Clinical cancer research : an official journal of the American Association for Cancer Research, ISSN 1078-0432, 9/2017, Volume 23, Issue 18, pp. 5366 - 5373
Journal Article
Reproductive Sciences, ISSN 1933-7191, 7/2019, Volume 26, Issue 7, pp. 979 - 987
Several features exist that distinguish endometriotic cells from eutopic endometrial cells. Progesterone resistance is one of the main distinguishing features,...
AZD4547 | endometriosis | FGF | HAND2 | PROGESTERONE | MECHANISMS | PATHOPHYSIOLOGY | OBSTETRICS & GYNECOLOGY | WOMEN | INHIBITOR AZD4547 | REPRODUCTIVE BIOLOGY | GENES | STROMAL CELLS
AZD4547 | endometriosis | FGF | HAND2 | PROGESTERONE | MECHANISMS | PATHOPHYSIOLOGY | OBSTETRICS & GYNECOLOGY | WOMEN | INHIBITOR AZD4547 | REPRODUCTIVE BIOLOGY | GENES | STROMAL CELLS
Journal Article
Annals of Oncology, ISSN 0923-7534, 06/2017, Volume 28, Issue 6, pp. 1316 - 1324
Background: Approximately 5%-10% of gastric cancers have a fibroblast growth factor receptor-2 (FGFR2) gene amplification. AZD4547 is a selective FGFR-1, 2, 3...
AZD4547 | Fibroblast growth factor receptor | Gastric cancer | Clinical efficacy | Fluorescence in situ hybridization | gastric cancer | PHASE-III | CANCER | CHEMOTHERAPY | fluorescence in situ hybridization | TRIAL | SUPPORTIVE CARE | INHIBITOR AZD4547 | ONCOLOGY | fibroblast growth factor receptor | PHOSPHATE HOMEOSTASIS | IRINOTECAN | clinical efficacy | PLUS | Piperazines - administration & dosage | Stomach Neoplasms - genetics | Humans | Paclitaxel - adverse effects | Antineoplastic Agents - administration & dosage | Stomach Neoplasms - drug therapy | Adenocarcinoma - drug therapy | Piperazines - adverse effects | Disease-Free Survival | Benzamides - administration & dosage | Pyrazoles - administration & dosage | Gene Amplification | Antineoplastic Agents - adverse effects | Cell Line, Tumor | Adenocarcinoma - genetics | Paclitaxel - administration & dosage | Benzamides - adverse effects | Receptor, Fibroblast Growth Factor, Type 2 - genetics | Pyrazoles - adverse effects
AZD4547 | Fibroblast growth factor receptor | Gastric cancer | Clinical efficacy | Fluorescence in situ hybridization | gastric cancer | PHASE-III | CANCER | CHEMOTHERAPY | fluorescence in situ hybridization | TRIAL | SUPPORTIVE CARE | INHIBITOR AZD4547 | ONCOLOGY | fibroblast growth factor receptor | PHOSPHATE HOMEOSTASIS | IRINOTECAN | clinical efficacy | PLUS | Piperazines - administration & dosage | Stomach Neoplasms - genetics | Humans | Paclitaxel - adverse effects | Antineoplastic Agents - administration & dosage | Stomach Neoplasms - drug therapy | Adenocarcinoma - drug therapy | Piperazines - adverse effects | Disease-Free Survival | Benzamides - administration & dosage | Pyrazoles - administration & dosage | Gene Amplification | Antineoplastic Agents - adverse effects | Cell Line, Tumor | Adenocarcinoma - genetics | Paclitaxel - administration & dosage | Benzamides - adverse effects | Receptor, Fibroblast Growth Factor, Type 2 - genetics | Pyrazoles - adverse effects
Journal Article
4.
Full Text
Discovery of Potent Irreversible Pan-Fibroblast Growth Factor Receptor (FGFR) Inhibitors
Journal of Medicinal Chemistry, ISSN 0022-2623, 10/2018, Volume 61, Issue 20, pp. 9085 - 9104
Fibroblast growth factor receptors (FGFR1ā4) are promising therapeutic targets in many cancers. With the resurgence of interest in irreversible inhibitors,...
