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Chemical Structure| 1265229-25-1 Chemical Structure| 1265229-25-1

Structure of Zoligratinib
CAS No.: 1265229-25-1

Chemical Structure| 1265229-25-1

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CH5183284 is a selective and orally available FGFR inhibitor with IC50 of 9.3 nM, 7.6 nM, 22 nM, and 290 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.

Synonyms: Debio 1347; CH5183284; FF284

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Product Details of Zoligratinib

CAS No. :1265229-25-1
Formula : C20H16N6O
M.W : 356.38
SMILES Code : O=C(C1=C(N)N(C2=CC=C3C(NC(C)=N3)=C2)N=C1)C(N4)=CC5=C4C=CC=C5
Synonyms :
Debio 1347; CH5183284; FF284
MDL No. :MFCD28502053
InChI Key :BEMNJULZEQTDJY-UHFFFAOYSA-N
Pubchem ID :66555680

Safety of Zoligratinib

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

Related Pathways of Zoligratinib

RTK

Isoform Comparison

Biological Activity

Target
  • FGFR2

    FGFR2, IC50:7.6 nM

  • FGFR3

    FGFR3, IC50:22 nM

  • FGFR4

    FGFR4, IC50:290 nM

  • FGFR1

    FGFR1, IC50:9.3 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
MCF-7 cells 10 μM 48 h Inhibition of FGF receptor (FGFR) signaling, blocking FGF-induced PGAM1 Y119 phosphorylation PMC11183095
A549 cells 10 μM 48 h Inhibition of FGF receptor (FGFR) signaling, blocking FGF-induced PGAM1 Y119 phosphorylation PMC11183095
H3122 LR3 cells 1 μM 72 h Evaluate the effect of Zoligratinib combined with ceritinib on H3122 LR3 cells, showing that the combination effectively inhibited cell growth. PMC9633314

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice H3122 LR3 xenograft model Oral 50 mg/kg Once daily for 6 days Evaluate the effect of Zoligratinib combined with alectinib on H3122 LR3 xenograft tumors, showing that the combination significantly inhibited tumor growth. PMC9633314

