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。


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| 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 |
99% | |||||||||||||||||
| Narazaciclib |
++
FGFR1, IC50: 26 nM |
RET | 99%+ | ||||||||||||||||
| Lactate |
+++
FGFR1, IC50: 8 nM |
+++
FGFR3, IC50: 9 nM |
FLT3,c-Kit | 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 |
99% | ||||||||||||||
| 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 |
FLT3,c-Kit | 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 |
99% | ||||||||||||||
| 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 | ✔ | 99% | |||||||||||||||||
| 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。 | |||||||||||||||||||
| 靶点 |
|
| 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] |
| Concentration | Treated Time | Description | References | |
| A2780-CP20 cells | 1 µM | 48 and 72 hours | To evaluate the effect of AZD4547 on the proliferation of A2780-CP20 cells, results showed no significant effect on resistant cells | Cancer Cell Int. 2024 Jan 25;24(1):43. |
| Adult mouse primary cardiomyocytes | 5 μM | 1 hour | AZD-4547 pretreatment prevents HG-induced inflammatory responses, fibrotic protein induction, and cellular hypertrophy | Acta Pharm Sin B. 2024 Apr;14(4):1693-1710. |
| Rat primary cardiomyocytes | 5 μM | 1 hour | AZD-4547 pretreatment prevents HG-induced inflammatory responses, fibrotic protein induction, and cellular hypertrophy | Acta Pharm Sin B. 2024 Apr;14(4):1693-1710. |
| H9C2 cells | 5 μM | 1 hour | AZD-4547 pretreatment mimics FGFR1 knockdown in preventing HG-induced inflammatory responses, fibrotic protein induction, and cellular hypertrophy | Acta Pharm Sin B. 2024 Apr;14(4):1693-1710. |
| H520 cells | 1 μM | 24 h | To investigate the effect of AZD-4547 on autophagy in FGFR1-amplified NSCLC cells, results showed that AZD-4547 induced increased autophagic activity. | J Exp Clin Cancer Res. 2017 May 30;36(1):72. |
| H1581 cells | 1 μM | 24 h | To investigate the effect of AZD-4547 on autophagy in FGFR1-amplified NSCLC cells, results showed that AZD-4547 induced increased autophagic activity. | J Exp Clin Cancer Res. 2017 May 30;36(1):72. |
| OMM1.3 | 0–10 μM | 8 days | AZD4547 significantly suppressed FGF2-induced resistance of OMM1.3 cells to BET inhibitors. | EMBO Mol Med. 2019 Feb;11(2):e9081. |
| UM004 | 0–10 μM | 8 days | AZD4547 significantly suppressed FGF2-induced resistance of UM004 cells to BET inhibitors. | EMBO Mol Med. 2019 Feb;11(2):e9081. |
| UM001 | 0–10 μM | 8 days | AZD4547 significantly suppressed FGF2-induced resistance of UM001 cells to BET inhibitors. | EMBO Mol Med. 2019 Feb;11(2):e9081. |
| JNA fibroblasts | 0 to 25 µg/mL | 72 h | AZD4547 inhibited JNA fibroblast proliferation, migration, and invasion through inhibition of FGFR and downstream signaling. | Int Forum Allergy Rhinol. 2017 Oct;7(10):973-979. |
| L929 | 0.1 μM | 24 h | AZD4547 at 0.1 μM effectively blocked TZ-induced necroptosis in L929 cells, demonstrating its inhibition in TLR3 and TLR4-mediated necroptosis. | Acta Pharmacol Sin. 2023 Apr;44(4):801-810. |
| HT29 | 0.019 μM | 24 h | AZD4547 at 0.019 μM significantly reduced TSZ-induced cell death in HT29 cells, demonstrating its dose-dependent necroptosis inhibition. | Acta Pharmacol Sin. 2023 Apr;44(4):801-810. |
| TOV-21G | 0.5 μM | 24 h | AZD4547 at 0.5 μM effectively blocked TSZ-induced cell necrosis, demonstrating its potential as a necroptosis inhibitor. | Acta Pharmacol Sin. 2023 Apr;44(4):801-810. |
| KatoIII cells | 100 nM | 14 days | To identify kinases that modulate cellular sensitivity to FGFR2 inhibition and validate the roles of ILK and CSK in regulating cell sensitivity to AZD4547. | Oncogenesis. 2019 May 10;8(5):33. |
