AZD-4547 | FGFR | AmBeed-信号通路专用抑制剂

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AZD-4547 98%

货号：A868383

AZD-4547（Fexagratinib ; ADSK091) 是一种有效的FGFR家族抑制剂，对FGFR1、FGFR2、FGFR3和FGFR4的IC50值分别为0.2 nM、2.5 nM、1.8 nM和165 nM。

AZD-4547 化学结构
CAS号：1035270-39-3

AZD-4547 3D分子结构
CAS号：1035270-39-3

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AZD-4547 纯度/质量文件产品仅供科研

货号：A868383 标准纯度： 98% 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Cell,2024. Ambeed. [ A125712 ]; • Cancer Discov., 2024. Ambeed. [ A285925 ]; • JMC, 2024, 67(17): 14974-14985. Ambeed. [ A288696 ]; • JMC, 2024, 67(17): 15061-15079. Ambeed. [ A524399 , A633512 , A144280 , A174613 ]; • EJNMMI Radiopharm. Chem., 2024, 9, 61. Ambeed. [ A1257961 , A622068 ]; 更多 >

FGFR 亚型比较

产品名称	FGFR ↓ ↑	FGFR1 ↓ ↑	FGFR2 ↓ ↑	FGFR3 ↓ ↑	FGFR4 ↓ ↑	其他靶点	纯度
Tyrphostin AG1296	+ FGFR (Swiss 3T3), IC50: 12.3 μM					PDGFR	99%+
Pazopanib	+ FGFR, IC50: 140 nM						99%
Erdafitinib	✔					RET	99%+
Gambogenic acid	✔						98+%
Sulfatinib		+++ FGFR1, IC50: 15 nM					99+%
Nintedanib esylate		+ FGFR1, IC50: 69 nM	++ FGFR2, IC50: 37 nM	+ FGFR3, IC50: 108 nM			98%
Zoligratinib		+++ FGFR1, IC50: 9.3 nM	+++ FGFR2, IC50: 7.6 nM	++ FGFR3, IC50: 22 nM	+ FGFR4, IC50: 290 nM		99%+
MK-2461		+ FGFR1, IC50: 65 nM	++ FGFR2, IC50: 39 nM	++ FGFR3, IC50: 50 nM			98%+
SU 5402		++ FGFR1, IC50: 30 nM					98%
Brivanib		+ FGFR1, IC50: 148 nM					99%+
Lucitanib		++ FGFR1, IC50: 17.5 nM	+ FGFR2, IC50: 82.5 nM				99%+
Ponatinib		++++ FGFR1, IC50: 2.2 nM					98%
PD-166866		+ FGFR1, IC50: 52.4 nM					98%
Narazaciclib		++ FGFR1, IC50: 26 nM				RET	99%+
Lactate		+++ FGFR1, IC50: 8 nM		+++ FGFR3, IC50: 9 nM		c-Kit,FLT3	85%
Lenvatinib mesylate		++ FGFR1, IC50: 46 nM				c-RET	99%
LY2874455		++++ FGFR1, IC50: 2.8 nM	++++ FGFR2, IC50: 2.6 nM	+++ FGFR3, IC50: 6.4 nM	+++ FGFR4, IC50: 6 nM		99%+
FIIN-2		+++ FGFR1, IC50: 3.09 nM	+++ FGFR2, IC50: 4.3 nM	++ FGFR3, IC50: 27 nM	++ FGFR4, IC50: 45.3 nM		98%
FIIN-3		+++ FGFR1, IC50: 13.1 nM	++ FGFR2, IC50: 21 nM	++ FGFR3, IC50: 31.4 nM	++ FGFR4, IC50: 35.3 nM		98%
Infigratinib		++++ FGFR1, IC50: 0.9 nM	++++ FGFR2, IC50: 1.4 nM	++++ FGFR3, IC50: 1.0 nM FGFR3 (K650E), IC50: 4.9 nM	+ FGFR4, IC50: 60 nM		99%+
Danusertib		++ FGFR1, IC50: 47 nM				RET	99%+
R1530		++ FGFR1, IC50: 28 nM					98%
ENMD-2076		+ FGFR1, IC50: 92.7 nM	+ FGFR2, IC50: 70.8 nM			RET,FLT3	98%
Dovitinib		+++ FGFR1, IC50: 8 nM		+++ FGFR3, IC50: 9 nM		c-Kit,FLT3	99%+
Sorafenib		+ FGFR1, IC50: 580 nM					99%
SSR128129E		+ FGFR1, IC50: 1.9 μM					99%+
AZD-4547		++++ FGFR1, IC50: 0.2 nM	++++ FGFR2, IC50: 2.5 nM	++++ FGFR3, IC50: 1.8 nM			98%
Lenvatinib		++ FGFR1, IC50: 46 nM				RET	98%
PD173074		++ FGFR1, IC50: ~25 nM					99%+
S49076		++ FGFR1, IC50: 18 nM	+++ FGFR2, IC50: 17 nM	+++ FGFR3, IC50: 15 nM			98%
Futibatinib		++++ FGFR1, IC50: 1.8 nM	++++ FGFR2, IC50: 1.4 nM	++++ FGFR3, IC50: 1.6 nM	+++ FGFR4, IC50: 3.7 nM		99%+
Ferulic Acid		+ FGFR1, IC50: 3.78 μM	+ FGFR2, IC50: 12.5 μM				98%
Nintedanib		+ FGFR1, IC50: 69 nM	++ FGFR2, IC50: 37 nM	+ FGFR3, IC50: 108 nM	+ FGFR4, IC50: 610 nM		99+%
ASP5878		++++ FGFR1, IC50: 0.47 nM	++++ FGFR2, IC50: 0.6 nM	++++ FGFR3, IC50: 0.74 nM	+++ FGFR4, IC50: 3.5 nM		98%
PRN1371		++++ FGFR1, IC50: 0.6 nM	++++ FGFR2, IC50: 1.3 nM	+++ FGFR3, IC50: 4.1 nM	++ FGFR4, IC50: 19.3 nM		99%
Derazantinib		+++ FGFR1, IC50: 4.5 nM	++++ FGFR2, IC50: 1.8 nM	+++ FGFR3, IC50: 4.5 nM	++ FGFR4, IC50: 34 nM	RET	99%+
ODM-203		+++ FGFR1, IC50: 11 nM	+++ FGFR2, IC50: 16 nM	+++ FGFR3, IC50: 6 nM	++ FGFR4, IC50: 35 nM		99%+
Pemigatinib		++++ FGFR1, IC50: 0.4 nM	++++ FGFR2, IC50: 0.5 nM	++++ FGFR3, IC50: 1.2 nM	++ FGFR4, IC50: 30 nM		99%+
SKLB 610			✔			PDGFR	99%+
Alofanib			✔				99%+
Lirafugratinib			✔				98%
Masitinib mesylate				✔		FAK	99%+
BLU9931				+ FGFR3, IC50: 150 nM	+++ FGFR4, IC50: 3 nM		99%+
BO-264				✔			99%+
Fisogatinib					+++ FGFR4, IC50: 5 nM		99%+
H3B-6527					++++ FGFR4, IC50: <1.2 nM		99%+
Roblitinib					++++ FGFR4, IC50: 1.9 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