CH5183284/DEBIO 1347 | AZD4547 | SELECTIVE INHIBITOR | DESIGN | CHEMISTRY, MEDICINAL | COVALENT INHIBITORS | JNJ-42756493 | OVERCOME RESISTANCE | DERIVATIVES | EGFR | STRATEGIES
CH5183284/DEBIO 1347 | AZD4547 | SELECTIVE INHIBITOR | DESIGN | CHEMISTRY, MEDICINAL | COVALENT INHIBITORS | JNJ-42756493 | OVERCOME RESISTANCE | DERIVATIVES | EGFR | STRATEGIES
Journal Article
Clinical Cancer Research, ISSN 1078-0432, 04/2015, Volume 21, Issue 7, pp. 1514 - 1524
The Lung Master Protocol (Lung-MAP, S1400) is a ground-breaking clinical trial designed to advance the efficient development of targeted therapies for squamous...
AZD4547 | PALBOCICLIB | SELECTIVE INHIBITOR | POTENT | GENOMICS | BAR | ONCOLOGY | CLINICAL-TRIALS | ALECTINIB | TARGETS | Lung Neoplasms - genetics | Lung Neoplasms - drug therapy | Carcinoma, Squamous Cell - drug therapy | Carcinoma, Non-Small-Cell Lung - genetics | Carcinoma, Squamous Cell - genetics | Humans | Antineoplastic Agents - therapeutic use | Biomarkers, Tumor - genetics | Carcinoma, Non-Small-Cell Lung - drug therapy | Research Design | Precision Medicine - methods
AZD4547 | PALBOCICLIB | SELECTIVE INHIBITOR | POTENT | GENOMICS | BAR | ONCOLOGY | CLINICAL-TRIALS | ALECTINIB | TARGETS | Lung Neoplasms - genetics | Lung Neoplasms - drug therapy | Carcinoma, Squamous Cell - drug therapy | Carcinoma, Non-Small-Cell Lung - genetics | Carcinoma, Squamous Cell - genetics | Humans | Antineoplastic Agents - therapeutic use | Biomarkers, Tumor - genetics | Carcinoma, Non-Small-Cell Lung - drug therapy | Research Design | Precision Medicine - methods
Journal Article
ONCOGENESIS, ISSN 2157-9024, 07/2016, Volume 5, Issue 7, pp. e241 - e241
Aberrant fibroblast growth factor receptor (FGFR) activation/expression is a common feature in lung cancer (LC). In this study, we evaluated the antitumor...
AZD4547 | AMPLIFICATION | ONCOLOGY | SQUAMOUS-CELL CARCINOMA | SENSITIVITY | INHIBITOR | GEFITINIB RESISTANCE | EXPRESSION | RECEPTOR TYROSINE KINASE | Original
AZD4547 | AMPLIFICATION | ONCOLOGY | SQUAMOUS-CELL CARCINOMA | SENSITIVITY | INHIBITOR | GEFITINIB RESISTANCE | EXPRESSION | RECEPTOR TYROSINE KINASE | Original
Journal Article
MedChemComm, ISSN 2040-2503, 2017, Volume 8, Issue 8, pp. 1604 - 1613
A diverse range of selective FGFR4 inhibitor hit series were identified using unbiased screening approaches and by the modification of known kinase inhibitor...
MEDICINAL CHEMISTRY | AZD4547 | POTENT | CHEMISTRY, MEDICINAL | PATHWAY | TYROSINE KINASE | BIOCHEMISTRY & MOLECULAR BIOLOGY | FGFR4 INHIBITORS | THERAPIES | CANCER | DISCOVERY | FAMILY
MEDICINAL CHEMISTRY | AZD4547 | POTENT | CHEMISTRY, MEDICINAL | PATHWAY | TYROSINE KINASE | BIOCHEMISTRY & MOLECULAR BIOLOGY | FGFR4 INHIBITORS | THERAPIES | CANCER | DISCOVERY | FAMILY
Journal Article
International Journal of Biochemistry and Cell Biology, ISSN 1357-2725, 09/2018, Volume 102, pp. 128 - 137
Amplification of has been regarded as a druggable target in gastric cancer (GC). Despite known potential of AZD4547, a selective inhibitor of FGFR 1ā3, to...
