Home Cart Sign in  
Chemical Structure| 1434048-34-6 Chemical Structure| 1434048-34-6

Structure of Fenebrutinib
CAS No.: 1434048-34-6

Chemical Structure| 1434048-34-6

*Storage: {[sel_prStorage]}

*Shipping: {[sel_prShipping]}

,{[proInfo.pro_purity]}

GDC-0853 is a potent and orally BTK inhibitor.

Synonyms: GDC-0853; RG-7845

4.5 *For Research Use Only !

{[proInfo.pro_purity]}
Cat. No.: {[proInfo.prAm]} Purity: {[proInfo.pro_purity]}

Change View

Size Price VIP Price

US Stock

Global Stock

In Stock
{[ item.pr_size ]} Inquiry {[ getRatePrice(item.pr_usd,item.pr_rate,item.mem_rate,item.pr_is_large_size_no_price, item.vip_usd) ]}

US Stock: ship in 0-1 business day
Global Stock: ship in 5-7 days

  • {[ item.pr_size ]}

In Stock

- +

Please Login or Create an Account to: See VIP prices and availability

US Stock: ship in 0-1 business day
Global Stock: ship in 2 weeks

  • 1-2 Day Shipping
  • High Quality
  • Technical Support
Product Citations

Alternative Products

Product Details of Fenebrutinib

CAS No. :1434048-34-6
Formula : C37H44N8O4
M.W : 664.80
SMILES Code : O=C1C(N2CCN1C3=NC=CC(C(C=C4NC5=NC=C(N6[C@@H](C)CN(C7COC7)CC6)C=C5)=CN(C)C4=O)=C3CO)=CC8=C2CC(C)(C)C8
Synonyms :
GDC-0853; RG-7845
MDL No. :N/A
InChI Key :WNEODWDFDXWOLU-QHCPKHFHSA-N
Pubchem ID :86567195

Safety of Fenebrutinib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Fenebrutinib

RTK

Isoform Comparison

Biological Activity

Description
Fenebrutinib (GDC-0853) is characterized as a strong, selective, orally administrable, and reversible inhibitor of Bruton's tyrosine kinase (Btk), with inhibition constants (Kis) of 0.91 nM for the wild-type Btk and 1.6, 1.3, 12.6, and 3.4 nM for the C481S, C481R, T474I, T474M mutants, respectively. It is identified as a candidate for the study of rheumatoid arthritis and systemic lupus erythematosus[1].

In Vitro:

Cell Line
Concentration Treated Time Description References
Platelets 50 nM 15 minutes Inhibition of spontaneous platelet aggregation PMC8744796
Platelets 0.011 μM 15 minutes Inhibition of FcγRIIA-mediated platelet aggregation with an IC50 of 11 nM. PMC6963242
Human iPSC-derived microglia 0.05 nM to 10 μM 24 hours To determine the IC50 of Fenebrutinib on TNF-α release after FcγR activation, the result was 5.1 nM. PMC11514909
Human iPSC-derived microglia 1 μM 24 hours To evaluate the inhibitory effect of Fenebrutinib on TNF-α release after FcγR activation, results showed Fenebrutinib significantly reduced TNF-α release. PMC11514909
Madin-Darby canine kidney cells (MDCK) 20 µM 90 minutes To determine the apparent permeability (Papp) of Fenebrutinib in the presence of varying concentrations of HP-β-CD. Results showed that as the concentration of HP-β-CD increased, the apparent permeability of Fenebrutinib decreased. PMC7689742
JeKo-1 cells 1.4 nM 17 hours Evaluate BTK degradation efficiency, PTD10 demonstrated highly potent BTK degradation in JeKo-1 cells PMC10332445

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Beagle dogs Pentagastrin-pretreated dog model Oral 100 mg Single dose To evaluate the effect of HP-β-CD on the absorption of Fenebrutinib. Results showed that compared to the control group, the HP-β-CD group had a 9-fold decrease in Cmax, a 7-fold decrease in AUC, prolonged Tmax, and a 6.5-fold increase in fecal recovery of Fenebrutinib. PMC7689742

