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Chemical Structure| 1448169-71-8 Chemical Structure| 1448169-71-8

Structure of Futibatinib
CAS No.: 1448169-71-8

Chemical Structure| 1448169-71-8

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FGFR-IN-1 is a potent and highly selective FGFR inhibitor, used for antitumor treatment.

Synonyms: TAS-120

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Product Details of Futibatinib

CAS No. :1448169-71-8
Formula : C22H22N6O3
M.W : 418.45
SMILES Code : C=CC(N1C[C@@H](N2N=C(C#CC3=CC(OC)=CC(OC)=C3)C4=C(N)N=CN=C42)CC1)=O
Synonyms :
TAS-120
MDL No. :MFCD29037352
InChI Key :KEIPNCCJPRMIAX-HNNXBMFYSA-N
Pubchem ID :71621331

Safety of Futibatinib

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

Related Pathways of Futibatinib

RTK

Isoform Comparison

Biological Activity

Target
  • FGFR2

    FGFR2, IC50:1.4 nM

  • FGFR3

    FGFR3, IC50:1.6 nM

  • FGFR4

    FGFR4, IC50:3.7 nM

  • FGFR1

    FGFR1, IC50:1.8 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
MCF10A cells 0.2 µM 3 hours 45 minutes To assess the effect of Futibatinib on FGFR signaling pathways, results showed Futibatinib significantly inhibited phosphorylation of Akt and ERK1/2 PMC10657448
ICC13-7 cells 10 nM 4 hours Evaluate the signaling inhibition effect of Futibatinib on FGFR2-PHGDH fusion protein PMC10767308
CCLP-1 cells 50 nM 4 hours Evaluate the signaling inhibition effect of Futibatinib on FGFR2-PHGDH fusion protein PMC10767308
H69-FGFR2-BICC1/BRAF V600E cells 40 μM 72 hours To evaluate the impact of BRAF V600E mutation on Futibatinib sensitivity, results showed BRAF V600E mutation significantly reduced the inhibitory effect of Futibatinib. PMC11900356
H69-FGFR2-BICC1/KRAS G12D cells 40 μM 72 hours To evaluate the impact of KRAS G12D mutation on Futibatinib sensitivity, results showed KRAS G12D mutation significantly reduced the inhibitory effect of Futibatinib. PMC11900356
H69 cells 12.5 nM 72 hours To evaluate the sensitivity of Futibatinib in FGFR2-BICC1 fusion cells, results showed Futibatinib significantly inhibited the growth of fusion cells. PMC11900356
SCMC 11.7 µM 72 hours Evaluate the inhibitory effect of Futibatinib on SCMC cells, results show Futibatinib has weaker inhibitory effect on SCMC cells. PMC10452847
RH4 6.64 µM 72 hours Evaluate the inhibitory effect of Futibatinib on RH4 cells, results show Futibatinib has weaker inhibitory effect on RH4 cells. PMC10452847
RMS559 0.48 µM 72 hours Evaluate the inhibitory effect of Futibatinib on RMS559 cells, results show Futibatinib significantly inhibits cell growth. PMC10452847
Ba/F3 TEL-FGFR4 1.33 nM 72 hours Evaluate the inhibitory effect of Futibatinib on Ba/F3 TEL-FGFR4 cells, results show Futibatinib selectively kills cells through FGFR4 inhibition. PMC10452847

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Rat Sprague-Dawley rats Oral 10 mg/kg Single dose For pharmacokinetic study, to determine the concentration of orelabrutinib in plasma PMC9486086
Female athymic nude mice Breast cancer PDX models Oral 15 mg/kg Daily for 28 days or until tumor diameter reached 1.5 cm3 To evaluate the antitumor activity of Futibatinib in FGFR-altered breast cancer PDX models, results showed significant tumor growth inhibition in FGFR2-amplified and FGFR2 Y375C mutant models PMC10657448
Nude mice FGFR2-BICC1 and FGFR2-BICC1/KRAS G12D xenograft models Oral gavage 5 mg/kg Futibatinib and 6 mg/kg Binimetinib Once daily for 14 days To evaluate the antitumor effect of Futibatinib alone or in combination with Binimetinib in FGFR2-BICC1 and FGFR2-BICC1/KRAS G12D xenograft models, results showed combination therapy significantly inhibited tumor growth in FGFR2-BICC1 model but had limited effect in FGFR2-BICC1/KRAS G12D model. PMC11900356
NOD SCID Gamma (NSG) mice RMS559, RH4, and SCMC xenograft models Oral gavage 5-25 mg/kg Once daily for three weeks Evaluate the efficacy of Futibatinib monotherapy in RMS xenograft models, results show Futibatinib monotherapy had no significant effect on tumor growth or survival. PMC10452847
NOD/SCID gamma mice Patient-derived xenograft (PDX) model Not used 6 mg/kg Once daily for up to 50 days Evaluate the antitumor activity of Futibatinib against FGFR2 kinase domain mutations in PDX models PMC7616615
NSG mice CCLP-1 xenograft model Oral gavage 6 mg/kg Once daily for 10 days Evaluate the in vivo efficacy of Futibatinib on FGFR2-PHGDH-N550K mutant tumors PMC10767308
NSG mice CCLP-1 xenograft model Oral gavage 6 mg/kg Once daily for 10 days Evaluate the in vivo efficacy of futibatinib against FGFR2-N550K mutation PMC10767308

