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Chemical Structure| 872511-34-7 Chemical Structure| 872511-34-7

Structure of Infigratinib
CAS No.: 872511-34-7

Chemical Structure| 872511-34-7

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Infigratinib (BGJ-398; NVP-BGJ398) demonstrates potent inhibition against the FGFR family, displaying IC50 values of 0.9 nM, 1.4 nM, 1 nM, and 60 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.

Synonyms: NVP-BGJ398; BGJ398; BGJ-398

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Product Details of Infigratinib

CAS No. :872511-34-7
Formula : C26H31Cl2N7O3
M.W : 560.48
SMILES Code : O=C(NC1=C(Cl)C(OC)=CC(OC)=C1Cl)N(C2=NC=NC(NC3=CC=C(N4CCN(CC)CC4)C=C3)=C2)C
Synonyms :
NVP-BGJ398; BGJ398; BGJ-398
MDL No. :MFCD22123241
InChI Key :QADPYRIHXKWUSV-UHFFFAOYSA-N
Pubchem ID :53235510

Safety of Infigratinib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of Infigratinib

RTK

Isoform Comparison

Biological Activity

Target
  • FGFR2

    FGFR2, IC50:1.4 nM

  • FGFR3

    FGFR3 (K650E), IC50:4.9 nM

    FGFR3, IC50:1.0 nM

  • FGFR4

    FGFR4, IC50:60 nM

  • FGFR1

    FGFR1, IC50:0.9 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
G401 cells 100 nM 5 min to 24 h The phosphoproteome of G401 cells was measured in response to Infigratinib, showing significant downregulation of phosphorylation at FRS2 S428 and GAB1 T503, indicating inhibition of the FGFR signaling pathway by the drug. PMC10883282
HCC01-0909 cells 1 µM 24 h Inhibits FGF/FGFR signaling pathway and its downstream targets, leading to G1 cell cycle arrest PMC6635738
ICC13-7 100 nM 24 h Evaluate the sensitivity of ICC13-7 cells to Infigratinib, showing an IC50 of 12 nM. PMC9064956
ICC21 100 nM 24 h Evaluate the sensitivity of ICC21 cells to Infigratinib, showing an IC50 of ~250 nM. PMC9064956
ICC10-6 100 nM 24 h Evaluate the sensitivity of ICC10-6 cells to Infigratinib, showing an IC50 >1000 nM, indicating resistance to Infigratinib. PMC9064956
PDXO67 300 nM 30 min To confirm FGFR2c activation via endogenous FGF2 PMC10703877
PDXO67 300 nM 72 h To evaluate the effect of BGJ398 on proliferation and cell death in PDXO67 PMC10703877
MPM cell lines 0.1 to 10 µM 72 h To evaluate the sensitivity of MPM cell lines to Infigratinib, 3 out of 13 cell lines were sensitive to Infigratinib, 4 were resistant, and the remaining 6 showed intermediate sensitivity. PMC6769772
ICC13-7 cells 100 nM 24 h To investigate the effect of Infigratinib on glucose metabolism in ICC13-7 cells, the results showed that Infigratinib significantly suppressed glycolytic gene expression and reduced glucose uptake and lactate secretion. PMC11076599
ICC21 cells 100 nM 24 h To investigate the effect of Infigratinib on glucose metabolism in ICC21 cells, the results showed that Infigratinib significantly suppressed glycolytic gene expression and reduced glucose uptake and lactate secretion. PMC11076599

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C.B-17 SCID mice HCC PDX xenograft model Oral 10, 20, 30 mg/kg Once daily for 14 days Infigratinib significantly inhibits tumor growth, reduces tumor burden, and suppresses FGFR signaling pathway and its downstream targets PMC6635738
Mice ICC21 subcutaneous xenograft model Oral 15 mg/kg Daily for 21 days Evaluate the efficacy of Infigratinib combined with Afatinib in the ICC21 subcutaneous xenograft model, showing significant tumor regression with combination therapy. PMC9064956
NSG mice C666-1 xenograft model oral 30 mg/kg once daily for 14 days Evaluate the antitumor effect of Infigratinib on the C666-1 xenograft model, results showed that Infigratinib significantly inhibited tumor growth PMC8993121
Mice NSG mice Oral 30 mg/kg Once daily for 21 days To evaluate the effect of Infigratinib on tumor growth inhibition and survival in EC PDX models PMC10703877
mice ICC13-7 xenograft model oral 15 mg/kg once daily for 10 days To investigate the effect of Infigratinib on tumor growth in the ICC13-7 xenograft model, the results showed that Infigratinib significantly inhibited tumor growth and reduced glucose uptake. PMC11076599