Resistance | mTOR | FGFR inhibitor | Gastric cancer | EphB3 | SIGNALING PATHWAYS | ADENOCARCINOMA | BIOCHEMISTRY & MOLECULAR BIOLOGY | KINASE | CELL BIOLOGY | EPITHELIAL-MESENCHYMAL TRANSITION | CELL LUNG-CANCER | AZD4547 | GROWTH-FACTOR RECEPTOR | COLORECTAL-CANCER | GENE AMPLIFICATION | PROGNOSTIC-SIGNIFICANCE | Tyrosine | Cellular signal transduction | Fibroblast growth factors | Stomach cancer
Resistance | mTOR | FGFR inhibitor | Gastric cancer | EphB3 | SIGNALING PATHWAYS | ADENOCARCINOMA | BIOCHEMISTRY & MOLECULAR BIOLOGY | KINASE | CELL BIOLOGY | EPITHELIAL-MESENCHYMAL TRANSITION | CELL LUNG-CANCER | AZD4547 | GROWTH-FACTOR RECEPTOR | COLORECTAL-CANCER | GENE AMPLIFICATION | PROGNOSTIC-SIGNIFICANCE | Tyrosine | Cellular signal transduction | Fibroblast growth factors | Stomach cancer
Journal Article
British Journal of Cancer, ISSN 0007-0920, 06/2014, Volume 110, Issue 12, pp. 2914 - 2922
Background: Recently, fibroblast growth factor receptor 1 (FGFR1) was discovered in squamous cell carcinomas (SCC) of the lung with FGFR1 amplification...
Amplification | Fluorescence in situ hybridisation | Squamous cell carcinoma | Prognosis | NSCLC | FGFR1 | ACTIVATION | GEFITINIB | prognosis | AZD4547 | amplification | ONCOLOGY | fluorescence it situ hybridisation | CARCINOMA | EXPRESSION | IN-SITU | squamous cell carcinoma | Lung Neoplasms - genetics | Carcinoma, Non-Small-Cell Lung - genetics | Lung Neoplasms - mortality | Tissue Array Analysis | Carcinoma, Squamous Cell - genetics | Humans | Middle Aged | In Situ Hybridization, Fluorescence | Male | Receptor, Fibroblast Growth Factor, Type 1 - genetics | Carcinoma, Non-Small-Cell Lung - mortality | Disease-Free Survival | Carcinoma, Squamous Cell - mortality | Gene Amplification | Aged, 80 and over | Adult | Female | Neoplasm Recurrence, Local - genetics | Aged | Molecular Diagnostics | fluorescence in situ hybridisation
Amplification | Fluorescence in situ hybridisation | Squamous cell carcinoma | Prognosis | NSCLC | FGFR1 | ACTIVATION | GEFITINIB | prognosis | AZD4547 | amplification | ONCOLOGY | fluorescence it situ hybridisation | CARCINOMA | EXPRESSION | IN-SITU | squamous cell carcinoma | Lung Neoplasms - genetics | Carcinoma, Non-Small-Cell Lung - genetics | Lung Neoplasms - mortality | Tissue Array Analysis | Carcinoma, Squamous Cell - genetics | Humans | Middle Aged | In Situ Hybridization, Fluorescence | Male | Receptor, Fibroblast Growth Factor, Type 1 - genetics | Carcinoma, Non-Small-Cell Lung - mortality | Disease-Free Survival | Carcinoma, Squamous Cell - mortality | Gene Amplification | Aged, 80 and over | Adult | Female | Neoplasm Recurrence, Local - genetics | Aged | Molecular Diagnostics | fluorescence in situ hybridisation
Journal Article
Cancer Discovery, ISSN 2159-8274, 06/2015, Volume 5, Issue 6, pp. 610 - 621
Large-scale genomic characterization of squamous cell lung cancers (SQCLC) has revealed several putative oncogenic drivers. There are, however, little data to...