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02983227 Rheumatoid Arthritis PHASE2 COMPLETED 2019-07-17 Arizona Arthritis & Rheumatolo... More >>gy Associates, P.C., Glendale, Arizona, 85306, United States|Medvin Clinical Research, Covina, California, 91723, United States|TriWest Research Associates, LLC, El Cajon, California, 92020, United States|Saint Jude Heritage Medical Grp, Fullerton, California, 92835, United States|RASF-Clinical Research Center, Boca Raton, Florida, 33486, United States|Clinical Research of West Florida, Clearwater, Florida, 33765, United States|Medication Management, Greensboro, North Carolina, 27408, United States|Oregon Health & Science Uni, Portland, Oregon, 97239, United States|Metroplex Clinical Research Centre, Dallas, Texas, 75231, United States|Baylor Research Inst., Dallas, Texas, 75246, United States|Accurate Clinical Research, Houston, Texas, 77089, United States|Instituto de Investigaciones Clinicas-Mar del Plata, Buenos Aires, B7600FZN, Argentina|APRILLUS, Buenos Aires, C1194AAO, Argentina|Instituto centenario, Buenos Aires, C1204AAD, Argentina|Centro de Investigacion en Enfermedades Reumaticas CIER, Ciudad Autonoma Buenos Aires, C1055AAF, Argentina|Expertia S.A- Mautalen Salud e Investigación, Ciudad Autonoma Buenos Aires, C1128AAE, Argentina|CCBR - Buenos Aires - AR; AxisMed SRL, Ciudad Autonoma Buenos Aires, C1430CKE, Argentina|ILAIM-CEOM Inst. Latinoamericano de Inv. Medicas, Cordoba, X5000BNB, Argentina|Centro de Investigaciones Medicas Mar Del Plata, Mar del Plata, B7600DHK, Argentina|Instituto de Investigaciones Clinicas, Rosario, S2000CVD, Argentina|CER San Juan Centro Polivalente de Asistencia e Investigacion Clinica, San Juan, 5400, Argentina|Centro Medico Privado de Reumatologia; Reumathology, San Miguel, T4000AXL, Argentina|CIP - Centro Internacional de Pesquisa X; Pesquisa Clinica, Goiania, GO, 74110-120, Brazil|CMiP - Centro Mineiro de Pesquisa*X*, Juiz de Fora, MG, 36010-570, Brazil|Centro de Estudos em Terapias Inovadoras - CETI, Curtiba, PR, 80030-110, Brazil|CCBR Brasil Centro de Pesquisas e Análises Clínicas Ltda., Rio de Janeiro, RJ, 21941-913, Brazil|LMK Servi?os Médicos S/S, Porto Alegre, RS, 90480-000, Brazil|CAEP - Centro Avancado de Estudos e Pesquisas Ltda., Campinas, SP, 13087-567, Brazil|IMA Brasil - Instituto de Medicina Avancada, Sao Paulo, SP, 05437-000, Brazil|MHAT "Eurohospital" - Plovdiv, OOD; Internal Department, Plovdiv, 4002, Bulgaria|UMHAT "Kaspela", EOOD, Plovdiv, 4002, Bulgaria|Medizinski Zentrar-1-Sevlievo EOOD, Sevlievo, 5400, Bulgaria|MHAT "Hadzhi Dimitar", OOD, Sliven, 8800, Bulgaria|Medical Center Excelsior OOD, Sofia, 1000, Bulgaria|NMTH "Tsar Boris III", Sofia, 1233, Bulgaria|DCC "Alexandrovska", EOOD; Clinic of Neurology, Sofia, 1431, Bulgaria|MC "Synexus - Sofia", EOOD, Sofia, 1784, Bulgaria|UMHAT "SofiaMed", OOD; Department of Neurology, Sofia, 1797, Bulgaria|Centro de Investigacion Medico Asistencial S.A.S, Barranquilla, 80020, Colombia|Centro de Investigacion en Reumatologia y Especialdades Medicas SAS. CIREEM, Bogota, 110221, Colombia|Riesgo de Fractura S.A., Bogota, 110221, Colombia|Consultorio Medico en Fundacion el Hospitalito de morelos A.C., Cuernavaca, Morelos, 62170, Mexico|Centro de Investigacion en Reumatologia, Merida, Yucatan, 97070, Mexico|Consultorio Particular del Dr. Miguel Cortes Hernandez, Cuernavaca, 62290, Mexico|Centro de Investigacion de Tratam Innovadores de Sin SC, Culiacan, 80230, Mexico|Centro de Investigacion en Enfermedades Reumaticas y Osteoporosis, Mexicali, 21100, Mexico|Centro de