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02706691 FGFR Gene Amplification|FGFR1 ... More >>Gene Amplification|FGFR2 Gene Amplification|FGFR2 Gene Mutation|FGFR3 Gene Mutation|Head and Neck Squamous Cell Carcinoma|Human Papillomavirus Infection|Recurrent Head and Neck Carcinoma|Recurrent Nasopharynx Carcinoma|Recurrent Oropharyngeal Squamous Cell Carcinoma Less << PHASE2 TERMINATED 2019-02-11 University of Chicago Comprehe... More >>nsive Cancer Center, Chicago, Illinois, 60637, United States Less <<
NCT04424966 Glioma|Glioblastoma|GBM EARLY_PHASE1 TERMINATED 2023-04-27 Chandler Regional Medical Cent... More >>er, Chandler, Arizona, 85224, United States|St. Joseph's Hospital and Medical Center, Phoenix, Arizona, 85013, United States|HonorHealth Scottsdale Osborn Medical Center, Scottsdale, Arizona, 85251, United States Less <<
NCT02657486 Bladder Cancer|Non-Muscle-Inva... More >>sive Urothelial Carcinoma Less << ACTIVE_NOT_RECRUITING 2025-01-26 Memorial Sloan Kettering Cance... More >>r Center, New York, New York, 10065, United States Less <<
NCT03510455 Tumor-Induced Osteomalacia|Onc... More >>ogenic Osteomalacia Less << PHASE2 TERMINATED 2020-05-04 National Institutes of Health ... More >>Clinical Center, Bethesda, Maryland, 20892, United States Less <<
NCT05019794 Gastric Cancer|Gastroesophagea... More >>l Junction Adenocarcinoma|Solid Tumor Less << PHASE2 UNKNOWN 2023-12-30 Beijing Cancer Hospital ( Depa... More >>rtment of Thoracic Oncology ), Beijing, Beijing, 100142, China|Beijing Cancer Hospital (Department of Gynecological Oncology), Beijing, Beijing, 100142, China|Beijing Cancer Hospital, Beijing, Beijing, 100142, China|Fujian Medical University Union Hospital, Fuzhou, Fujian, 350001, China|Fujian Cancer Hospital, Fuzhou, Fujian, 350014, China|The Sixth Affiliated Hospital, Sun Yat-sen University, Guangzhou, Guangdong, 510655, China|Affiliated Hospital of Hebei University, Baoding, Hebei, 071030, China|Harbin Medical University Cancer Hospital, Harbin, Heilongjiang, 150081, China|Hubei Cancer Hospital, Wuan, Hubei, 430079, China|The First People's Hospital of Changzhou, Changzhou, Jiangsu, 213004, China|Nanjing Drum Tower Hospital, Nanjing, Jiangsu, 210008, China|Liaoning Cancer Hospital & Institute, Shenyang, Liaoning, 110042, China|Zhongshan Hospital Fudan University, Shanghai, Shanghai, 200032, China|Shanxi Provincial Cancer Hospital, Taiyuan, Shanxi, 030013, China|The First Affiliated Hospital Zhejiang University School of Medicine, Hangzhou, Zhejiang, 310003, China|Sir Run Run Shaw hospital, Zhejiang University school of Medicine, Hangzhou, Zhejiang, 310016, China|Henan Cancer Hospital, Henan, Zhengzhou, 450008, China Less <<
NCT05222165 Advanced Solid Tumor|CNS Tumor... More >>|Recurrent WHO Grade II Glioma Less << PHASE1|PHASE2 WITHDRAWN 2022-12-16 Lucile Packard Children's Hosp... More >>ital at Stanford University Medical Center, Palo Alto, California, 94304, United States|Children's National Hospital - Brain Tumor Institute, Washington, District of Columbia, 20010-2916, United States|Nicklaus Children's Hospital, Miami, Florida, 33155, United States|Memorial Sloan Kettering Cancer Center, New York, New York, 10065, United States|Duke Cancer Institute (DCI) - The Preston Robert Tisch Brain Tumor Center, Durham, North Carolina, 27702-3624, United States|UPCM - Children's Hospital of Pittsburgh, Pittsburgh, Pennsylvania, 15224-1529, United States|University of Alberta - Stollery Children's Hospital (SCH), Edmonton, Alberta, T6G 2B7, Canada|McMaster Children's Hospital (MCH), Hamilton, Ontario, L8N 3Z5, Canada|University of Toronto - The Hospital for Sick Children (SickKids), Toronto, Ontario, M5G 1X8, Canada|Universitaetsklinikum Heidelberg (UKHD) - Zentrum fuer Kinder- und Jugendmedizin - Klinik Kinderheilkunde III, Heidelberg, Baden-Wuerttemberg, 69120, Germany Less <<
