Centrum Medyczne Nowa Sol Nowa Sól, Poland Ai Centrum Medyczne sp. z o.o. sp.k. Poznań, Poland Niepubliczny Zaklad Opieki Zdrowotnej "Nasz Lekarz" Praktyka Grupowa Lekarzy Rodzinnych z, Przychodnia Specjalistyczna Toruń, Poland Centrum Medyczne AMED, Warszawa Targowek Warsaw, Poland Spain Hospital Universitario de Fuenlabrada, Servicio de Reumatologia Fuenlabrada, Spain Hospital Infanta Luisa, Servicio de Reumatologia Sevilla, Spain Ukraine CI of Healthcare Kharkiv CCH #8 Dept of Rheumatology Kharkiv MA of PGE of MOHU, Ch of Cardiology and Funct Diagnostics Kharkiv, Ukraine CNI Consultative and Diagnostic Center of Pecherskyi District of Kyiv, Department of Therapy Kiev, Ukraine SI NSС M.D. Strazhesko Institute of Cardiology of NAMSU, Unit of Non-coronary HD&Rh Kyiv, Ukraine CH of State Border Service of Ukraine (Military Base 2522) Dept of Therapy, D.Halytskyi Lviv NMU, Ch of Family Medicine & Dermatology, Venereology L'viv, Ukraine M.V. Sklifosovskyi Poltava RCH Dept of Rheumatology HSEIU UMSA, Ch of Family Medicine and Therapy Poltava, Ukraine CI of TRC Ternopil', Ukraine M.I. Pyrogov VRCH Dept of Rheumatology M.I. Pyrogov VNMU, Ch of IM #1 Vinnytsia, Ukraine SRI of Invalid Rehabilitation (EST Complex) of Vinnytsia M.I.Pyrogov NMU MOHU, Un of Therapy and CRh Dept of Therapy Vinnytsia, Ukraine MCIC MC LLC Health Clinic, Unit of Cardiology and Rheumatology Vinnytsya, Ukraine Collapse << |
靶点 | Description | IC50 |
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JAK1 | IC50:10nM | |
JAK2 | IC50:28nM | |
JAK3 | IC50:810nM | |
Tyk2 | IC50:116nM |
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