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT05727176 Advanced Cholangiocarcinoma|FG... More >>FR2 Fusions|Gene Rearrangement Less << PHASE2 RECRUITING 2025-12-26 University of California San D... More >>iego UCSD - Moores Cancer Center, La Jolla, California, 92093, United States|Tampa General Hospital Cancer Institute, Tampa, Florida, 33606, United States|Henry Ford Health System, Detroit, Michigan, 48202, United States|Gabrail Cancer Center Research, Canton, Ohio, 44718, United States|Texas Oncology, Abilene, Texas, 79606-5208, United States|The Liver Institute at Methodist Dallas Medical Center, Dallas, Texas, 75203, United States|Texas Onc Methodist (Charlton), Dallas, Texas, 75237, United States|Center for Oncology and Blood Disorders, Houston, Texas, 77030, United States|CEMIC, Caba, 1431, Argentina|Hospital Britanico, Ciudad Autonoma de Buenos Aires, AEB1280, Argentina|Sanatorio de la Mujer, Rosario, S2013, Argentina|St Vincent's Hospital Sydney - The Kinghorn Cancer Centre, Sydney, New South Wales, 2010, Australia|Alfred Health, Medical Oncology Unit, Second floor William Buckland Radiotherapy Center, Melbourne, Victoria, 3004, Australia|St John of God Subiaco Hospital, Subiaco, Western Australia, 6008, Australia|Instituto do Cancer do Estado de Sao Paulo, Cerqueira César, 01246-000, Brazil|IOP - Instituto de Oncologia do Parana, Curitiba, 80530-010, Brazil|Hospital Erasto Gaertner, Curitiba, 81520-060, Brazil|Hospital de Base de Sao Jose do Rio Preto, S?o José Do Rio Preto, 15090-000, Brazil|Fundacao Antonio Prudente - A.C.Camargo Cancer Center, S?o Paulo, 01508-010, Brazil|Guangdong Provincial People's Hospitall, Guangzhou, Guangdong, 510080, China|Harbin Medical University - Cancer Hospital, Harbin, Heilongjiang, China|Jilin Cancer Hospital, Changchun, Jilin, 130028, China|Shandong University - Shandong Cancer Hospital, Jinan, Shandong, 250117, China|West China Hospital- Sichuan University, Chengdu, Sichuan, 610041, China|Sir Run Run Shaw Hospital, Zhejiang University, Hangzhou, Zhejiang, 310016, China|Shanghai Gobroad Cancer Hospital China Pharmaceutical University, Shanghai, 200123, China|Tongji University Shanghai East Hospital, Shanghai, China|The University of Hong Kong, Hong Kong Island, 999077, Hong Kong|The Chinese University of Hong Kong Prince of Wales Hospital, New Territories, 999077, Hong Kong|Policlinico S. Orsola-Malpighi, Bologna, 40138, Italy|IRCCS Humanitas Research Hospital, Rozzano, 20089, Italy|AOUI Verona - Ospedale Borgo Roma, Verona, 37134, Italy|Tohoku University Hospital, Sendai, Miyagi, 980-8574, Japan|National Cancer Center Hospital East, Kashiwa-Shi, 277-0882, Japan|Nagasaki University Hospital, Nagasaki-shi, 852-8501, Japan|Nagoya University Hospital, Nagoya-shi, 466-8560, Japan|Osaka Metropolitan University Hospital, Osaka-Fu, 558-8585, Japan|Inje University Haeundae Paik Hospital, Busan, 48108, Korea, Republic of|Dong-A University Hospital, Busan, 49201, Korea, Republic of|Kyungpook National University Hospital, Daegu, 41944, Korea, Republic of|Gyeongsang National University Hospital, Jinju, 52727, Korea, Republic of|CHA Bundang Medical Center, Seongnam, 13532, Korea, Republic of|Yonsei University Health System - Severance Hospital, Seoul, 03722, Korea, Republic of|The Catholic University of Korea, St. Mary's Hospital, Seoul, 06591, Korea, Republic of|Szpital Wojewdzki w Koszalinie im. Mikoaja Kopernika, Koszalin, 75-581, Poland|Centrum Onkologii Ziemi Lubelskiej im. w. Jana z Dukli, Lublin, 20-0920, Poland|Europejskie Centrum Zdrowia Otwock Sp. Z.o.o., Otwock, 05-400, Poland|Centrum Onkologii-Instytut im. Marii Sk?odowskiej - Curie, Warszawa, 02-034, Poland|Funda??o