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT03834220 Solid Tumor PHASE2 TERMINATED 2022-01-04 Ironwood Cancer & Research Cen... More >>ters - Scottsdale, Scottsdale, Arizona, 85260, United States|University of Arizona Cancer Center, Tucson, Arizona, 85721, United States|Moores UCSD Cancer Center, La Jolla, California, 92093, United States|University of California San Francisco, San Francisco, California, 94115, United States|Sarcoma Oncology Center, Santa Monica, California, 90403, United States|H. Lee Moffitt Cancer Center and Research Institute, Inc, Tampa, Florida, 33612, United States|James Graham Brown Cancer Center, Louisville, Kentucky, 10202, United States|Tulane University Cancer Center, New Orleans, Louisiana, 70122, United States|The John Hopkins Hospital, Baltimore, Maryland, 21231, United States|Massachusetts General Hospital, Boston, Massachusetts, 02114, United States|Dana-Farber Cancer Institute, Boston, Massachusetts, 02215, United States|University of Michigan, Ann Arbor, Michigan, 48109, United States|Memorial Sloan Kettering Cancer Center, Middletown, New Jersey, 07748, United States|Rutgers Cancer Institute of New Jersey, New Brunswick, New Jersey, 08901, United States|Memorial Sloan Kettering Cancer Center, Harrison, New York, 10604, United States|Memorial Sloan-Kettering Hospital, New York, New York, 10065, United States|University of North Carolina at Chapel Hill, Chapel Hill, North Carolina, 27599, United States|UC Health, LLC., Cincinnati, Ohio, 45229, United States|The Ohio State University Wexner Medical Center - James Cancer Hospital, Columbus, Ohio, 43210, United States|CTCA Cancer Treatment Centers, Tulsa, Oklahoma, 74133, United States|West Penn - Allegheny Oncology Network, Pittsburgh, Pennsylvania, 15224, United States|MD Anderson Cancer Center, Houston, Texas, 77030, United States|University of Utah Hospitals & Clinics, Salt Lake City, Utah, 84108, United States|Fred Hutchinson/Seattle Care Alliance, Seattle, Washington, 98109, United States|University of Wisconsin, Madison, Wisconsin, 53706, United States|Southern Highlands Private Hospital, Bowral, NSW 2576, Australia|Peninsula and Southeast Oncology (PASO), Frankston, 3199, Australia|Linear Clinical Research, B Block Sir Charles Gairdner Hospital, Nedlands, 6009, Australia|John Flynn Private Hospital, Tugun, 4224, Australia|LKH - Universit?tsklinikum der PMU Salzburg, Salzburg, 5020, Austria|Landesklinikum Wiener Neustadt, Wiener Neustadt, 2700, Austria|Hospital de Caridade de Ijuí, Avenida David J Martins, Ijuí, 98700-000, Brazil|Hospital de Clínicas de Porto Alegre, Rio Grande, 90035-903, Brazil|CEPHO - Centro de Estudos e Pesquisas de Hematologia e Oncologia, Santo André, 09060-870, Brazil|ICESP - Instituto do Cancer do Estado de S?o Paulo Octavio Frias de Oliveira, Avenida Doutor Arnaldo, S?o Paulo, 01246-000, Brazil|MHAT - Dobrich, Dobrich, 9300, Bulgaria|Complex Oncological Center - Plovdiv, EOOD, Plovdiv, 4004, Bulgaria|MHAT "Serdika", EOOD, Sofia, 1632, Bulgaria|General Hospital Varazdin, Vara?din, 42000, Croatia|University Hospital Centre, Sestre Milosrdnice, Zagreb, 10000, Croatia|Fakultni nemocnice u sv. Anny v Brne, Brno, 656 91, Czechia|Fakultni nemocnice Hradec Kralove, Hradec Králové, 50005, Czechia|Fakultni nemocnice Olomouc, Olomouc, 775 20, Czechia|Thomayerova nemocnice, Prague, 14000, Czechia|Fakultni nemocnice Kralovske Vinohrady, Praha, 100 34, Czechia|?lborg Universitets Hospital, Aalborg, 9100, Denmark|Herlev Hospital, Herlev, 2730, Denmark|Odense Universitetshospital, Odense, 5000, Denmark|Docrates Sy?p?sairaala, Helsinki, 00180, Finland|Helsinki University Hospital, Helsinki, 00290, Finland|ICO - Site Paul Papin, Angers, 49055, France|CHU Bordeaux - H?pital Saint André, Groupe Hospitalier Sud - H?pital Haut-Lévêque, Bordeaux, 33075, France|Centre Oscar Lambret, Lille, 59020, France|Groupe Hospitalier Sud - H?pital Haut Lévêque, Pessac, 33604, France|ICO - Site René Gauducheau, Saint-Herblain, 44805, France|Institut