AZD-4547 生物活性

靶点	FGFR2 FGFR2, IC50:2.5 nM FGFR3 FGFR3, IC50:1.8 nM FGFR1 FGFR1, IC50:0.2 nM
描述	The FGFR (fibroblast growth factor receptor) family, comprising four members, FGFR1, FGFR2, FGFR3 and FGFR4, belongs to the RTKs which serve as high affinity receptors for FGFs controlling cell proliferation, migration, apoptosis and differentiation. AZD4547 is a highly potent inhibitor of FGFR1-3 with IC50 values of 0.2nM, 2.5nM, and 1.8nM and displays weaker activity against FGFR4 (IC50=165nM). AZD4547 has potent in vitro antiproliferative effects with IC50 values ranged from 18nM to 281nM, as well as inhibition on FGFR auto-phosphorylation downstream p-MAPK, p-FRS2 and p-PLCγ induced by FGF, on tumor cell lines with deregulated FGFR expression as KG1a expressing a truncated wild-type FGFR1 fusion protein, Sum52-PE cells expressing wild-type FGFR2 and KMS11 cells expressing translocated/Y373C mutated FGFR3 protein, but no effect on MCF7 cells with no identified defects in FGFR expression or signaling. Twice daily oral administration of AZD4547 at dose of 3mg/kg caused 53% tumor growth inhibition while doses of 12.5mg/kg once daily and 6.25 mg/kg twice daily resulted in complete tumor stasis in female SCID mice bearing KMS11 tumors. 12.5mg/kg once daily AZD4547 resulted in 65% tumor growth inhibition in KG1a model. The pharmacodynamic effect of AZD4547 can be shown by decreased p-FGFR3 in mice, within 15 minutes of drug administration^[1].
作用机制	AZD4547 competes with ATP for binding to FGF receptors 1, 2 and 3, thus inhibiting autophosphorylation and downstream signaling.^[2]

AZD-4547 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
4T1		Growth Inhibition Assay		IC50=0.64±0.11 μM	24642893
4T1	1.25-20 μM	Apoptosis Assay	24 h	induces apoptosis dose dependently	24642893
A549	0.1/1 μM	Cell viability Assay	48 h	enhances Erlotinib induced viability loss	26053020
AN3-CA FGFR2 N550K, K310R		Growth Inhibition Assay		GI50=0.031 ± 0.023 μM	26294741

AZD-4547 动物研究

Dose	Mice: 1.5 mg/kg - 50 mg/kg^[1] (p.o.)
Administration	p.o.