Investigacion Clínica GRAMEL S.C, Mexico, 03720, Mexico|Policlinica Medica de Queretaro S.C., Queretaro, 76000, Mexico|Clinical Research Institute, Tlalnepantla, 54055, Mexico|Unidad de Enfermedades Reumaticas y Cronicodegenerativas, Torreon, 27000, Mexico|NZOZ ZDROWIE Osteo-Medic, Bialystok, 15-351, Poland|Szpital Uniwersytecki; nr 2 im. Dr J. Biziela, Bydgoszcz, 85-168, Poland|Centrum Medyczne Pratia Katowice I, Katowice, 40-081, Poland|CCBR - Lodz - PL, Lodz, 90-368, Poland|ETYKA Osrodek Badan Kliniczynch, Olsztyn, 10-117, Poland|Ai Centrum Medyczne Sp. Z O.O Sp.K., Poznan, 61-113, Poland|Medycyna Kliniczna, Warszawa, 00-660, Poland|Centrum Medyczne AMED, Warszawa, 03-291, Poland|KO-MED Centra Kliniczne Zamosc, Zamosc, 22400, Poland|SBIH of Yaroslavl region " Regional Clinical Hospital "; Therapy, Yaroslavl, Jaroslavl, 150062, Russian Federation|Federal State Budgetary Scientific Institution Research Institute of Rheumatology V.A. Nasonova, Moscow, Moskovskaja Oblast, 115522, Russian Federation|SBIH of Moscow "City Clinical Hospital # 1 n. a. N. I. Pirogov", Moscow, Moskovskaja Oblast, 119049, Russian Federation|SPb SBIH "Clinical Rheumatological Hospital # 25", Saint-Petersburg, Sankt Petersburg, 190068, Russian Federation|Sanavita LLC, Sankt-peterburg, Sankt Petersburg, 195257, Russian Federation|LLC Medical Sanitary Unit, Sankt-peterburg, Sankt Petersburg, 196066, Russian Federation|Center of Family Medicine LC, Yekaterinburg, Sankt Petersburg, 620043, Russian Federation|SBHI of Yaroslavl Region Clinical Hospital #3, Yaroslavl, Volgograd, 150051, Russian Federation|SMMIH "Chelyabinsk Regional Clinical Hospital", Chelyabinsk, Voronez, 454076, Russian Federation|SAHI of Kem. "Regional Clinical Hospital for War Veterans", Kemerovo, 650000, Russian Federation|OOO Family Polyclinic, Korolev, Moscow Region, 141060, Russian Federation|Practical Medicine, Moscow, 115404, Russian Federation|Limited Liability Company "Centre of Medical Common Practice", Novosibirsk, 630091, Russian Federation|Ultramed, Omsk, 644024, Russian Federation|SEIHPE Saratov State Medical University n.a. V.I. Razumovskiy, Saratov, 410012, Russian Federation|NIH "Departmental Hospital on Station Smolensk of OJSC "Russian Railways", Smolensk, 214025, Russian Federation|Siberian State Medical University, Tomsk, 634050, Russian Federation|SHI Ulyanovsk Reg Clinical Hospital, Ulyanovsk, 432063, Russian Federation|Territorial Clinical Hospital #2, Vladivostok, 690035, Russian Federation|Institute of Rheumatology, Belgrade, 11000, Serbia|Clinical Center Kragujevac, Kragujevac, 34000, Serbia|Institute of Treatment and Rehabilitation "Niska Banja", Niska Banja, 18205, Serbia|Special hospital for rheumatic diseases Novi Sad, Novi Sad, 21000, Serbia|General Hospital "Dr Laza K. Lazarevic" Sabac, Sabac, 15000, Serbia|MI of Healthcare Kyiv RCH P.L. Shupyk NMA of PGE, Kyiv, Chernihiv Governorate, 01601, Ukraine|CI of Healthcare Kharkiv CCH #8 Dept of Therapy Kharkiv MA of PGE of MOHU, Kharkiv, Kharkiv Governorate, 61176, Ukraine|CI of TRC, Ternopil, Kherson Governorate, 46002, Ukraine|Regional CH Dep of Rheumatology SHEI Ivano-Frankivsk NMU, Ivano-Frankivsk, KIEV Governorate, 76008, Ukraine|SI NSС M.D. Strazhesko Institute of Cardiology of NAMSU, Kyiv, KIEV Governorate, 03680, Ukraine|Medical Center of Revmotsentr LLC, Kyiv, KIEV Governorate, 04070, Ukraine|Medical Center of Limited Liability Company Medical Clinic Blagomed, Kyiv, KIEV Governorate, 1023, Ukraine|Med Center of International Institute of Clinical Trials LLC; Medical Center "OK!Clinic+", Kyiv, KIEV