NCT01975701 Recurrent Glioblastoma or Othe... More >>r Glioma Subtypes Less << PHASE2 COMPLETED 2018-10-03 Novartis Investigative Site, L... More >>os Angeles, California, 90095, United States|University of California San Francisco Dept of Onc., San Francisco, California, 94101, United States|Novartis Investigative Site, Chicago, Illinois, 60611, United States|Novartis Investigative Site, Boston, Massachusetts, 02215, United States|Novartis Investigative Site, New York, New York, 10032, United States|Novartis Investigative Site, Columbus, Ohio, 43221, United States|Novartis Investigative Site, Dallas, Texas, 75246, United States|Novartis Investigative Site, Dallas, Texas, 75251, United States|Novartis Investigative Site, Houston, Texas, 77030, United States|Novartis Investigative Site, Melbourne, Victoria, 3050, Australia|Novartis Investigative Site, Leuven, 3000, Belgium|University Medical Center Utrecht, Utrecht, The Netherlands, 3508 GA, Netherlands|Novartis Investigative Site, Barcelona, Catalunya, 08035, Spain|Novartis Investigative Site, Hospitalet de LLobregat, Catalunya, 08907, Spain|Novartis Investigative Site, Madrid, 28041, Spain|Novartis Investigative Site, Madrid, 28050, Spain|Novartis Investigative Site, Zürich, 8091, Switzerland Less <<
NCT06206278 Gastric Cancer|Gastroesophagea... More >>l Junction Adenocarcinoma Less << PHASE2 TERMINATED 2024-05-31 Anhui Provincial Cancer Hospit... More >>al, Hefei, Anhui, 230031, China|The Second Hospital of Anhui Medical University, Hefei, Anhui, 230601, China|Beijing Cancer Center, Beijing, Beijing, 100142, China|The First Affiliated Hospital of Xiamen University, Xiamen, Fujian, China|The Second Hospital Lanzhou University, Lanzhou, Gansu, 730030, China|Dongguan City People's Hospital, Dongguan, Guangdong, 523059, China|Guangzhou First People's Hospital, Guangzhou, Guangdong, 510180, China|The Sixth Affiliated Hospital, Sun Yat-sen University, Guangzhou, Guangdong, 510655, China|The Second Affiliated Hospital of Guilin Medical University, Guilin, Guangxi, 541199, China|Liuzhou People's Hospital, Liuzhou, Guangxi, 545006, China|Affiliated Hospital of Hebei University, Baoding, Hebei, 071030, China|Harbin Medical University Cancer Hospital, Harbin, Heilongjiang, 150081, China|The First Affiliated Hospital of Zhengzhou University, Zhengzhou, Henan, 450052, China|Tongji Hospital, Tongji Medical College of HUST, Wuhan, Hubei, 430030, China|Hubei Cancer Hospital, Wuhan, Hubei, 430079, China|Hunan Provincial People's Hospital, Changsha, Hunan, 410002, China|Nanjing Drum Tower Hospital, Nanjing, Jiangsu, 210008, China|Jilin Cancer Hospital, Changchun, Jilin, 130012, China|The First Hospital of China Medical University, Shenyang, Liaoning, 110002, China|The First Affiliated Hospital of Xi'an Jiaotong University, Xi'an, Shaanxi, China|Central Hospital Affiliated to Shandong First Medical University, Jinan, Shandong, 250013, China|Shandong Provincial Cancer Hosptial, Jinan, Shandong, 250117, China|The Affiliated Hospital of Qingdao University, Qingdao, Shandong, 266000, China|Zhongshan Hospital Fudan University, Shanghai, Shanghai, 200032, China|Shanxi Provincial Cancer Hospital, Taiyuan, Shanxi, 030013, China|West China Hospital of Sichuan University, Chengdu, Sichuan, 610041, China|Sichuan Cancer Hospital, Chengdu, Sichuan, 610042, China|Tianjin Medical University Cancer Institute&Hospital, Tianjin, Tianjin, 300060, China|Yunnan Cancer Hospital, Kunming, Yunnan, 650118, China|The First Affiliated Hospital Zhejiang University School of Medicine, Hangzhou, Zhejiang, 310013, China Less <<