AZD-4547 临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02299999	Metastatic Breast Cancer	Phase 2	Recruiting	December 2022	France ... 展开 >> Institut de Cancérologie de l'Ouest/Paul Papin Recruiting Angers, France Contact: Mario CAMPONE, MD mario.campone@ico.unicancer.fr Principal Investigator: Mario CAMPONE, MD Institut Sainte-Catherine Recruiting Avignon, France Contact: Alice Mege, MD a.mege@isc84.org Principal Investigator: Alice Mege, MD Polyclinique Bordeaux Nord Aquitaine Recruiting Bordeaux, France, 33077 Contact: Nadine DOHOLLOU, MD n.dohollou@bordeauxnord.com Contact: Nadine DOHOLLOU, MD Institut Bergonié Recruiting Bordeaux, France Contact: Hervé Bonnefoi, MD h.bonnefoi@bordeaux.unicancer.fr Principal Investigator: Hervé Bonnefoi, MD Centre François Baclesse Recruiting Caen, France Contact: Christelle Lévy, MD c.levy@baclesse.unicancer.fr Principal Investigator: Christelle Lévy, MD Centre Jean Perrin Recruiting Clermont-Ferrand, France Contact: Marie-Ange Mouret Reynier, MD marie-ange.mouret-reynier@cjp.fr Principal Investigator: Marie-Ange Mouret Reynier, MD Ch Alpes Leman Not yet recruiting Contamine Sur Arve, France, 74130 Contact: Carol ALLIOT, MD calliot@ch-alpes-leman.fr Contact: Carol ALLIOT, MD Centre Georges François Leclerc Recruiting Dijon, France, 21079 Contact: Nicolas Isambert, MD nisambert@cgfl.fr Principal Investigator: Nicolas Isambert, MD Chd Vendee Recruiting La Roche-sur-Yon, France, 85925 Contact: Tifenn L'Haridon, MD tifenn.lharidon@chd-vendee.fr Contact: Tifenn L'Haridon, MD Centre Oscar Lambret Recruiting Lille, France Contact: Nuria KOTECKI, MD Principal Investigator: Nuria KOTECKI, MD Chu Dupuytren Not yet recruiting Limoges, France, 87000 Contact: Laurence VENAT-BOUVET, MD laurence.venat-bouvet@chu-limoges.fr Contact: Laurence VENAT-BOUVET, MD Hopital Privé Jean Mermoz Not yet recruiting Lyon, France, 69008 Contact: Olfa DERBEL, MD o.derbelmermoz@gmail.com Contact: Olfa DERBEL, MD Centre Hospitalier Lyon Sud Recruiting Lyon, France Contact: Benoit You, MD Principal Investigator: Benoit You, MD Centre Léon Bérard Recruiting Lyon, France Contact: Thomas Bachelot, MD thomas.bachelot@lyon.unicancer.fr Principal Investigator: Thomas Bachelot, MD Institut Paoli Calmettes Recruiting Marseille, France Contact: Anthony Gonçalves, MD goncalvesa@ipc.unicancer.fr Principal Investigator: Anthony Gonçalves, MD Institut Régional du Cancer Montpellier Val d'Aurelle Recruiting Montpellier, France Contact: William Jacot, MD william.jacot@icm.unicancer.fr Principal Investigator: William Jacot, MD Centre Alexis Vautrin Recruiting Nancy, France Contact: Elisabeth Luporsi, MD e.luporsi@nancy.unicancer.fr Principal Investigator: Elisabeth Luporsi, MD Institut de Cancérologie de l'Ouest/ René Gauducheau Recruiting Nantes, France Contact: Mario Campone, MD mario.campone@ico.unicancer.fr Principal Investigator: Mario Campone, MD Centre Antoine Lacassagne Recruiting Nice, France Contact: Jean-Marc Ferrero, MD jean-marc.ferrero@nice.unicancer.fr Principal Investigator: Jean-Marc Ferrero, MD Institut Curie Recruiting Paris, France Contact: Marie-Paule Sablin, MD mariepaule.sablin@curie.fr Principal Investigator: Marie-Paule Sablin, MD Centre Eugène Marquis Recruiting Rennes, France Contact: Claudia Lefeuvre-Plesse, MD c.lefeuvre@rennes.unicancer.fr Principal Investigator: Claudia Lefeuvre-Plesse, MD Centre Henri Becquerel Recruiting Rouen, France Contact: Jean-Christophe Théry, MD Principal Investigator: Jean-Christophe Théry, MD Institut Curie Recruiting Saint-Cloud, France Contact: Florence COUSSY, MD florence.coussy@curie.fr Principal Investigator: Florence COUSSY, MD Hopitaux Universitaire de Strasbourg - Hopital Civil Recruiting Strasbourg, France Contact: Philippe BARTHELEMY, MD philippe.barthelemy@chru-strasbourg.fr Principal Investigator: Philippe BARTHELEMY, MD Hopitaux Du Leman Recruiting Thonon-les-Bains, France, 74200 Contact: Francesco DEL PIANO, MD f-delpiano@ch-hopitauxduleman.fr Contact: Francesco DEL PIANO, MD Institut Claudius Regaud Recruiting Toulouse, France Contact: Florence Dalenc, MD dalenc.florence@iuct-oncopole.fr Principal Investigator: Florence Dalenc, MD Gustave Roussy Recruiting Villejuif, France Contact: Monica Arnedos, MD Monica.ARNEDOS@gustaveroussy.fr Principal Investigator: Monica Arnedos, MD Sub-Investigator: Fabrice André, MD 收起 <<
NCT02664935	Non-Small Cell Lung Cancer ... 展开 >> Carcinoma, Squamous Cell Adenocarcinoma 收起 <<	Phase 2	Recruiting	September 2021	United Kingdom ... 展开 >> Belfast City Hospital, Belfast Health and Social Care Trust Recruiting Belfast, United Kingdom Contact: Paula Scullin Queen Elizabeth Hospital Birmingham, University Hospitals Birmingham NHS Foundation Trust Recruiting Birmingham, United Kingdom, B15 2GW Contact: Gary Middleton, MB BS MD FRCP Principal Investigator: Gary Middleton, MB BS MD FRCP Birmingham Heartlands Hospital, Heart of England NHS Foundation Trust Recruiting Birmingham, United Kingdom Addenbrooke's Hospital, Cambridge University Hospitals NHS Foundation Trust Recruiting Cambridge, United Kingdom, CB2 0QQ Contact: David Gilligan, BSc (Hons) MB BChir FRCP FRCR cctc@addenbrookes.nhs.uk Principal Investigator: David Gilligan, BSc (Hons) MB BChir FRCP FRCR Velindre Cancer Centre, Velindre NHS Trust Recruiting Cardiff, United Kingdom, CF14 2TL Contact: Alison Brewster, BSC MB BCh FRCR MD 029 2061 5888 Principal Investigator: Alison Brewster, BSC MB BCh FRCR MD Edinburgh Cancer Centre, Western General Hospital Recruiting Edinburgh, United Kingdom, EH4 2XU Contact: Melanie Mackean, MB ChB MRCP MSc MD Principal Investigator: Melanie Mackean, MB ChB MRCP MSc MD Royal Devon and Exeter Hospital Recruiting Exeter, United Kingdom Contact: Elizabeth Toy Principal Investigator: Elizabeth Toy Cancer Research UK Clinical Trials Unit, Beatson West of Scotland Cancer Centre Recruiting Glasgow, United Kingdom, G12 0YN Contact: Noelle O'Rourke, BA MB MCh MA MCRP MD FRCR CCST Principal Investigator: Noelle O'Rourke, BA MB MCh MA MCRP MD FRCR CCST St. James' University Hospital, Leeds Teaching Hospital NHS Trust Recruiting Leeds, United Kingdom, LS9 7TF Contact: Clive Mulatero, BA MB BCh MA PhD FRCP Principal Investigator: Clive Mulatero, BA MB BCh MA PhD FRCP Leicester Royal Infirmary, University Hospitals of Leicester NHS Trust Recruiting Leicester, United Kingdom Contact: Dean Fennell Royal Marsden Hospital, The Royal Marsden NHS Foundation Trust Recruiting London, United Kingdom, SW3 6JJ Contact: Sanjay Popat Principal Investigator: Sanjay Popat, BSc MB BS MRCP PhD FRCP Charing Cross Hospital, Imperial College Healthcare NHS Trust Recruiting London, United Kingdom Contact: Conrad Lewanski Guy's Hospital, Guy's and St Thomas' NHS Foundation Trust Recruiting London, United Kingdom Contact: James Spicer St Bartholomew's Hospital, Barts Health NHS Trust Recruiting London, United Kingdom Contact: John Conibear University College Hospital, University College London Hospitals NHS Foundation Trust Recruiting London, United Kingdom The Christie Hospital, The Christie NHS Foundation Trust Recruiting Manchester, United Kingdom Contact: Yvonne Summers Sir Bobby Robson Cancer Trial Research Centre, The Newcastle upon Tyne Hospitals Recruiting Newcastle, United Kingdom, NE7 7DN Contact: Alastair Greystoke Principal Investigator: Alastair Greystoke, BSc MBChB MRCP MSc PhD Churchill Hospital, Oxford University Hospitals NHS Foundation Trust Recruiting Oxford, United Kingdom Contact: Denis Talbot Weston Park Hospital, Sheffield Teaching Hospitals NHS Foundation Trust Recruiting Sheffield, United Kingdom Contact: Sarah Danson Southampton General Hospital, University Hospital Southampton NHS Foundation Trust Recruiting Southampton, United Kingdom, SO16 6YD Contact: Christian Ottensmeier clinicaltrials@uhs.nhs.uk Principal Investigator: Christian Ottensmeier 收起 <<
