Structure of Zoligratinib
CAS No.: 1265229-25-1
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
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
4.5
*For Research Use Only !
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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 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302 |
Precautionary Statements: | P280-P305+P351+P338 |
Target |
|
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 << |
Tags: Zoligratinib | Debio 1347 | CH5183284 | Debio1347 | Debio-1347 | CH5183284 | CH 5183284 | CH-5183284 | FGFR | Fibroblast growth factor receptor | 1265229-25-1
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P230 | Keep wetted |
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P232 | Protect from moisture. |
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P234 | Keep only in original container. |
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P263 | Avoid contact during pregnancy/while nursing. |
P264 | Wash hands thoroughly after handling. |
P265 | Wash skin thouroughly after handling. |
P270 | Do not eat, drink or smoke when using this product. |
P271 | Use only outdoors or in a well-ventilated area. |
P272 | Contaminated work clothing should not be allowed out of the workplace. |
P273 | Avoid release to the environment. |
P280 | Wear protective gloves/protective clothing/eye protection/face protection. |
P281 | Use personal protective equipment as required. |
P282 | Wear cold insulating gloves/face shield/eye protection. |
P283 | Wear fire/flame resistant/retardant clothing. |
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P285 | In case of inadequate ventilation wear respiratory protection. |
P231 + P232 | Handle under inert gas. Protect from moisture. |
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Response | |
Code | Phrase |
P301 | IF SWALLOWED: |
P304 | IF INHALED: |
P305 | IF IN EYES: |
P306 | IF ON CLOTHING: |
P307 | IF exposed: |
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P338 | Remove contact lenses, if present and easy to do. Continue rinsing. |
P340 | Remove victim to fresh air and keep at rest in a position comfortable for breathing. |
P341 | If breathing is difficult, remove victim to fresh air and keep at rest in a position comfortable for breathing. |
P342 | If experiencing respiratory symptoms: |
P350 | Gently wash with plenty of soap and water. |
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P363 | Wash contaminated clothing before reuse. |
P370 | In case of fire: |
P371 | In case of major fire and large quantities: |
P372 | Explosion risk in case of fire. |
P373 | DO NOT fight fire when fire reaches explosives. |
P374 | Fight fire with normal precautions from a reasonable distance. |
P376 | Stop leak if safe to do so. Oxidising gases (section 2.4) 1 |
P377 | Leaking gas fire: Do not extinguish, unless leak can be stopped safely. |
P378 | |
P380 | Evacuate area. |
P381 | Eliminate all ignition sources if safe to do so. |
P390 | Absorb spillage to prevent material damage. |
P391 | Collect spillage. Hazardous to the aquatic environment |
P301 + P310 | IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician. |
P301 + P312 | IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell. |
P301 + P330 + P331 | IF SWALLOWED: Rinse mouth. Do NOT induce vomiting. |
P302 + P334 | IF ON SKIN: Immerse in cool water/wrap in wet bandages. |
P302 + P350 | IF ON SKIN: Gently wash with plenty of soap and water. |
P303 + P361 + P353 | IF ON SKIN (or hair): Remove/Take off Immediately all contaminated clothing. Rinse SKIN with water/shower. |
P304 + P312 | IF INHALED: Call a POISON CENTER or doctor/physician if you feel unwell. |
P304 + P340 | IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing. |
P304 + P341 | IF INHALED: If breathing is difficult, remove victim to fresh air and keep at rest in a position comfortable for breathing. |
P305 + P351 + P338 | IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing. |
P306 + P360 | IF ON CLOTHING: Rinse Immediately contaminated CLOTHING and SKIN with plenty of water before removing clothes. |
P307 + P311 | IF exposed: call a POISON CENTER or doctor/physician. |
P308 + P313 | IF exposed or concerned: Get medical advice/attention. |