NCT04972253 Bladder Transitional Cell Carc... More >>inoma|Bladder Cancer|Fibroblast Growth Factor Receptor Less << PHASE1 WITHDRAWN 2025-12-23 -
NCT01697605 Tumor With Alterations of the ... More >>FGF-R Less << PHASE1 COMPLETED 2019-02-07 Novartis Investigative Site, G... More >>uangzhou, Guangdong, 51000, China|Novartis Investigative Site, Chengdu, Sichuan, 610041, China|Novartis Investigative Site, Guangzhou, 510060, China|Nagoya University Hospital, Nagoya-city, Aichi, 466-8560, Japan|National Cancer Center Hospital East (NCEE), Kashiwa, Chiba, 277-8577, Japan|Novartis Investigative Site, Kobe-shi, Hyogo, 650-0017, Japan|Novartis Investigative Site, Sayama, Osaka, 589 8511, Japan|Shizuoka Cancer Center, Sunto-gun, Shizuoka, 411-8777, Japan Less <<
NCT04233567 Advanced Malignant Solid Neopl... More >>asm|Cholangiocarcinoma|Metastatic Malignant Solid Neoplasm|Refractory Malignant Solid Neoplasm Less << PHASE2 ACTIVE_NOT_RECRUITING 2025-12-31 Ohio State University Comprehe... More >>nsive Cancer Center, Columbus, Ohio, 43210, United States Less <<
NCT01004224 Advanced Solid Tumors With Alt... More >>erations of FGFR1, 2 and or 3|Squamous Lung Cancer With FGFR1 Amplification|Bladder Cancer With FGFR3 Mutation or Fusion|Advanced Solid Tumors With FGFR1 Amplication|Advanced Solid Tumors With FGFR2 Amplication|Advanced Solid Tumors With FGFR3 Mutation Less << PHASE1 COMPLETED 2018-10-08 Novartis Investigative Site, D... More >>uarte, California, 91010 3000, United States|Novartis Investigative Site, Los Angeles, California, 90033, United States|Novartis Investigative Site, Los Angeles, California, 90095, United States|University of Colorado Dept. of Anschutz Cancer (3), Aurora, Colorado, 80045, United States|Novartis Investigative Site, New Haven, Connecticut, 06520, United States|Novartis Investigative Site, Boston, Massachusetts, 02114, United States|Novartis Investigative Site, Detroit, Michigan, 48201, United States|Memorial Sloan Kettering Cancer Center Onc. Dept.., New York, New York, 10021, United States|Novartis Investigative Site, New York, New York, 10029, United States|Novartis Investigative Site, Columbus, Ohio, 43221, United States|Novartis Investigative Site, Philadelphia, Pennsylvania, 19104, United States|Thomas Jefferson University Hospital Onc Dept, Philadelphia, Pennsylvania, 19107-5098, United States|Novartis Investigative Site, Pittsburgh, Pennsylvania, 15232, United States|Novartis Investigative Site, Memphis, Tennessee, 38120, United States|Novartis Investigative Site, Nashville, Tennessee, 37203, United States|Novartis Investigative Site, Salt Lake City, Utah, 84103, United States|Novartis Investigative Site, Heidelberg, Victoria, 3084, Australia|Novartis Investigative Site, Vienna, A-1100, Austria|Novartis Investigative Site, Bordeaux Cedex, 33075, France|Novartis Investigative Site, Lyon Cedex, 69373, France|Novartis Investigative Site, Marseille, 13273, France|Novartis Investigative Site, Montpellier Cedex 5, 34298, France|Novartis