NCT02117167	Non-small Cell Lung Cancer Met... 展开 >>astatic 收起 <<	Phase 2	Recruiting	February 2022	France ... 展开 >> Centre Hospitalier Henri Duffau Recruiting Avignon, France Contact: Nicolas CLOAREC, MD nicolas.cloarec@ch-avignon.fr Principal Investigator: Nicolas CLOAREC, MD Centre Hospitalier Universitaire de Besancon - Hopital Jean Minjoz Recruiting Besancon, France Contact: Virginie WESTEEL, MD virginie.westeel@univ.fcomte.fr Principal Investigator: Virginie WESTEEL, MD Hôpital Avicenne Recruiting Bobigny, France Contact: Boris DUCHEMANN, MD boris.duchemann@aphp.fr Principal Investigator: Boris DUCHEMANN, MD Institut Bergonié Recruiting Bordeaux, France Contact: François Chomy, MD f.chomy@bordeaux.unicancer.fr Principal Investigator: François Chomy, MD Hôpital Ambroise Paré Recruiting Boulogne Billancourt, France Contact: Etienne GIROUX LEPRIEUR, MD etienne.giroux-leprieur@aphp.fr Principal Investigator: Etienne GIROUX LEPRIEUR, MD Hospices Civils de Lyon- Hôpital Louis Pradel Recruiting Bron, France Contact: Nicolas Girard, MD nicolas.girard@chu-lyon.fr Principal Investigator: Nicolas Girard, MD Centre François Baclesse Recruiting Caen, France Contact: Radj Gervais, MD r.gervais@baclesse.unicancer.fr Principal Investigator: Radj Gervais, MD CHU Caen Recruiting Caen, France Contact: Gérard Zalcman, MD zalcman-g@chu-caen.fr Principal Investigator: Gérard Zalcman, MD Chu de Caen - Hopital Cote de Nacre Recruiting Caen, France Contact: Jeannick MADELAINE, MD madelaine-j@chu-caen.fr Principal Investigator: Jeannick MADELAINE, MD Hôpital Louis Pasteur Recruiting Chartres, France Contact: Claire Lethrosne, MD clethrosne@ch-chartres.fr Principal Investigator: Claire Lethrosne, MD centre Jean Perrin Recruiting Clermont-Ferrand, France Contact: Xavier Durando, MD xavier.durando@cjp.fr Principal Investigator: Xavier Durando, MD CHU Clermont Ferrand - Hôpital Gabriel Montpied Recruiting Clermont-Ferrand, France Contact: Henri Janicot, MD hjanicot@chu-clermontferrand.fr Principal Investigator: Henri Janicot, MD Hopitaux Civils de Colmar Recruiting Colmar, France Contact: Lionel MOREAU, MD lionel.moreau@ch-colmar.fr Principal Investigator: Lionel MOREAU, MD Centre Hopsitalier Intercommunal de Créteil Recruiting Créteil, France Contact: Isabelle Monnet, MD isabelle.monnet@chicreteil.fr Principal Investigator: Isabelle Monnet, MD Centre Georges François Leclerc Recruiting Dijon, France Contact: Bruno Coudert, MD bcoudert@cgfl.fr Principal Investigator: Bruno Coudert, MD CHU Grenoble Recruiting Grenoble, France Contact: Denis Moro-Sibilot, MD Dmoro-Sibilot@chu-grenoble.fr Principal Investigator: Denis Moro-Sibilot, MD Chd Vendee Recruiting La Roche Sur Yon, France Contact: Tifenn L'HARIDON, MD Principal Investigator: Tifenn L'HARIDON, MD CH du Mans Recruiting Le Mans, France Contact: Olivier Molinier, MD omolinier@ch-lemans.fr Principal Investigator: Olivier Molinier, MD Centre Oscar Lambret Recruiting Lille, France Contact: Eric Dansin, MD e-dansin@o-lambret.fr Principal Investigator: Eric Dansin, MD CHRU de Lille Recruiting Lille, France Contact: Alexis Cortot, MD Alexis.CORTOT@CHRU-LILLE.FR Principal Investigator: Alexis Cortot, MD Centre Léon Bérard Recruiting Lyon, France Contact: Maurice Pérol, MD maurice.perol@lyon.unicancer.fr Principal Investigator: Maurice Pérol, MD Hôpital Nord Recruiting Marseille, France Contact: Fabrice Barlesi, MD fabrice.barlesi@ap-hm.fr Principal Investigator: Fabrice Barlési, MD Institut Paoli Calmettes Recruiting Marseille, France Contact: Anne MADROSZYK, MD madroszyka@ipc.unicancer.fr Principal Investigator: Anne MADROSZYK, MD Institut de cancérologie de l'Ouest Recruiting Nantes, France Contact: Jaafar Bennouna, MD jaafar.bennouna@ico.unicancer.fr Principal Investigator: Jaafar Bennouna, MD Centre Antoine Lacassagne Recruiting Nice, France Contact: Josiane OTTO, MD josiane.otto@nice.unicancer.fr Principal Investigator: Josiane OTTO, MD Chr Orleans Recruiting Orleans, France Contact: Hugues MOREL, MD hugues.morel@chr-orleans.fr Contact: , MD Principal Investigator: Hugues MOREL AH-HP Hôpital Saint Louis Recruiting Paris, France Contact: Damien Pouessel, MD damien.pouessel@sls.aphp.fr Principal Investigator: Damien Pouessel, MD AP-HP Hôpital Cochin Recruiting Paris, France Contact: Jeanne Chapron, MD jeanne.chapron@cch.aphp.fr Principal Investigator: Jeanne Chapron, MD AP-HP Hôpital Européen Georges Pompidou Withdrawn Paris, France AP-HP Hôpital Tenon Recruiting Paris, France Contact: Marie Wislez, MD marie.wislez@tnn.aphp.fr Principal Investigator: Marie Wislez, MD Institut Curie Recruiting Paris, France Contact: Catherine Daniel, MD catherine.daniel@curie.fr Principal Investigator: Catherine Daniel, MD Centre Hospitalier de Pau Recruiting PAU, France Contact: Aldo RENAULT, MD aldo.renault@ch-pau.fr Principal Investigator: Aldo RENAULT, MD Centre Hospitalier Lyon Sud Recruiting Pierre Bénite, France Contact: Jean-Pierre Souquet, MD pierre-jean.souquet@chu-lyon.fr Principal Investigator: Jean-Pierre Souquet, MD CHR Pontchailloux Withdrawn Rennes, France Chru Strasbourg - Nouvel Hopital Civil Recruiting Strasbourg, France Contact: Philippe BARTHELEMY, MD Principal Investigator: Philippe BARTHELEMY, MD CHI de Toulon - Hôpital Sainte-Musse Recruiting Toulon, France Contact: Xavier TCHIKNAVORIAN, MD Principal Investigator: Xavier TCHIKNAVORIAN, MD CHU Toulouse -Hôpital Larrey Recruiting Toulouse, France Contact: Julien Mazières, MD mazieres.j@chu-toulouse.fr Principal Investigator: Julien Mazières, MD Hôpital Bretonneau Recruiting Tours, France Contact: Eric Pichon, MD e.pichon@chu-tours.fr Principal Investigator: Eric Pichon, MD Gustave Roussy Recruiting Villejuif, France Contact: Benjamin Besse, MD Benjamin.BESSE@gustaveroussy.fr Principal Investigator: Benjamin Besse, MD Sub-Investigator: Jean-Charles Soria, MD 收起 <<