Governorate, 2091, Ukraine|Lviv Regional Clinical Hospital Dept of Rehmuaatology D. Halytskyi Lviv NMU, Lviv, KIEV Governorate, 79010, Ukraine|CH of State Border Service of Ukraine (Military Base 2522); Dept of Therapy, D.Halytskyi Lviv NMU, Lviv, KIEV Governorate, 79014, Ukraine|A.Novak Transcarpathian Regional Clinical Hospital, Uzhgorod, KIEV Governorate, 88018, Ukraine|National Pirogov Memorial Medical University, Vinnytsia, Podolia Governorate, 21018, Ukraine|Railway Transp DCH of HealthCenter Branch of PJSC Ukr Railway Dept of Rheumatology, Dnipro, Tavria Okruha, 49008, Ukraine|City Clinical Hospital #9 Dept of Therapy SI Zaporizhzhia MA of PGE of MoHU, Zaporizhzhia, Tavria Okruha, 69065, Ukraine|CI City Hospital #1, Zaporizhzhia, Tavria Okruha, 69104, Ukraine|CI Lutsk CCH Volyn Regional Center of Cardiovascular Pathology and Thrombolysis, Lutsk, Volhynian Governorate, 43024, Ukraine|GI L.T.Malaya Therapy National Institute of the NAMS of Ukraine, Kharkiv, 61039, Ukraine|CNI Consultative and Diagnostic Center of Desnianskyi District of Kyiv, Kyiv, 02232, Ukraine|M.V. Sklifosovsky Poltava RCH Dept of Rheumatology HSEIU UMSA, Poltava, 36011, Ukraine|CI City Hospital #7, Zaporizhzhia, 69118, Ukraine|CI Zaporizhzhia Regional Clinical Hospital of ZRC, Zaporizhzhia, 69600, Ukraine Less <<
NCT03407482 Lupus Erythematosus, Systemic PHASE2 TERMINATED 2019-11-20 Valerius Medical Group, Los Al... More >>amitos, California, 90720, United States|RASF-Clinical Research Center, Boca Raton, Florida, 33486, United States|Bay Area Arthritis and Osteoporosis, Brandon, Florida, 33511, United States|Clinical Research of West Florida, Clearwater, Florida, 33765, United States|Institute of Arthritis Research, Idaho Falls, Idaho, 83404, United States|Ochsner Clinic Foundation, Baton Rouge, Louisiana, 70809, United States|Shanahan Rheumatology & Immunology, PLLC, Raleigh, North Carolina, 27617, United States|Tekton Research Inc, Austin, Texas, 78745, United States|Accurate Clinical Research, Houston, Texas, 77058-3675, United States|Accurate Clinical Research, Houston, Texas, 77089, United States|Arthritis Clinic Of Central Texas, San Marcos, Texas, 78666, United States|APRILLUS, Buenos Aires, C1194AAO, Argentina|Hospital Italiano de La Plata, La Plata, 1900, Argentina|CER San Juan Centro Polivalente de Asistencia e Investigacion Clinica, San Juan, 5400, Argentina|Centro Médico Privado de Reumatología, San Miguel de Tucuman, T4000AXL, Argentina|CIP - Centro Internacional de Pesquisa, Goiania, GO, 74110-120, Brazil|Centro Mineiro de Pesquisa - CMIP, Juiz de Fora, MG, 36036-330, Brazil|Edumed - Educa??o e Saúde SA, Curitiba, PR, 80440-080, Brazil|Centro de Pesquisas em Diabetes - CPD, Porto Alegre, RS, 90035-170, Brazil|Clinica de Neoplasias Litoral, Itajai, SC, 88301-220, Brazil|Faculdade de Medicina do ABC - FMABC, Santo Andre, SP, 09060-650, Brazil|Centro Multidisciplinar de Estudos Clínicos - CEMEC*X*, Santo Andre, SP, 09190-510, Brazil|Centro de Pesquisas Clinicas; CPCLIN, Sao Paulo, SP, 01228-200, Brazil|Hospital Abreu Sodré - AACD, Sao Paulo, SP, 04023-000, Brazil|MHAT Plovdiv, Plovdiv, 4003, Bulgaria|Medical Center "Teodora", EOOD, Ruse, 7000, Bulgaria|Medical Center Excelsior OOD, Sofia, 1000, Bulgaria|UMHAT "Sv. Ivan Rilski", EAD, Sofia, 1431, Bulgaria|MC "Synexus - Sofia", EOOD, Sofia, 1784, Bulgaria|Medical Center "Nov Rehabilitatsionen Tsentar", EOOD, Stara Zagora, 6000, Bulgaria|CTR Estudios SPA, Providencia, 7500571, Chile|Dermacross, Santiago, 66901, Chile|Centro de Estudios Reumatologi, Santiago, 