SURVIVAL | AZD4547 | AMPLIFICATION | ONCOLOGY | PATHWAY | ADENOCARCINOMA | COPY NUMBER | SENSITIVITY | MUTATIONS | CARCINOMA | EXPRESSION | Lung Neoplasms - mortality | Carcinoma, Squamous Cell - genetics | Carcinoma, Squamous Cell - pathology | Humans | Middle Aged | Receptor, Fibroblast Growth Factor, Type 1 - metabolism | Lung Neoplasms - pathology | Male | Phosphatidylinositol 3-Kinases - metabolism | Receptor, Fibroblast Growth Factor, Type 1 - genetics | DNA Copy Number Variations | Genetic Variation | Brain Neoplasms - secondary | Neoplasm Metastasis | Carcinoma, Squamous Cell - mortality | DNA Mutational Analysis | Aged, 80 and over | Female | Lung Neoplasms - genetics | PTEN Phosphohydrolase - genetics | Gene Expression | PTEN Phosphohydrolase - deficiency | Serpins - genetics | Signal Transduction | Risk Factors | Kaplan-Meier Estimate | Carcinoma, Squamous Cell - therapy | Genotype | Lung Neoplasms - therapy | Phosphatidylinositol 3-Kinases - genetics | Gene Amplification | Aged | High-Throughput Nucleotide Sequencing | Mutation | Neoplasm Staging | Clonal Evolution | brain metastasis | squamous cell lung cancer | PI3K | FGFR1
SURVIVAL | AZD4547 | AMPLIFICATION | ONCOLOGY | PATHWAY | ADENOCARCINOMA | COPY NUMBER | SENSITIVITY | MUTATIONS | CARCINOMA | EXPRESSION | Lung Neoplasms - mortality | Carcinoma, Squamous Cell - genetics | Carcinoma, Squamous Cell - pathology | Humans | Middle Aged | Receptor, Fibroblast Growth Factor, Type 1 - metabolism | Lung Neoplasms - pathology | Male | Phosphatidylinositol 3-Kinases - metabolism | Receptor, Fibroblast Growth Factor, Type 1 - genetics | DNA Copy Number Variations | Genetic Variation | Brain Neoplasms - secondary | Neoplasm Metastasis | Carcinoma, Squamous Cell - mortality | DNA Mutational Analysis | Aged, 80 and over | Female | Lung Neoplasms - genetics | PTEN Phosphohydrolase - genetics | Gene Expression | PTEN Phosphohydrolase - deficiency | Serpins - genetics | Signal Transduction | Risk Factors | Kaplan-Meier Estimate | Carcinoma, Squamous Cell - therapy | Genotype | Lung Neoplasms - therapy | Phosphatidylinositol 3-Kinases - genetics | Gene Amplification | Aged | High-Throughput Nucleotide Sequencing | Mutation | Neoplasm Staging | Clonal Evolution | brain metastasis | squamous cell lung cancer | PI3K | FGFR1
Journal Article
Oncotarget, ISSN 1949-2553, 2017, Volume 8, Issue 43, pp. 74539 - 74553
Amplification of the fibroblast growth factor receptor 1 (FGFR1) is believed to predict response to FGFR inhibitors. The aim of this study was to investigate...
Clinical stage | Disease free survival time | FGFR1 high amplification | ESCC | Prognostic marker | SURVIVAL | PROTEIN | LANDSCAPE | disease free survival time | clinical stage | CANCER | CELL BIOLOGY | AZD4547 | prognostic marker | SQUAMOUS-CELL CARCINOMA | EXPRESSION
Clinical stage | Disease free survival time | FGFR1 high amplification | ESCC | Prognostic marker | SURVIVAL | PROTEIN | LANDSCAPE | disease free survival time | clinical stage | CANCER | CELL BIOLOGY | AZD4547 | prognostic marker | SQUAMOUS-CELL CARCINOMA | EXPRESSION
Journal Article
AGING-US, ISSN 1945-4589, 09/2019, Volume 11, Issue 18, pp. 7780 - 7795
Rapid appearance of resistance to fibroblast growth factor receptor (FGFR) inhibitors hampers targeted regimens in bladder cancer. In the present study, we...