Gustave Roussy, Villejuif, 94805, France|General Hospital of Athens Laiko, Athens, 11527, Greece|General Hospital of Athens of Chest Diseases "SOTIRIA", Athens, 11527, Greece|General Hospital of Athens "Alexandra", Athens, 11528, Greece|University General Hospital of Ioannina, Ioánnina, 45500, Greece|Seoul National University Bundang Hospital, Department of Oncology Medical office, Gyeonggi-do, 13605, Korea, Republic of|The Catholic University of Korea, St. Vincent's Hospital, CRC Room, 3F, Gyeonggi-do, Korea, Republic of|Gachon University Gil Medical Center, CRC Room, 18F, Artificial intelligence hospital, Incheon, 21565, Korea, Republic of|Korea University Anam Hospital, Seoul, 02841, Korea, Republic of|Seoul National University Hospital (SNUH), Seoul, 03080, Korea, Republic of|Ajou University Hospital, CRC room, Clinical Trial Center, Suwon, 16499, Korea, Republic of|VU Medisch Centrum, Amsterdam, 1081 HV, Netherlands|Haga Ziekenhuis, Den Haag, 2545 AA, Netherlands|Akershus University Hospital, L?renskog, 1478, Norway|Radiumhospitalet, Montebello, Oslo, 0310, Norway|Cebu Doctors' University Hospital (CDUH), Research Office, Cebu City, 6000, Philippines|Philippine General Hospital, Clinical Trial Unit Room 5, Medical Research Laboratory, Ermita, 1000, Philippines|St. Luke's Medical Center, Human Cancer Biobank Research Center, Quezon City, 1112, Philippines|Szpital Kliniczny im.Heliodora Swiecickiego Uniwersytetu Medycznego im.K. Marcinkowskiego w Poznaniu, Poznań, 60-355, Poland|MTZ Clinical Research, Warszawa, 02-106, Poland|Centrum Onkologii-Instytut im.M.Sklodowskiej Curie, Warszawa, 02-781, Poland|S.C Delta Health Care S.R.L, Bucuresti, 014142, Romania|S.C Medisprof S.R.L., Cluj-Napoca, 400641, Romania|S.C Centrul de Oncologie Sf. Nectarie S.R.L., Craiova, 200347, Romania|S.C Oncocenter Oncologie Clinica S.R.L., Timi?oara, 300166, Romania|SBIH of Arkhangelsk region "Arkhangelsk Clinical Oncological Dispensary", Arkhangel'sk, 163045, Russian Federation|TSBHI "Altai Territorial oncological dispensary", Barnaul, 656049, Russian Federation|LLC Evimed, Chelyabinsk, 454048, Russian Federation|FSBSI "Russian Oncological Scientific Center n.a. N.N. Blokhin", Moscow, 115478, Russian Federation|BHI of Omsk region "Clinical Oncology Dispensary", Omsk, 644013, Russian Federation|Tomsk Research Instutite of Oncology, Tomsk, 634028, Russian Federation|Singapore National Cancer Center (SNCC), Singapore, 169610, Singapore|Tan Tock Seng Hospital, Communicable Disease Centre, Singapore, 308440, Singapore|Hospital Universitari Vall d'Hebron, Barcelona, 08035, Spain|Centro Integral Oncologico Clara Campal, Madrid, 28050, Spain|Hospital Clinico Universitario de Valencia, Valencia, 46010, Spain|Shuang Ho Hospital, New Taipei City, 23561, Taiwan|Taichung Veterans General Hospital, The Radiation Oncology Department, Taichung, 40705, Taiwan|National Cheng Kung University Hospital, Tainan, 704, Taiwan|National Taiwan University Hospital, Taipei, 10048, Taiwan|Taipei Medical University Hospital (TMUH), Taipei, 11031, Taiwan|Taipei Veterans General Hospital, Medical Science & Technology Building, Taipei, 11217, Taiwan|Linkou Chang-Gung Memorial Hospital, Taoyuan, 33305, Taiwan|CI Dnipropetrovsk CMCH #4 of Dnipropetrovsk RC Dept of Chemotherapy SI Dnipropetrovsk MA of MOHU, Dnipro, 49102, Ukraine|SI V.T. Zaycev Institute of general & urgent surgery of National academy medical sciences of Ukraine, Department of purulent surgery, Kharkiv, 61018, Ukraine|Communal Non-profit Enterprise Regional Center of Oncology, Kharkiv, 61070, Ukraine|Ninewells Hospital, Dundee, DD1 9SY, United Kingdom|Guy's Hospital, London, SE1 9RY, United Kingdom|Hammersmith Hospital, London, W12 0HS, United Kingdom|The Christie, Manchester, M20 4BX, United Kingdom Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.81mL

0.56mL

0.28mL

14.03mL

2.81mL

1.40mL

28.06mL

5.61mL

2.81mL

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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