7501126, Chile|Biomedica, Santiago, Chile|Centro Integral de Reumatologia del Caribe SAS CIRCARIBE SAS, Barranquilla, 00000, Colombia|Centro de Investigacion Medico Asistencial S.A.S, Barranquilla, 80020, Colombia|Medicity S.A.S., Bucaramanga, 680003, Colombia|Servimed S.A.S., Bucaramanga, 680003, Colombia|Hospital Pablo Tobon Uribe, Medellin, 050034, Colombia|Konkuk University Medical Center, Seoul, 05030, Korea, Republic of|Centro de Investigacion Alberto Bazzoni S.A. de C.V., Torreon, Coahuila, 27000, Mexico|Unidad de Atencion Medica e Investigacion en Salud S.C., Mérida, Yucatan, 97000, Mexico|Hospital Angeles Lindavista, Mexico, 07760, Mexico|Hospital Universitario de Saltillo, Saltillo, 25000, Mexico|Hospital Central Dr. Ignacio Morones Prieto, San Luis Potosi S.l.p., 78240, Mexico|Fundación Profesor Novoa Santos, A Coruna, LA Coru?a, 15006, Spain|Hospital Universitari Vall d'Hebron, Barcelona, 08035, Spain|Hospital General Universitario Gregorio Mara?on, Madrid, 28007, Spain|Hospital Clinico Universitario Valladolid, Valladolid, 47005, Spain|Hospital Universitario Rio Hortega, Valladolid, 47012, Spain|Kaohsiung Chang Gung Memorial Hospital, Kaohsiung City, 00833, Taiwan|National Taiwan University Hospital, Taipei, 10002, Taiwan|Guy's Hospital; Louise Coote Lupus Unit, London, SE1 9RT, United Kingdom Less <<
NCT03693625 Urticaria PHASE2 TERMINATED 2019-10-23 Clinical Research Center of Al... More >>abama, LLC, Birmingham, Alabama, 35209, United States|Allergy & Asthma Immunology Associates, Scottsdale, Arizona, 85251, United States|Kern Allergy Med Clinic, Inc., Bakersfield, California, 93301, United States|Southern California Research Center, Mission Viejo, California, 92691, United States|Allergy & Asthma Consultants, Redwood City, California, 94063, United States|Integrated Research Group Inc, Riverside, California, 92506, United States|Renstar Medical Research, Ocala, Florida, 34470, United States|Vital Prospects Clinical Research Institute PC - CRN, Tulsa, Oklahoma, 74136, United States|Asthma, Nasal Disease, and Allergy Research Center of New England, East Providence, Rhode Island, 02914, United States|Timber Lane Allergy and Asthma Research, LLC, Burlington, Vermont, 05403, United States Less <<
NCT01991184 Lymphocytic Leukemia, Chronic,... More >> Diffuse Large B-Cell Lymphoma Less << PHASE1 COMPLETED 2022-03-08 Stanford Cancer Center, Stanfo... More >>rd, California, 94305-5820, United States|Washington University School of Medicine, Saint Louis, Missouri, 63110, United States|The Ohio State University Wexner Medical Center, Columbus, Ohio, 43212, United States|Willamette Valley Cancer Ctr - 520 Country Club, Eugene, Oregon, 97401-8122, United States|Oregon Health Sciences Uni, Portland, Oregon, 97239, United States|Sarah Cannon Cancer Center - Tennessee Oncology, Pllc, Nashville, Tennessee, 37203, United States|Seattle Cancer Care Alliance, Seattle, Washington, 98109, United States|Princess Alexandra Hospital Woolloongabba; Clinical Hematology and Medical Oncology, Woolloongabba, Queensland, 4102, Australia|Peter MacCallum Cancer Centre; Department of Haematology, Melbourne, Victoria, 3002, Australia|Linear Clinical Research Limited, Nedlands, Western Australia, 6009, Australia Less <<
NCT03596632 Healthy Participants PHASE1 COMPLETED 2018-08-23 Covance Clinical Research Unit... More >>, Inc, Madison, Wisconsin, 53704, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.50mL

0.30mL

0.15mL

7.52mL

1.50mL

0.75mL

15.04mL

3.01mL

1.50mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

Historical Records

Categories