AZD-4547 参考文献

[1]Gavine PR, Mooney L, et al. AZD4547: an orally bioavailable, potent, and selective inhibitor of the fibroblast growth factor receptor tyrosine kinase family. Cancer Res. 2012 Apr 15;72(8):2045-56.

AZD-4547 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.16mL

0.43mL

0.22mL

10.79mL

2.16mL

1.08mL

21.57mL

4.31mL

2.16mL

AZD-4547 技术信息

CAS号	1035270-39-3
分子式	C₂₆H₃₃N₅O₃
分子量	463.572

别名
运输	蓝冰

存储条件

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 120 mg/mL(258.86 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

4% DMSO+30% PEG 300+5% Tween 80+water 5 mg/mL

临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT02299999	Metastatic Breast Cancer	Phase 2	Recruiting	December 2022	France ... 展开 >> Institut de Cancérologie de l'Ouest/Paul Papin Recruiting Angers, France Contact: Mario CAMPONE, MD mario.campone@ico.unicancer.fr Principal Investigator: Mario CAMPONE, MD Institut Sainte-Catherine Recruiting Avignon, France Contact: Alice Mege, MD a.mege@isc84.org Principal Investigator: Alice Mege, MD Polyclinique Bordeaux Nord Aquitaine Recruiting Bordeaux, France, 33077 Contact: Nadine DOHOLLOU, MD n.dohollou@bordeauxnord.com Contact: Nadine DOHOLLOU, MD Institut Bergonié Recruiting Bordeaux, France Contact: Hervé Bonnefoi, MD h.bonnefoi@bordeaux.unicancer.fr Principal Investigator: Hervé Bonnefoi, MD Centre François Baclesse Recruiting Caen, France Contact: Christelle Lévy, MD c.levy@baclesse.unicancer.fr Principal Investigator: Christelle Lévy, MD Centre Jean Perrin Recruiting Clermont-Ferrand, France Contact: Marie-Ange Mouret Reynier, MD marie-ange.mouret-reynier@cjp.fr Principal Investigator: Marie-Ange Mouret Reynier, MD Ch Alpes Leman Not yet recruiting Contamine Sur Arve, France, 74130 Contact: Carol ALLIOT, MD calliot@ch-alpes-leman.fr Contact: Carol ALLIOT, MD Centre Georges François Leclerc Recruiting Dijon, France, 21079 Contact: Nicolas Isambert, MD nisambert@cgfl.fr Principal Investigator: Nicolas Isambert, MD Chd Vendee Recruiting La Roche-sur-Yon, France, 85925 Contact: Tifenn L'Haridon, MD tifenn.lharidon@chd-vendee.fr Contact: Tifenn L'Haridon, MD Centre Oscar Lambret Recruiting Lille, France Contact: Nuria KOTECKI, MD Principal Investigator: Nuria KOTECKI, MD Chu Dupuytren Not yet recruiting Limoges, France, 87000 Contact: Laurence VENAT-BOUVET, MD laurence.venat-bouvet@chu-limoges.fr Contact: Laurence VENAT-BOUVET, MD Hopital Privé Jean Mermoz Not yet recruiting Lyon, France, 69008 Contact: Olfa DERBEL, MD o.derbelmermoz@gmail.com Contact: Olfa DERBEL, MD Centre Hospitalier Lyon Sud Recruiting Lyon, France Contact: Benoit You, MD Principal Investigator: Benoit You, MD Centre Léon Bérard Recruiting Lyon, France Contact: Thomas Bachelot, MD thomas.bachelot@lyon.unicancer.fr Principal Investigator: Thomas Bachelot, MD Institut Paoli Calmettes Recruiting Marseille, France Contact: Anthony Gonçalves, MD goncalvesa@ipc.unicancer.fr Principal Investigator: Anthony Gonçalves, MD Institut Régional du Cancer Montpellier Val d'Aurelle Recruiting Montpellier, France Contact: William Jacot, MD william.jacot@icm.unicancer.fr Principal Investigator: William Jacot, MD Centre Alexis Vautrin Recruiting Nancy, France Contact: Elisabeth Luporsi, MD e.luporsi@nancy.unicancer.fr Principal Investigator: Elisabeth Luporsi, MD Institut de Cancérologie de l'Ouest/ René Gauducheau Recruiting Nantes, France Contact: Mario Campone, MD mario.campone@ico.unicancer.fr Principal Investigator: Mario Campone, MD Centre Antoine Lacassagne Recruiting Nice, France Contact: Jean-Marc Ferrero, MD jean-marc.ferrero@nice.unicancer.fr Principal Investigator: Jean-Marc Ferrero, MD Institut Curie Recruiting Paris, France Contact: Marie-Paule Sablin, MD mariepaule.sablin@curie.fr Principal Investigator: Marie-Paule Sablin, MD Centre Eugène Marquis Recruiting Rennes, France Contact: Claudia Lefeuvre-Plesse, MD c.lefeuvre@rennes.unicancer.fr Principal Investigator: Claudia Lefeuvre-Plesse, MD Centre Henri Becquerel Recruiting Rouen, France Contact: Jean-Christophe Théry, MD Principal Investigator: Jean-Christophe Théry, MD Institut Curie Recruiting Saint-Cloud, France Contact: Florence COUSSY, MD florence.coussy@curie.fr Principal Investigator: Florence COUSSY, MD Hopitaux Universitaire de Strasbourg - Hopital Civil Recruiting Strasbourg, France Contact: Philippe BARTHELEMY, MD philippe.barthelemy@chru-strasbourg.fr Principal Investigator: Philippe BARTHELEMY, MD Hopitaux Du Leman Recruiting Thonon-les-Bains, France, 74200 Contact: Francesco DEL PIANO, MD f-delpiano@ch-hopitauxduleman.fr Contact: Francesco DEL PIANO, MD Institut Claudius Regaud Recruiting Toulouse, France Contact: Florence Dalenc, MD dalenc.florence@iuct-oncopole.fr Principal Investigator: Florence Dalenc, MD Gustave Roussy Recruiting Villejuif, France Contact: Monica Arnedos, MD Monica.ARNEDOS@gustaveroussy.fr Principal Investigator: Monica Arnedos, MD Sub-Investigator: Fabrice André, MD 收起 <<
NCT02664935	Non-Small Cell Lung Cancer ... 展开 >> Carcinoma, Squamous Cell Adenocarcinoma 收起 <<	Phase 2	Recruiting	September 2021	United Kingdom ... 展开 >> Belfast City Hospital, Belfast Health and Social Care Trust Recruiting Belfast, United Kingdom Contact: Paula Scullin Queen Elizabeth Hospital Birmingham, University Hospitals Birmingham NHS Foundation Trust Recruiting Birmingham, United Kingdom, B15 2GW Contact: Gary Middleton, MB BS MD FRCP Principal Investigator: Gary Middleton, MB BS MD FRCP Birmingham Heartlands Hospital, Heart of England NHS Foundation Trust Recruiting Birmingham, United Kingdom Addenbrooke's Hospital, Cambridge University Hospitals NHS Foundation Trust Recruiting Cambridge, United Kingdom, CB2 0QQ Contact: David Gilligan, BSc (Hons) MB BChir FRCP FRCR cctc@addenbrookes.nhs.uk Principal Investigator: David Gilligan, BSc (Hons) MB BChir FRCP FRCR Velindre Cancer Centre, Velindre NHS Trust Recruiting Cardiff, United Kingdom, CF14 2TL Contact: Alison Brewster, BSC MB BCh FRCR MD 029 2061 5888 Principal Investigator: Alison Brewster, BSC MB BCh FRCR MD Edinburgh Cancer Centre, Western General Hospital Recruiting Edinburgh, United Kingdom, EH4 2XU Contact: Melanie Mackean, MB ChB MRCP MSc MD Principal Investigator: Melanie Mackean, MB ChB MRCP MSc MD Royal Devon and Exeter Hospital Recruiting Exeter, United Kingdom Contact: Elizabeth Toy Principal Investigator: Elizabeth Toy Cancer Research UK Clinical Trials Unit, Beatson West of Scotland Cancer Centre Recruiting Glasgow, United Kingdom, G12 0YN Contact: Noelle O'Rourke, BA MB MCh MA MCRP MD FRCR CCST Principal Investigator: Noelle O'Rourke, BA MB MCh MA MCRP MD FRCR CCST St. James' University Hospital, Leeds Teaching Hospital NHS Trust Recruiting