Champalimaud, Lisboa, 1400-038, Portugal|Centro Hospitalar Lisboa Norte CHLN EPE - Hospital de Santa Maria, Lisbon, 1649-035, Portugal|Hospital Vall d'Hebron, Barcelona, 08035, Spain|Institut Català d'Oncologia de l'Hospitalet de Llobregat - Hospital Duran i Reynals, Barcelona, 08908, Spain|Hospital General Universitario Gregorio Maranon, Madrid, 28007, Spain|Clinica Universidad de Navarra, Medical Oncology Service (Mariano Ponz Sarvise), Madrid, 28027, Spain|Hospital Universitario Fundación Jimenez Díaz, Madrid, 28040, Spain|Hospital Universitario 12 de octubre, Madrid, 28043, Spain|Clinica Universidad de Navarra, Pamplona, 31008, Spain Less <<
NCT04507503 Advanced Cholangiocarcinoma APPROVED_FOR_MARKETING - Banner MD Anderson, Gilbert, A... More >>rizona, 85234, United States|University of California, San Francisco (UCSF), San Francisco, California, 94143, United States|UCLA Division of Hematology-Oncology, Santa Monica, California, 90404, United States|Mount Sinai Center of Florida, Miami Beach, Florida, 33140, United States|Advent Health Orlando, Orlando, Florida, 32804, United States|University of Chicago, Chicago, Illinois, 60637, United States|Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins, Baltimore, Maryland, 21231, United States|Massachusetts General Hospital, Boston, Massachusetts, 02114, United States|Dana Farber Cancer Institute, Boston, Massachusetts, 02215, United States|University of Kansas Cancer Center, Lee's Summit, Missouri, 64064, United States|Duke University Medical Center, Durham, North Carolina, 27710, United States|Providence Portland Medical Center, Portland, Oregon, 97213, United States|MD Anderson, Houston, Texas, 77030, United States|Utah Cancer Specialists, Salt Lake City, Utah, 84106, United States|Seattle Cancer Care Alliance, Seattle, Washington, 98109, United States|Aurora Cancer care, Grafton, Wisconsin, 53024, United States Less <<
NCT02052778 Cholangiocarcinoma|Urothelial ... More >>Cancer|Advanced and Metastatic Cancer Patients With Tumors Harboring FGF/FGFR Tumors|Primary CNS Tumors|Breast Cancer|Gastric Cancer Less << PHASE1|PHASE2 COMPLETED 2021-05-29 Banner MD Anderson Cancer Cent... More >>er, Gilbert, Arizona, 85234, United States|Mayo Clinic (AZ), Scottsdale, Arizona, 85259, United States|The University of Arizona Cancer Center - North Campus, Tucson, Arizona, 85719, United States|City of Hope National Medical Center, Duarte, California, 91010, United States|UCSF Helen Diller Family Comprehensive Cancer Center. Mission Bay, San Francisco, California, 94158, United States|Cancer Treatment Centers of America, Newnan, Georgia, 30265, United States|Cancer Treatment Centers of America Zion, IL, Zion, Illinois, 60099, United States|The University of Kansas Cancer Center, Fairway, Kansas, 66205, United States|Massachusetts General Hospital, Boston, Massachusetts, 02114, United States|Dana Farber Cancer Institution, Boston, Massachusetts, 02215, United States|Wayne State Universtity (Karmanos Cancer Institute), Detroit, Michigan, 48201, United States|Mayo Clinic (MN), Rochester, Minnesota, 55905, United States|New Mexico Cancer Care Alliancer, Albuquerque, New Mexico, 87106, United States|Roswell Park Cancer Institute, Buffalo, New York, 14263, United States|Hospital of the University of Pennsylvania, Philadelphia, Pennsylvania, 19104, United States|Sidney Kimmel Cancer Center at Jefferson, Philadelphia, Pennsylvania, 19107, United States|University of Pittsburgh Medical Center Hillman Cancer Center, Pittsburgh, Pennsylvania, 15232, United States|Greenville Health System ITOR,Clinical Research Unit, Greenville, South Carolina, 29605, United States|Spartanburg