P309 + P311 | IF exposed or if you feel unwell: call a POISON CENTER or doctor/physician. |
P332 + P313 | IF SKIN irritation occurs: Get medical advice/attention. |
P333 + P313 | IF SKIN irritation or rash occurs: Get medical advice/attention. |
P335 + P334 | Brush off loose particles from skin. Immerse in cool water/wrap in wet bandages. |
P337 + P313 | IF eye irritation persists: Get medical advice/attention. |
P342 + P311 | IF experiencing respiratory symptoms: call a POISON CENTER or doctor/physician. |
P370 + P376 | In case of fire: Stop leak if safe to Do so. |
P370 + P378 | In case of fire: |
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P370 + P380 + P375 | In case of fire: Evacuate area. Fight fire remotely due to the risk of explosion. |
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H201 | Explosive; mass explosion hazard |
H202 | Explosive; severe projection hazard |
H203 | Explosive; fire, blast or projection hazard |
H204 | Fire or projection hazard |
H205 | May mass explode in fire |
H220 | Extremely flammable gas |
H221 | Flammable gas |
H222 | Extremely flammable aerosol |
H223 | Flammable aerosol |
H224 | Extremely flammable liquid and vapour |
H225 | Highly flammable liquid and vapour |
H226 | Flammable liquid and vapour |
H227 | Combustible liquid |
H228 | Flammable solid |
H229 | Pressurized container: may burst if heated |
H230 | May react explosively even in the absence of air |
H231 | May react explosively even in the absence of air at elevated pressure and/or temperature |
H240 | Heating may cause an explosion |
H241 | Heating may cause a fire or explosion |
H242 | Heating may cause a fire |
H250 | Catches fire spontaneously if exposed to air |
H251 | Self-heating; may catch fire |
H252 | Self-heating in large quantities; may catch fire |
H260 | In contact with water releases flammable gases which may ignite spontaneously |
H261 | In contact with water releases flammable gas |
H270 | May cause or intensify fire; oxidizer |
H271 | May cause fire or explosion; strong oxidizer |
H272 | May intensify fire; oxidizer |
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H281 | Contains refrigerated gas; may cause cryogenic burns or injury |
H290 | May be corrosive to metals |
Health hazards | |
Code | Phrase |
H300 | Fatal if swallowed |
H301 | Toxic if swallowed |
H302 | Harmful if swallowed |
H303 | May be harmful if swallowed |
H304 | May be fatal if swallowed and enters airways |
H305 | May be harmful if swallowed and enters airways |
H310 | Fatal in contact with skin |
H311 | Toxic in contact with skin |
H312 | Harmful in contact with skin |
H313 | May be harmful in contact with skin |
H314 | Causes severe skin burns and eye damage |
H315 | Causes skin irritation |
H316 | Causes mild skin irritation |
H317 | May cause an allergic skin reaction |
H318 | Causes serious eye damage |
H319 | Causes serious eye irritation |
H320 | Causes eye irritation |
H330 | Fatal if inhaled |
H331 | Toxic if inhaled |
H332 | Harmful if inhaled |
H333 | May be harmful if inhaled |
H334 | May cause allergy or asthma symptoms or breathing difficulties if inhaled |
H335 | May cause respiratory irritation |
H336 | May cause drowsiness or dizziness |
H340 | May cause genetic defects |
H341 | Suspected of causing genetic defects |
H350 | May cause cancer |
H351 | Suspected of causing cancer |
H360 | May damage fertility or the unborn child |
H361 | Suspected of damaging fertility or the unborn child |
H361d | Suspected of damaging the unborn child |
H362 | May cause harm to breast-fed children |
H370 | Causes damage to organs |
H371 | May cause damage to organs |
H372 | Causes damage to organs through prolonged or repeated exposure |
H373 | May cause damage to organs through prolonged or repeated exposure |
Environmental hazards | |
Code | Phrase |
H400 | Very toxic to aquatic life |
H401 | Toxic to aquatic life |
H402 | Harmful to aquatic life |
H410 | Very toxic to aquatic life with long-lasting effects |
H411 | Toxic to aquatic life with long-lasting effects |
H412 | Harmful to aquatic life with long-lasting effects |
H413 | May cause long-lasting harmful effects to aquatic life |
H420 | Harms public health and the environment by destroying ozone in the upper atmosphere |
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