Leeds, United Kingdom, LS9 7TF Contact: Clive Mulatero, BA MB BCh MA PhD FRCP Principal Investigator: Clive Mulatero, BA MB BCh MA PhD FRCP Leicester Royal Infirmary, University Hospitals of Leicester NHS Trust Recruiting Leicester, United Kingdom Contact: Dean Fennell Royal Marsden Hospital, The Royal Marsden NHS Foundation Trust Recruiting London, United Kingdom, SW3 6JJ Contact: Sanjay Popat Principal Investigator: Sanjay Popat, BSc MB BS MRCP PhD FRCP Charing Cross Hospital, Imperial College Healthcare NHS Trust Recruiting London, United Kingdom Contact: Conrad Lewanski Guy's Hospital, Guy's and St Thomas' NHS Foundation Trust Recruiting London, United Kingdom Contact: James Spicer St Bartholomew's Hospital, Barts Health NHS Trust Recruiting London, United Kingdom Contact: John Conibear University College Hospital, University College London Hospitals NHS Foundation Trust Recruiting London, United Kingdom The Christie Hospital, The Christie NHS Foundation Trust Recruiting Manchester, United Kingdom Contact: Yvonne Summers Sir Bobby Robson Cancer Trial Research Centre, The Newcastle upon Tyne Hospitals Recruiting Newcastle, United Kingdom, NE7 7DN Contact: Alastair Greystoke Principal Investigator: Alastair Greystoke, BSc MBChB MRCP MSc PhD Churchill Hospital, Oxford University Hospitals NHS Foundation Trust Recruiting Oxford, United Kingdom Contact: Denis Talbot Weston Park Hospital, Sheffield Teaching Hospitals NHS Foundation Trust Recruiting Sheffield, United Kingdom Contact: Sarah Danson Southampton General Hospital, University Hospital Southampton NHS Foundation Trust Recruiting Southampton, United Kingdom, SO16 6YD Contact: Christian Ottensmeier clinicaltrials@uhs.nhs.uk Principal Investigator: Christian Ottensmeier 收起 <<
NCT02117167	Non-small Cell Lung Cancer Met... 展开 >>astatic 收起 <<	Phase 2	Recruiting	February 2022	France ... 展开 >> Centre Hospitalier Henri Duffau Recruiting Avignon, France Contact: Nicolas CLOAREC, MD nicolas.cloarec@ch-avignon.fr Principal Investigator: Nicolas CLOAREC, MD Centre Hospitalier Universitaire de Besancon - Hopital Jean Minjoz Recruiting Besancon, France Contact: Virginie WESTEEL, MD virginie.westeel@univ.fcomte.fr Principal Investigator: Virginie WESTEEL, MD Hôpital Avicenne Recruiting Bobigny, France Contact: Boris DUCHEMANN, MD boris.duchemann@aphp.fr Principal Investigator: Boris DUCHEMANN, MD Institut Bergonié Recruiting Bordeaux, France Contact: François Chomy, MD f.chomy@bordeaux.unicancer.fr Principal Investigator: François Chomy, MD Hôpital Ambroise Paré Recruiting Boulogne Billancourt, France Contact: Etienne GIROUX LEPRIEUR, MD etienne.giroux-leprieur@aphp.fr Principal Investigator: Etienne GIROUX LEPRIEUR, MD Hospices Civils de Lyon- Hôpital Louis Pradel Recruiting Bron, France Contact: Nicolas Girard, MD nicolas.girard@chu-lyon.fr Principal Investigator: Nicolas Girard, MD Centre François Baclesse Recruiting Caen, France Contact: Radj Gervais, MD r.gervais@baclesse.unicancer.fr Principal Investigator: Radj Gervais, MD CHU Caen Recruiting Caen, France Contact: Gérard Zalcman, MD zalcman-g@chu-caen.fr Principal Investigator: Gérard Zalcman, MD Chu de Caen - Hopital Cote de Nacre Recruiting Caen, France Contact: Jeannick MADELAINE, MD madelaine-j@chu-caen.fr Principal Investigator: Jeannick MADELAINE, MD Hôpital Louis Pasteur Recruiting Chartres, France Contact: Claire Lethrosne, MD clethrosne@ch-chartres.fr Principal Investigator: Claire Lethrosne, MD centre Jean Perrin Recruiting Clermont-Ferrand, France Contact: Xavier Durando, MD xavier.durando@cjp.fr Principal Investigator: Xavier Durando, MD CHU Clermont Ferrand - Hôpital Gabriel Montpied Recruiting Clermont-Ferrand, France Contact: Henri Janicot, MD hjanicot@chu-clermontferrand.fr Principal Investigator: Henri Janicot, MD Hopitaux Civils de Colmar Recruiting Colmar, France Contact: Lionel MOREAU, MD lionel.moreau@ch-colmar.fr Principal Investigator: Lionel MOREAU, MD Centre Hopsitalier Intercommunal de Créteil Recruiting Créteil, France Contact: Isabelle Monnet, MD isabelle.monnet@chicreteil.fr Principal Investigator: Isabelle Monnet, MD Centre Georges François Leclerc Recruiting Dijon, France Contact: Bruno Coudert, MD bcoudert@cgfl.fr Principal Investigator: Bruno Coudert, MD CHU Grenoble Recruiting Grenoble, France Contact: Denis Moro-Sibilot, MD Dmoro-Sibilot@chu-grenoble.fr Principal Investigator: Denis Moro-Sibilot, MD Chd Vendee Recruiting La Roche Sur Yon, France Contact: Tifenn L'HARIDON, MD Principal Investigator: Tifenn L'HARIDON, MD CH du Mans Recruiting Le Mans, France Contact: Olivier Molinier, MD omolinier@ch-lemans.fr Principal Investigator: Olivier Molinier, MD Centre Oscar Lambret Recruiting Lille, France Contact: Eric Dansin, MD e-dansin@o-lambret.fr Principal Investigator: Eric Dansin, MD CHRU de Lille Recruiting Lille, France Contact: Alexis Cortot, MD Alexis.CORTOT@CHRU-LILLE.FR Principal Investigator: Alexis Cortot, MD Centre Léon Bérard Recruiting Lyon, France Contact: Maurice Pérol, MD maurice.perol@lyon.unicancer.fr Principal Investigator: Maurice Pérol, MD Hôpital Nord Recruiting Marseille, France Contact: Fabrice Barlesi, MD fabrice.barlesi@ap-hm.fr Principal Investigator: Fabrice Barlési, MD Institut Paoli Calmettes Recruiting Marseille, France Contact: Anne MADROSZYK, MD madroszyka@ipc.unicancer.fr Principal Investigator: Anne MADROSZYK, MD Institut de cancérologie de l'Ouest Recruiting Nantes, France Contact: Jaafar Bennouna, MD jaafar.bennouna@ico.unicancer.fr Principal Investigator: Jaafar Bennouna, MD Centre Antoine Lacassagne Recruiting Nice, France Contact: Josiane OTTO, MD josiane.otto@nice.unicancer.fr Principal Investigator: Josiane OTTO, MD Chr Orleans Recruiting Orleans, France Contact: Hugues MOREL, MD hugues.morel@chr-orleans.fr Contact: , MD Principal Investigator: Hugues MOREL AH-HP Hôpital Saint Louis Recruiting Paris, France Contact: Damien Pouessel, MD damien.pouessel@sls.aphp.fr Principal Investigator: Damien Pouessel, MD AP-HP Hôpital Cochin Recruiting Paris, France Contact: Jeanne Chapron, MD jeanne.chapron@cch.aphp.fr Principal Investigator: Jeanne Chapron, MD AP-HP Hôpital Européen Georges Pompidou Withdrawn Paris, France AP-HP Hôpital Tenon Recruiting Paris, France Contact: Marie Wislez, MD marie.wislez@tnn.aphp.fr Principal Investigator: Marie Wislez, MD Institut Curie Recruiting Paris, France Contact: Catherine Daniel, MD catherine.daniel@curie.fr Principal Investigator: Catherine Daniel, MD Centre Hospitalier de Pau Recruiting PAU, France Contact: Aldo RENAULT, MD aldo.renault@ch-pau.fr Principal Investigator: Aldo RENAULT, MD Centre Hospitalier Lyon Sud Recruiting Pierre Bénite, France Contact: Jean-Pierre Souquet, MD pierre-jean.souquet@chu-lyon.fr Principal Investigator: Jean-Pierre Souquet, MD CHR Pontchailloux Withdrawn Rennes, France Chru Strasbourg - Nouvel Hopital Civil Recruiting Strasbourg, France Contact: Philippe BARTHELEMY, MD Principal Investigator: Philippe BARTHELEMY, MD CHI de Toulon - Hôpital Sainte-Musse Recruiting Toulon, France Contact: Xavier TCHIKNAVORIAN, MD Principal Investigator: Xavier TCHIKNAVORIAN, MD CHU Toulouse -Hôpital Larrey Recruiting Toulouse, France Contact: Julien Mazières, MD mazieres.j@chu-toulouse.fr Principal Investigator: Julien Mazières, MD Hôpital Bretonneau Recruiting Tours, France Contact: Eric Pichon, MD e.pichon@chu-tours.fr Principal Investigator: Eric Pichon, MD Gustave Roussy Recruiting Villejuif, France Contact: Benjamin Besse, MD Benjamin.BESSE@gustaveroussy.fr Principal Investigator: Benjamin Besse, MD Sub-Investigator: Jean-Charles Soria, MD 收起 <<