Medical Center, Spartanburg, South Carolina, 29303, United States|Mary Crowley Cancer Research - Medical City, Dallas, Texas, 75230, United States|The University of Texas MD Anderson Cancer Center, Houston, Texas, 77030, United States|University of Utah, Huntsman Cancer Hospital, Salt Lake City, Utah, 84112, United States|University of Virginia Cancer Center, Charlottesville, Virginia, 22903, United States|Virginia Mason Cancer Center, Seattle, Washington, 98101, United States|University of Wisconsin Clinical Science Center, Madison, Wisconsin, 53792, United States|Medical College of Wisconsin, Milwaukee, Wisconsin, 53226, United States|Royal Melbourne Hospital, Melbourne, Australia|Sunnybrook Research Institue, Toronto, M4N3M5, Canada|Centre Léon Bérard Bat, Lyon, Cedex, 69373, France|Institut Bergonie, Bordeaux, 33076, France|Hospices Civils de Lyon, Bron, 69677, France|Pitié-Salpêtrière Hospital, Paris, 75013, France|Rennes, Centre Eugène Marquis, Rennes cedex, 35042, France|Institute Goustave-Roussy-DITEP, Villejuif, 94805, France|University Hospital Essen, West German Cancer Center, Department of Medical Oncology, Essen, 45147, Germany|The Chinese University of Hong Kong, Sha Tin, Hong Kong|Fondazione I.R.C.C.S. Istituto Neurologico Carlo Besta, Milano, 20133, Italy|UOC Oncologia Medica 1 I"V - Istituto Oncologico Veneto - IRCCS, Padova, 35128, Italy|Hokkaido University Hospital, Hokkaido, 060-8648, Japan|Kyoto University Hospital, Department of Clinical Pharmacology and Therapeutics, Kyoto, 606-8507, Japan|Tohoku University Hospital, Miyagi, 980-8574, Japan|Osaka International Cancer Institute, Osaka, 541-8567, Japan|National Cancer Center Hospital, Tokyo, 104-0045, Japan|Yonsei University, Severance Hospital (Seoul), Seoul, 03722, Korea, Republic of|ASAN Medical Center (Seoul), Seoul, 05505, Korea, Republic of|Samsung Medical Center (Seoul), Seoul, 06351, Korea, Republic of|Seoul National University Hospital, Seoul, 110-744, Korea, Republic of|University Hospital Jenna, Jenna, 07740, Netherlands|Val D'Hebron University Hospital, Barcelona, 08035, Spain|Hospital Clinic i Provincial de Barcelona,, Barcelona, 08036, Spain|University Hospital Ramón y Cajal, Madrid, 28034, Spain|Centro Integral Oncológico Clara Campal - Hospital Universitario Madrid Sanchinarro, Madrid, Spain|Cheng Kung University Hospital, Tainan, 704, Taiwan|National Taiwan University Hospital, Taipei, 10048, Taiwan|Guy's and St Thomas' NHS Foundation Trust, London, SE1 9RT, United Kingdom|Sarah Cannon Research Institute, London, W1G 6AD, United Kingdom|University College London Hospital, London, W1T 7HA, United Kingdom|The Christie NHS Foundation Trust, Manchester, M20 4BX, United Kingdom Less <<
NCT04189445 Advanced or Metastatic Solid T... More >>umor|Advanced or Metastatic Gastric or Gastroesophageal Cancer|Myeloid or Lymphoid Neoplasms (MLN) Less << PHASE2 ACTIVE_NOT_RECRUITING 2025-03-31 Banner MD Anderson Cancer Cent... More >>er, Gilbert, Arizona, 85234-2165, United States|UCLA Medical Center, Los Angeles, California, 90404, United States|Georgetown University - Lombardi Comprehensive Cancer Center, Washington, District of Columbia, 20007, United States|University of Chicago Comprehensive Cancer Center, Chicago, Illinois, 60637, United States|University of Maryland, Baltimore, Maryland, 21201, United States|Beth Israel Deaconess Medical Center, Boston, Massachusetts, 02215-5400, United States|Henry Ford Hospital, Woodhaven, Michigan, 48183, United States|Mercy Clinic Oncology and Hematology - Coletta, Oklahoma City, Oklahoma, 73120, United States|Fox Chase Cancer Center, Philadelphia, Pennsylvania, 53705, United States|Houston