MIGRATION | SIGNALING PATHWAYS | COMPREHENSIVE MOLECULAR CHARACTERIZATION | SENSITIVITY | CELL BIOLOGY | GERIATRICS & GERONTOLOGY | AZD4547 | INVASION | xenograft | bladder cancer | GROWTH | sulfated polysaccharide of Sepiella maindroni ink | CARCINOMA | EXPRESSION | FGFR therapy resistance
MIGRATION | SIGNALING PATHWAYS | COMPREHENSIVE MOLECULAR CHARACTERIZATION | SENSITIVITY | CELL BIOLOGY | GERIATRICS & GERONTOLOGY | AZD4547 | INVASION | xenograft | bladder cancer | GROWTH | sulfated polysaccharide of Sepiella maindroni ink | CARCINOMA | EXPRESSION | FGFR therapy resistance
Journal Article
Annals of Oncology, ISSN 0923-7534, 06/2017, Volume 28, Issue 6, pp. 1250 - 1259
Background: We conducted co-clinical trials in patient-derived xenograft (PDX) models to identify predictive biomarkers for the multikinase inhibitor dovitinib...
Biomarker | Dovitinib | Squamous cell lung cancer | Fibroblast growth factor receptor | Patient-derived xenograft | SURVIVAL | XENOGRAFT MODELS | NUMBER | PANEL | dovitinib | squamous cell lung cancer | biomarker | CANCER | AZD4547 | AMPLIFICATION | ONCOLOGY | fibroblast growth factor receptor | patient-derived xenograft | Lung Neoplasms - genetics | Lung Neoplasms - drug therapy | Signal Transduction | Carcinoma, Squamous Cell - genetics | Humans | Receptors, Fibroblast Growth Factor - antagonists & inhibitors | Clinical Trials as Topic | Biomarkers - blood | Whole Exome Sequencing | Carcinoma, Squamous Cell - drug therapy | Quinolones - therapeutic use | Receptors, Fibroblast Growth Factor - metabolism | Mutation | Benzimidazoles - therapeutic use
Biomarker | Dovitinib | Squamous cell lung cancer | Fibroblast growth factor receptor | Patient-derived xenograft | SURVIVAL | XENOGRAFT MODELS | NUMBER | PANEL | dovitinib | squamous cell lung cancer | biomarker | CANCER | AZD4547 | AMPLIFICATION | ONCOLOGY | fibroblast growth factor receptor | patient-derived xenograft | Lung Neoplasms - genetics | Lung Neoplasms - drug therapy | Signal Transduction | Carcinoma, Squamous Cell - genetics | Humans | Receptors, Fibroblast Growth Factor - antagonists & inhibitors | Clinical Trials as Topic | Biomarkers - blood | Whole Exome Sequencing | Carcinoma, Squamous Cell - drug therapy | Quinolones - therapeutic use | Receptors, Fibroblast Growth Factor - metabolism | Mutation | Benzimidazoles - therapeutic use
Journal Article
Annals of Surgical Oncology, ISSN 1068-9265, 4/2019, Volume 26, Issue 4, pp. 1093 - 1102
The prognosis of scirrhous gastric carcinoma (SGC), which is characterized by rapid infiltration and proliferation of cancer cells accompanied by extensive...
Oncology | Medicine & Public Health | Surgical Oncology | Surgery | AZD4547 | SURGERY | FACTOR RECEPTOR INHIBITOR | SELECTIVE INHIBITOR | KERATINOCYTE GROWTH-FACTOR | ONCOLOGY | SAFETY | GENE AMPLIFICATION | MYOFIBROBLASTS | K-SAM | PHASE-I | CARCINOMA | Fibroblast growth factors | Epidermal growth factor | Stomach cancer | Analysis | Cancer
Oncology | Medicine & Public Health | Surgical Oncology | Surgery | AZD4547 | SURGERY | FACTOR RECEPTOR INHIBITOR | SELECTIVE INHIBITOR | KERATINOCYTE GROWTH-FACTOR | ONCOLOGY | SAFETY | GENE AMPLIFICATION | MYOFIBROBLASTS | K-SAM | PHASE-I | CARCINOMA | Fibroblast growth factors | Epidermal growth factor | Stomach cancer | Analysis | Cancer
Journal Article
International Journal of Molecular Medicine, ISSN 1107-3756, 10/2013, Volume 32, Issue 4, pp. 763 - 767
Angiogenesis is a process of neovascular formation from pre-existing blood vessels, which consists of sequential steps for vascular destabilization, angiogenic...