NCT02546661	Muscle Invasive Bladder Cancer	Phase 1	Recruiting	March 27, 2020	-
NCT01202591	FGFR Inhibition, Pharmacokinet... 展开 >>ics, Biomarkers ER+ Breast Cancer 收起 <<	Phase 1 Phase 2	Completed	-	Belgium ... 展开 >> Research Site Leuven, Belgium Research Site Namur, Belgium Czech Republic Research Site Brno, Czech Republic Research Site Praha 4, Czech Republic France Research Site Villejuif Cedex, France Germany Research Site Erlangen, Germany Research Site München, Germany Research Site Rostock, Germany Hungary Research Site Budapest, Hungary Research Site Kaposvár, Hungary Research Site Nyíregyháza, Hungary Research Site Szeged, Hungary Italy Research Site Genova, Italy Research Site Lido di Camaiore, Italy Research Site Roma, Italy Romania Research Site Cluj Napoca, Romania United Kingdom Research Site Dundee, United Kingdom Research Site London, United Kingdom Research Site Manchester, United Kingdom Research Site Oxford, United Kingdom Research Site Sutton, United Kingdom 收起 <<
NCT02154490	Recurrent Squamous Cell Lung C... 展开 >>arcinoma Stage IV Squamous Cell Lung Carcinoma AJCC v7 收起 <<	Phase 2 Phase 3	Recruiting	April 1, 2022	-
NCT02465060	Advanced Malignant Solid Neopl... 展开 >>asm Bladder Carcinoma Breast Carcinoma Cervical Carcinoma Colon Carcinoma Colorectal Carcinoma Endometrial Carcinoma Esophageal Carcinoma Gastric Carcinoma Glioma Head and Neck Carcinoma Kidney Carcinoma Liver and Intrahepatic Bile Duct Carcinoma Lung Carcinoma Lymphoma Malignant Uterine Neoplasm Melanoma Ovarian Carcinoma Pancreatic Carcinoma Plasma Cell Myeloma Prostate Carcinoma Rectal Carcinoma Recurrent Bladder Carcinoma Recurrent Breast Carcinoma Recurrent Cervical Carcinoma Recurrent Colon Carcinoma Recurrent Colorectal Carcinoma Recurrent Esophageal Carcinoma Recurrent Gastric Carcinoma Recurrent Glioma Recurrent Head and Neck Carcinoma Recurrent Liver Carcinoma Recurrent Lung Carcinoma Recurrent Lymphoma Recurrent Malignant Solid Neoplasm Recurrent Melanoma Recurrent Ovarian Carcinoma Recurrent Pancreatic Carcinoma Recurrent Plasma Cell Myeloma Recurrent Prostate Carcinoma Recurrent Rectal Carcinoma Recurrent Skin Carcinoma Recurrent Thyroid Gland Carcinoma Recurrent Uterine Corpus Carcinoma Refractory Lymphoma Refractory Malignant Solid Neoplasm Refractory Plasma Cell Myeloma Skin Carcinoma Thyroid Gland Carcinoma Uterine Corpus Cancer 收起 <<	Phase 2	Recruiting	-	-
NCT01202591	-		Completed	-	-
NCT01457846	Gastro-oesophageal Junction Ca... 展开 >>ncer Gastric Cancer 收起 <<	Phase 2	Terminated	-	-
NCT01457846	-		Terminated	-	-
NCT01795768	Gastric Cancer ... 展开 >> Oesophageal Cancer Breast Cancer Squamous Cell Carcinoma of the Lung 收起 <<	Phase 2	Unknown	September 2015	United Kingdom ... 展开 >> Royal Marsden NHS Foundation Trust Recruiting London and Surrey, Surrey, United Kingdom, SM2 5PT Contact: Angela Gillbanks +44(0)2086613156 angela.gillbanks@rmh.nhs.uk Principal Investigator: David Cunningham, MD FRCP Sub-Investigator: Nicholas Turner, MA MRCP PhD Sub-Investigator: Sanjay Popat, BSc MBBS MRCP PhD Sub-Investigator: Elizabeth Smyth, MB MRCP MSc 收起 <<
NCT00979134	Cancer Advanc... 展开 >>ed Solid Malignancies 收起 <<	Phase 1	Completed	-	-
NCT01791985	Breast Cancer	Phase 1 Phase 2	Active, not recruiting	June 2017	United Kingdom ... 展开 >> Queen's Hospital, Burton-on-Trent Burton-on-Trent, Staffs, United Kingdom, DE13 0RB Russells Hall Hospital, West C8 Admin Office, 2nd Floor Dudley, West Midlands, United Kingdom, DY1 2HQ Cambridge University Hospitals NHS Foundation Trust, Addenbrooke's Hospital, Breast Cancer Research Unit, PO Box 97, Hills Road, Cambridge, United Kingdom, CB2 0QQ Greater Glasgow Health Board, Beatson West of Scotland Cancer Centre, 1053 Great Western Road, Glasgow, United Kingdom, G12 0YN Imperial College Healthcare NHS Trust, Charing Cross Hospital,1st Floor, Department of Medical Oncology, Fulham Palace Road London, United Kingdom, W6 8RF The Christie NHS Foundation Trust, Wilmslow Road, Withington Manchester, United Kingdom, M20 4BX The Newcastle upon Tyne Hospitals NHS Foundation Trust, Sir Bobby Robson Cancer Trials Research Centre, Freeman Hospital, High Heaton Newcastle upon Tyne, United Kingdom, NE7 7DN Poole Hospital NHS Foundation Trust, Top Floor, Linac Office, Poole, United Kingdom, BH15 2JB 收起 <<
NCT01213160	Cancer Advanc... 展开 >>ed Solid Malignancies 收起 <<	Phase 1	Completed	-	Japan ... 展开 >> Research Site Chuo-ku, Japan Research Site Nagoya-shi, Japan Research Site Sapporo-shi, Japan 收起 <<
NCT01824901	Recurrent Non-small Cell Lung ... 展开 >>Cancer Squamous Cell Lung Cancer 收起 <<	Phase 1 Phase 2	Completed	-	United States, Georgia ... 展开 >> Emory University Atlanta, Georgia, United States, 30322 United States, Illinois Northwestern University Chicago, Illinois, United States, 60611 United States, Maryland Johns Hopkins University Baltimore, Maryland, United States, 21287-8936 United States, Massachusetts Eastern Cooperative Oncology Group (ECOG) Research Base Brookline, Massachusetts, United States, 02445-7648 United States, Texas University of Texas Southwestern Medical Center Dallas, Texas, United States, 75390 收起 <<
NCT02965378	FGFR1 Gene Amplification ... 展开 >> FGFR1 Gene Mutation FGFR2 Gene Amplification FGFR2 Gene Mutation FGFR3 Gene Amplification FGFR3 Gene Mutation Recurrent Squamous Cell Lung Carcinoma Stage IV Squamous Cell Lung Carcinoma AJCC v7 收起 <<	Phase 2 Phase 3	Active, not recruiting	April 1, 2022	-
NCT02824133	Recurrent IDHwt Gliomas With F... 展开 >>GFR3-TACC3 Fusion Recurrent IDHwt Gliomas With FGFR1-TACC1 Fusion 收起 <<	Phase 1 Phase 2	Suspended(Intermedary analysis... 展开 >> of 12 first patients' data results) 收起 <<	September 2018	France ... 展开 >> Neuro onsology unit - Groupe Hospitalier Pitié-Salpêtrière Paris, France, 75013 收起 <<
NCT01824901	-		Completed	-	-