Investigative Site, Paris, 75015, France|Novartis Investigative Site, Saint-Herblain Cédex, 44805, France|Novartis Investigative Site, Suresnes, 92150, France|Novartis Investigative Site, Toulouse Cedex 9, 31059, France|Novartis Investigative Site, Villejuif Cedex, 94805, France|Novartis Investigative Site, Koeln, Nordrhein-Westfalen, 50937, Germany|Novartis Investigative Site, Essen, 45147, Germany|Novartis Investigative Site, Hannover, 30625, Germany|Novartis Investigative Site, Marburg, 35039, Germany|Novartis Investigative Site, Ramat Gan, 5265601, Israel|Novartis Investigative Site, Tel Aviv, 6423906, Israel|Novartis Investigative Site, Meldola, FC, 47014, Italy|Novartis Investigative Site, Seoul, Korea, 05505, Korea, Republic of|Novartis Investigative Site, Seoul, 03080, Korea, Republic of|Novartis Investigative Site, Amsterdam, 1066 CX, Netherlands|Novartis Investigative Site, Amsterdam, 1081 HV, Netherlands|Novartis Investigative Site, Singapore, 169610, Singapore|Novartis Investigative Site, Sevilla, Andalucia, 41013, Spain|Novartis Investigative Site, Barcelona, Catalunya, 08035, Spain|Novartis Investigative Site, Valencia, Comunidad Valenciana, 46009, Spain|Novartis Investigative Site, Barcelona, 08041, Spain|Novartis Investigative Site, Madrid, 28009, Spain|Novartis Investigative Site, Madrid, 28041, Spain|Novartis Investigative Site, Madrid, 28050, Spain|Novartis Investigative Site, Taipei, 10048, Taiwan|Novartis Investigative Site, Bangkok, 10330, Thailand|Novartis Investigative Site, Chiang Mai, 50200, Thailand|Novartis Investigative Site, Izmir, 35040, Turkey Less <<
NCT02160041 Solid Tumor|Hematologic Malign... More >>ancies Less << PHASE2 TERMINATED 2018-04-30 Alabama Oncology St. Vincent's... More >> Birmingham, Birmingham, Alabama, 35211, United States|North County Oncology Medical Clinic Inc, Oceanside, California, 92056, United States|San Francisco General Hospital San Francisco Gen Hosp (7), San Francisco, California, 94110, United States|Rocky Mountain Cancer Centers Rocky Mountain Cancer Ctr (50), Greenwood Village, Colorado, 80304, United States|Norwalk Hospital, Norwalk, Connecticut, 06856, United States|Florida Cancer Specialists Florida Cancer Specialists 36, Fort Myers, Florida, 33901, United States|University of Miami Sylvester Comprehensive Cancer, Miami, Florida, 33136, United States|NorthWest Georgia Oncology Centers NW Georgia Oncology, Marietta, Georgia, 30060, United States|Harbin Clinic Medical Oncology Clin. Res., Rome, Georgia, 30165, United States|Illinois Cancer Specialists, Arlington Heights, Illinois, 60005, United States|Lurie Children's Hospital of Chicago Developmental Therapeutics, Chicago, Illinois, 60611, United States|Community Clinical Research Center, Anderson, Indiana, 46011, United States|Indiana University Indiana Univ. - Purdue Univ., Indianapolis, Indiana, 46202, United States|Northern Indiana Cancer Research Consortium No. Indiana Cancer Res., South Bend, Indiana, 46617, United States|University of Louisville / James Graham Brown Cancer Center SC, Louisville, Kentucky, 40202, United States|St. Agnes Hospital St. Agnes Hospital (2), Baltimore, Maryland, 21229, United States|Southcoast Centers for Cancer Care, Fairhaven, Massachusetts, 02719, United States|Cancer and Hematology Centers of West Michigan Dept. of Oncology, Grand Rapids, Michigan, 49546, United States|Minnesota Oncology Hematology, P.A. Minnesota Oncology Hem (27), Minneapolis, Minnesota, 55404, United States|Research