Dovitinib | Lung cancer | Colorectal cancer | Breast cancer | Ponatinib | Vascular medicine | Bevacizumab | AZD4547 | Sunitinib | Sorafenib | Chitosan | Gastric cancer | Field cancerization | Poly(lactic-co-glycolic acid) | sunitinib | VASCULAR DEVELOPMENT | MEDICINE, RESEARCH & EXPERIMENTAL | chitosan | CELLS | vascular medicine | ANTI-VEGF | colorectal cancer | sorafenib | gastric cancer | breast cancer | dovitinib | OVARIAN-CANCER | DELIVERY | lung cancer | BREAST-CANCER | field cancerization | THERAPY | DISEASE | bevacizumab | ponatinib | poly(lactic-co-glycolic acid) | ENDOTHELIAL GROWTH-FACTOR | Cell Proliferation | Epigenesis, Genetic | Humans | MicroRNAs - metabolism | Vascular Endothelial Growth Factor A - genetics | Antibodies, Monoclonal, Humanized - genetics | Fibroblast Growth Factor 4 - genetics | Neoplasms - therapy | Neoplasms - genetics | Angiogenesis Inhibitors - therapeutic use | Fibroblast Growth Factor 2 - metabolism | Fibroblast Growth Factor 4 - metabolism | Neovascularization, Pathologic - therapy | Antibodies, Monoclonal, Humanized - therapeutic use | Signal Transduction | Endothelial Cells - metabolism | Vascular Endothelial Growth Factor A - therapeutic use | Genotype | Fibroblast Growth Factor 2 - genetics | Macular Degeneration - genetics | Macular Degeneration - therapy | Neovascularization, Pathologic - genetics | MicroRNAs - genetics | Neoplasms - pathology | Macular Degeneration - pathology
Dovitinib | Lung cancer | Colorectal cancer | Breast cancer | Ponatinib | Vascular medicine | Bevacizumab | AZD4547 | Sunitinib | Sorafenib | Chitosan | Gastric cancer | Field cancerization | Poly(lactic-co-glycolic acid) | sunitinib | VASCULAR DEVELOPMENT | MEDICINE, RESEARCH & EXPERIMENTAL | chitosan | CELLS | vascular medicine | ANTI-VEGF | colorectal cancer | sorafenib | gastric cancer | breast cancer | dovitinib | OVARIAN-CANCER | DELIVERY | lung cancer | BREAST-CANCER | field cancerization | THERAPY | DISEASE | bevacizumab | ponatinib | poly(lactic-co-glycolic acid) | ENDOTHELIAL GROWTH-FACTOR | Cell Proliferation | Epigenesis, Genetic | Humans | MicroRNAs - metabolism | Vascular Endothelial Growth Factor A - genetics | Antibodies, Monoclonal, Humanized - genetics | Fibroblast Growth Factor 4 - genetics | Neoplasms - therapy | Neoplasms - genetics | Angiogenesis Inhibitors - therapeutic use | Fibroblast Growth Factor 2 - metabolism | Fibroblast Growth Factor 4 - metabolism | Neovascularization, Pathologic - therapy | Antibodies, Monoclonal, Humanized - therapeutic use | Signal Transduction | Endothelial Cells - metabolism | Vascular Endothelial Growth Factor A - therapeutic use | Genotype | Fibroblast Growth Factor 2 - genetics | Macular Degeneration - genetics | Macular Degeneration - therapy | Neovascularization, Pathologic - genetics | MicroRNAs - genetics | Neoplasms - pathology | Macular Degeneration - pathology
Journal Article
European Journal of Medicinal Chemistry, ISSN 0223-5234, 01/2017, Volume 126, pp. 476 - 490
The fibroblast growth factor receptor (FGFR) family receptor tyrosine kinase (RTK) includes four structurally related members, termed as FGFR1, FGFR2, FGFR3,...