Methodist Cancer Center, Houston, Texas, 77030, United States|The University of Texas M. D. Anderson Cancer Center, Houston, Texas, 77030, United States|Institut Jules Bordet, Bruxelles, 1000, Belgium|Centre Antoine Lacassagne, Nice, Alpes Maritimes, 06200, France|Centre Paul Strauss, Strasbourg, Bas Rhin, 67000, France|Centre Georges Fran?ois Leclerc, Dijon, C?te-d'Or, 21079, France|Institut Bergonié, Bordeaux, Gironde, 33076, France|H?pital Saint-Louis, Paris Cedex 10, Paris, 75475, France|Centre Léon Bérard, Lyon, Rhone, 69008, France|Centre Hospitalier Lyon Sud, Pierre Benite cedex, Rhone, 69495, France|Institut Gustave Roussy, Villejuif, Val De Marne, 94805, France|Universitaetsklinikum Freiburg, Freiburg, Baden Wuerttemberg, 79106, Germany|Universitaetsklinikum Heidelberg, Heidelberg, Baden Wuerttemberg, 69120, Germany|Universitaetsklinikum Koeln, Koeln, Nordrhein Westfalen, 50924, Germany|The University of Hong Kong, Hong Kong, Hong Kong|Hong Kong United Oncology Centre, Jordon, 0000, Hong Kong|Istituto Scientifico Romagnolo Per Lo Studio e La Cura Dei Tumori, Meldola, Forli - Cesena, 47014, Italy|Ospedale Sacro Cuore Don Calabria, Negrar, Verona, 37024, Italy|Azienda Ospedaliera Universitaria Careggi, Florence, 50134, Italy|IEO Istituto Europeo di Oncologia, Milano, 20141, Italy|Azienda Ospedaliera Universitaria Integrata Verona (Ospedale Borgo Trento), Verona, 37124, Italy|Aichi Cancer Center Hospital, Nagoya-shi, Aichi-Ken, 464-8681, Japan|National Cancer Center Hospital East, Kashiwa-shi, Chiba-Ken, 277-8577, Japan|NHO Shikoku Cancer Center, Matsuyama-shi, Ehime-Ken, 791-0280, Japan|Hokkaido University Hospital, Sapporo-shi, Hokkaido, 060-8648, Japan|Osaka University Hospital, Suita-shi, Osaka-Fu, 565-0871, Japan|National Cancer Center Hospital, Chuo-ku, Tokyo-To, 104-0045, Japan|Seoul National University Bundang Hospital, Seongnam, Gyeonggi-do, 13620, Korea, Republic of|Asan Medical Center, Seoul, 05505, Korea, Republic of|Seoul National University Hospital, Seul, 03080, Korea, Republic of|Severance Hospital, Yonsei University Health System, Seul, 03722, Korea, Republic of|Samsung Medical Center, Seul, 06351, Korea, Republic of|Antoni van Leeuwenhoek, Amsterdam, 1066 CX, Netherlands|Erasmus Medisch Centrum, Rotterdam, 3015 AA, Netherlands|Centro Hospitalar de Lisboa Central, E.P.E. - Hospital de Santo António dos Capuchos, Lisboa, 1169-050, Portugal|Funda??o Champalimaud, Lisboa, 4099-001, Portugal|Centro Hospitalar do Porto, E.P.E - Hospital de Santo Antonio, Porto, 4099-001, Portugal|National University Cancer Institute, Singapore, 119074, Singapore|Hospital Universitari Vall d'Hebron, Barcelona, 08035, Spain|Hospital Universitario Ramon y Cajal, Madrid, 28034, Spain|Hospital Universitario HM Madrid Sanchinarro, Madrid, 28050, Spain|Clinica Universidad de Navarra, Pamplona, 31008, Spain|Hospital Universitario Virgen Macarena, Sevilla, 41009, Spain|Instituto Valenciano de Oncologia IVO, Valencia, 46009, Spain|Hospital Clinico Universitario de Valencia, Valencia, 46010, Spain|Hospital Universitari i Politecnic La Fe, Valencia, 46026, Spain|Karolinska universitetssjukhuset - Solna, Solna, 171 64, Sweden|Akademiska Sjukhuset, Uppsala, 75185, Sweden|Acibadem Adana Hospital, Adana, 01130, Turkey|Acibadem Maslak Hospital, Istanbul, 34457, Turkey|Namik Kemal University, Tekirda?, 59100, Turkey|Sarah Cannon Research Institute UK, London, Greater London, W1G 6AD, United Kingdom Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.39mL

0.48mL

0.24mL

11.95mL

2.39mL

1.19mL

23.90mL

4.78mL

2.39mL

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

 

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