Medical Center Research Med Center (2), Kansas City, Missouri, 64132, United States|Billings Clinic Billings Clinic (8), Billings, Montana, 59101, United States|Dartmouth Hitchcock Medical Center Dartmouth Hitchcock - Lebanon, Bedford, New Hampshire, 03110, United States|Rutgers Cancer Institute of New Jersey, New Brunswick, New Jersey, 08903, United States|New Mexico Cancer Center, Albuquerque, New Mexico, 87109, United States|Waverly Hematology Oncology, Cary, North Carolina, 27518, United States|University of N C at Chapel Hill Physician Office Building, Chapel Hill, North Carolina, 27599-7600, United States|Duke University Medical Center Seeley G. Mudd Bldg., Durham, North Carolina, 27710, United States|Wake Forest Baptist Health Hem & Onc Medical Center, Winston-Salem, North Carolina, 27157, United States|Sanford Hematology Oncology, Fargo, North Dakota, 58122, United States|Oncology Hematology Care Inc Oncology Hematology Care 2, Cincinnati, Ohio, 45242, United States|University Hospitals of Cleveland Seidman Cancer Center University Hospitals, Cleveland, Ohio, 44106, United States|Cleveland Clinic Foundation Taussig Cancer Institute, Cleveland, Ohio, 44195, United States|Bend Memorial Clinic Bend Mem. Clinic, Bend, Oregon, 97701, United States|Northwest Cancer Specialists Northwest Cancer, Portland, Oregon, 97210, United States|Lehigh Valley Health Network, Allentown, Pennsylvania, 18103, United States|Cancer Treatment Centers of America Eastern Regional Medical Center, Philadelphia, Pennsylvania, 19124, United States|University of Pittsburgh Cancer Institute Hillman Cancer Center (2), Pittsburgh, Pennsylvania, 15232, United States|Rhode Island Hospital Rhode Island Hosp. (2), Providence, Rhode Island, 02903, United States|Sanford University of South Dakota Medical Center Sanford Health, Sioux Falls, South Dakota, 57104, United States|Chattanooga Oncology and Hematology Assoicates, PC Chattanooga Oncology, Chattanooga, Tennessee, 37404, United States|Tennessee Oncology Tennessee Oncology (3), Nashville, Tennessee, 37203, United States|The Center for Cancer and Blood Disorders, Fort Worth, Texas, 76104, United States|Oncology Consultants Oncology Group, Houston, Texas, 77024, United States|Houston Methodist Cancer Center, Houston, Texas, 77030, United States|MD Anderson Cancer Center/University of Texas MD Anderson Cancer Center (3), Houston, Texas, 77030, United States|Texas Oncology, McAllen, Texas, 78503, United States|Cancer Therapy & Research Center UT Health Science Center Oncology Dept., San Antonio, Texas, 78229, United States|Texas Oncology Cancer Care & Research Center Texas Oncology, Waco, Texas, 76712, United States|Deke Slayton Cancer Center Deke Slayton Cancer Center (2), Webster, Texas, 77598, United States|Intermountain Medical Center Intermountain Healthcare, Murray, Utah, 84157, United States|Northern Utah Cancer Associates Northern Utah Assoc (3), Ogden, Utah, 84403, United States|University of Utah / Huntsman Cancer Institute SC-2, Salt Lake City, Utah, 84103, United States|Utah Cancer Specialists Utah Cancer Specialists (11), Salt Lake City, Utah, 84106, United States|Virginia Cancer Specialists Fairfax Northern Virginia, Fairfax, Virginia, 22031, United States|Shenandoah Oncology Shenandoah Oncology (5), Winchester, Virginia, 22601, United States|Northwest Medical Specialties NW Medical Specialties, Tacoma, Washington, 98405, United States Less <<

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