| human hepatic stellate cells (HSCs) | 10 pg/mL | 24 h | To evaluate the expression of proliferation, fibrosis, and angiogenesis markers in HSCs after rhFGF1 treatment. Results showed that rhFGF1 treatment increased the mRNA expression of these markers compared to untreated cells. | Hepatol Commun. 2022 Jul;6(7):1574-1588. |
| human cholangiocyte cell line (H69) | 10 pg/mL | 24 h | To evaluate the expression of proliferation, fibrosis, senescence, and angiogenesis markers in H69 cells after rhFGF1 treatment. Results showed that rhFGF1 treatment increased the mRNA expression of these markers compared to untreated cells. | Hepatol Commun. 2022 Jul;6(7):1574-1588. |
| Administration | Dosage | Frequency | Description | References | ||
| BALB/c nude mice | Intraperitoneal xenograft model | Oral | 25 mg/kg | Once daily until the end of the experiment | To evaluate the anti-tumor effect of AZD4547 in the resistant A2780-CP20 cell xenograft model, results showed no significant effect on the resistant model | Cancer Cell Int. 2024 Jan 25;24(1):43. |
| Mice | STZ-induced type 1 diabetic mice | Oral | 5 mg/kg | Every other day for 20 weeks | AZD-4547 treatment prevents diabetes-induced cardiac inflammation, fibrosis, and dysfunction | Acta Pharm Sin B. 2024 Apr;14(4):1693-1710. |
| Nude mice | UM001 xenograft model | Oral gavage | 5 mg/kg | Once daily for 23 days | AZD4547 alone had a moderate effect on reducing UM001 tumor volume, but the combination of PLX51107 and AZD4547 significantly suppressed tumor growth. | EMBO Mol Med. 2019 Feb;11(2):e9081. |
| Mice | TNF-induced systemic inflammatory response syndrome (SIRS) model | Oral | 5 and 10 mg/kg | 1 hour before administration, continuous observation | AZD4547 at 5 and 10 mg/kg significantly reduced TNF-induced hypothermia and death, demonstrating its protective effects in the SIRS model. | Acta Pharmacol Sin. 2023 Apr;44(4):801-810. |
| Nude mice | U87MG xenograft model | Intraperitoneal injection | 30 mg/kg | Once daily for two weeks | AZD4547 was less effective than CYY292 in inhibiting U87MG tumor growth and caused weight loss in nude mice. | Genes Dis. 2023 Apr 3;11(1):479-494 |
| Mice | Osteosarcoma lung metastasis model | Oral | 12.5 mg/kg | Daily for 14 days | To study the effects of AZD4547 on osteosarcoma lung metastasis, results showed that AZD4547 significantly reduced the number and size of metastatic lung nodules | Oncogene. 2016 Jun 2;35(22):2852-61 |
| Nude mice | MCF-7 xenograft model | Oral | 12.5 mg/kg | Once daily for six weeks | To evaluate the inhibitory effect of AZD4547 in combination with AZD5363 on tumor growth in MCF-7 xenograft models. The results showed that AZD4547 alone did not significantly inhibit tumor growth, but its anti-tumor effect was slightly enhanced when combined with AZD5363. | Breast Cancer Res. 2013;15(4):R55 |
| Mice | Bile duct–ligated (BDL) mice and multidrug resistance 2 knockout (Mdr2−/−) mice | Intraperitoneal injection | 100 ng/kg | Once daily for 7 days | To evaluate the effect of AZD4547 on hepatic fibrosis, biliary proliferation, and inflammation in BDL and Mdr2?/? mice. Results showed that AZD4547 treatment significantly reduced hepatic fibrosis, biliary proliferation, and inflammation. | Hepatol Commun. 2022 Jul;6(7):1574-1588. |
| Dose | Mice: 1.5 mg/kg - 50 mg/kg[1] (p.o.) |
| Administration | p.o. |
| 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 << |
| 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 |
|
| CAS号 | 1035270-39-3 |
| 分子式 | C26H33N5O3 |
| 分子量 | 463.57 |
| SMILES Code | O=C(NC1=NNC(CCC2=CC(OC)=CC(OC)=C2)=C1)C3=CC=C(N4C[C@@H](C)N[C@@H](C)C4)C=C3 |
| MDL No. | MFCD22580423 |
| 别名 | |
| 运输 | 蓝冰 |
| InChI Key | VRQMAABPASPXMW-HDICACEKSA-N |
| Pubchem ID | 51039095 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Keep in dark place, sealed in dry, store in freezer, under -20°C |
| 溶解方案 |
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 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
|
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