4T1		Growth Inhibition Assay		IC50=0.64±0.11 μM	24642893
4T1	1.25-20 μM	Apoptosis Assay	24 h	induces apoptosis dose dependently	24642893
A549	0.1/1 μM	Cell viability Assay	48 h	enhances Erlotinib induced viability loss	26053020
AN3-CA FGFR2 N550K, K310R		Growth Inhibition Assay		GI50=0.031 ± 0.023 μM	26294741
BaF3 FLT3-TEL		Growth Inhibition Assay		GI50=4.6 ± 0.577 μM	26294741
BaF3 Parental		Growth Inhibition Assay		GI50﹥10 μM	26294741
BaF3 RET-TEL		Growth Inhibition Assay		GI50=0.39 ± 0.048 μM	26294741
CT26		Growth Inhibition Assay		IC50＞20 μM	24642893
HCT116		Growth Inhibition Assay		IC50=15.9±1.82 μM	24642893
HEC1A Normal FGFR2		Growth Inhibition Assay		GI50﹥10 μM	26294741
Hep3B		Growth Inhibition Assay	72 h	IC50=6.43 μM	26351320
HepG2		Growth Inhibition Assay	72 h	IC50=8.73 μM	26351320
HGC-27	1 nM-10 μM	Growth Inhibition Assay	72 h	IC50 of 5-10 μM, inhibits cell viability dose dependently	25576915
Hur7		Growth Inhibition Assay	72 h	IC50=7.25 μM	26351320
Ishikawa FGFF2 over exp.		Growth Inhibition Assay		GI50=4.5 ± 1.51 μM	26294741
KATOIII	1 nM-10 μM	Growth Inhibition Assay	72 h	IC50 of 10-100 nM, inhibits cell viability dose dependently	25576915
KG1a		Growth Inhibition Assay		IC50=0.018 μM	22369928
KMS11		Growth Inhibition Assay		IC50=0.281 μM	22369928
MCF7		Growth Inhibition Assay		IC50>30 μM	22369928
MDA-MB-231		Growth Inhibition Assay		IC50＞20 μM	24642893
MDA-MB-468		Growth Inhibition Assay		IC50=4.9±0.85 μM	24642893
MFE280 FGFR2 S252W		Growth Inhibition Assay		GI50=0.218 ± 0.073 μM	26294741
MFE296 FGFR2 N550K		Growth Inhibition Assay		GI50=0.730 ± 0.057 μM	26294741
MKN-28	1 nM-10 μM	Growth Inhibition Assay	72 h	IC50 of 5-10 μM, inhibits cell viability dose dependently	25576915
MOLM14 FLT3/ITD		Growth Inhibition Assay		GI50=0.484 ± 0.157 μM	26294741
MV4-11 FLT3/ITD		Growth Inhibition Assay		GI50=0.459 ± 0.046 μM	26294741
NCI-N87	1 nM-10 μM	Growth Inhibition Assay	72 h	IC50 of 5-10 μM, inhibits cell viability dose dependently	25576915
PLC/PRF5		Growth Inhibition Assay	72 h	IC50=6.55 μM	26351320
SGC-7901	1 nM-10 μM	Growth Inhibition Assay	72 h	IC50 of 5-10 μM, inhibits cell viability dose dependently	25576915
SK-HEP-1		Growth Inhibition Assay	72 h	IC50=0.084 μM	26351320
SK-HEP-1	1 µM	Clonogenic assay	24 h	decreases colony formation significantly	26351320
SK-HEP-1	0-2 μM	Function Assay	48 h	causes a decrease of FRS2，AKT, and ERK phosphorylation	26351320
SNU-16	1 nM-10 μM	Growth Inhibition Assay	72 h	IC50 of 10-100 nM, inhibits cell viability dose dependently	25576915
SNU449		Growth Inhibition Assay	72 h	IC50=0.082 μM	26351320
SNU449	1 µM	Clonogenic assay	24 h	decreases colony formation significantly	26351320
SNU449	0-2 μM	Function Assay	48 h	causes a decrease of FRS2，AKT, and ERK phosphorylation	26351320
SNU475		Growth Inhibition Assay	72 h	IC50=5.4 μM	26351320
Sum52-PE		Growth Inhibition Assay		IC50=0.041 μM	22369928
SW480		Growth Inhibition Assay		IC50＞20 μM	24642893
SW620		Growth Inhibition Assay		IC50＞20 μM	24642893
TT RET C634W		Growth Inhibition Assay		GI50=2.9 ± 0.904 μM	26294741

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FGFR2	FGFR2, IC50:2.5 nM
FGFR3	FGFR3, IC50:1.8 nM
FGFR1	FGFR1, IC50:0.2 nM

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