DFG-in/out | Pharmacological activity | Irreversible | FGFR | Small molecule inhibitor | Crystal structure | DOMAIN | CHEMISTRY, MEDICINAL | SENSITIVITY | NVP-BGJ398 | ENDOMETRIAL CANCER | FAMILY | AZD4547 | GROWTH-FACTOR RECEPTOR | SELECTIVE INHIBITOR | MUTATION | OPPORTUNITY | Small Molecule Libraries - chemistry | Small Molecule Libraries - pharmacology | Protein Kinase Inhibitors - chemistry | Humans | Protein Binding | Protein Kinase Inhibitors - pharmacology | Small Molecule Libraries - metabolism | Receptor Protein-Tyrosine Kinases - metabolism | Protein Kinase Inhibitors - metabolism | Tyrosine | Analysis | Pharmacy | Crystals | Phenols | Drugstores | Fibroblast growth factors | Structure | Phosphotransferases
DFG-in/out | Pharmacological activity | Irreversible | FGFR | Small molecule inhibitor | Crystal structure | DOMAIN | CHEMISTRY, MEDICINAL | SENSITIVITY | NVP-BGJ398 | ENDOMETRIAL CANCER | FAMILY | AZD4547 | GROWTH-FACTOR RECEPTOR | SELECTIVE INHIBITOR | MUTATION | OPPORTUNITY | Small Molecule Libraries - chemistry | Small Molecule Libraries - pharmacology | Protein Kinase Inhibitors - chemistry | Humans | Protein Binding | Protein Kinase Inhibitors - pharmacology | Small Molecule Libraries - metabolism | Receptor Protein-Tyrosine Kinases - metabolism | Protein Kinase Inhibitors - metabolism | Tyrosine | Analysis | Pharmacy | Crystals | Phenols | Drugstores | Fibroblast growth factors | Structure | Phosphotransferases
Journal Article
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Structure-based discovery of a series of 5H-pyrrolo[2, 3-b]pyrazine FGFR kinase inhibitors
Molecules, ISSN 1420-3049, 2018, Volume 23, Issue 3, p. 698
Fibroblast growth factor receptors (FGFRs), a subfamily of receptor tyrosine kinases, are aberrant in various cancer types, and considered to be promising...
Pyrrolo[2,3-b]pyrazine | FGFR | Kinase inhibitor | Cancer | CH5183284/DEBIO 1347 | AZD4547 | kinase inhibitor | SELECTIVE INHIBITOR | POTENT | pyrrolo[2,3-b]pyrazine | BIOCHEMISTRY & MOLECULAR BIOLOGY | cancer | TARGETING FGFR | CHEMISTRY, MULTIDISCIPLINARY | Tyrosine | Fibroblast growth factor | Hepatocyte growth factor | Cyclin-dependent kinases | Growth factor receptors | Kinases | c-Met protein | Receptors | Inhibitors | Pyrazine | Growth factors | Fibroblast growth factor receptor 1 | Crystal structure | Fibroblast growth factor receptors
Pyrrolo[2,3-b]pyrazine | FGFR | Kinase inhibitor | Cancer | CH5183284/DEBIO 1347 | AZD4547 | kinase inhibitor | SELECTIVE INHIBITOR | POTENT | pyrrolo[2,3-b]pyrazine | BIOCHEMISTRY & MOLECULAR BIOLOGY | cancer | TARGETING FGFR | CHEMISTRY, MULTIDISCIPLINARY | Tyrosine | Fibroblast growth factor | Hepatocyte growth factor | Cyclin-dependent kinases | Growth factor receptors | Kinases | c-Met protein | Receptors | Inhibitors | Pyrazine | Growth factors | Fibroblast growth factor receptor 1 | Crystal structure | Fibroblast growth factor receptors
Journal Article
Clinical Pharmacology & Therapeutics, ISSN 0009-9236, 05/2015, Volume 97, Issue 5, pp. 488 - 491
Although the proportion of patients with squamous cell carcinoma of the lung has declined over the last two decades, the disease is still fatal for tens of...
AZD4547 | 1ST-LINE TREATMENT | THERAPY | PHASE-II | PHARMACOLOGY & PHARMACY | MUTATIONS | INHIBITOR | CANCER | CHEMOTHERAPY | EGFR | Lung Neoplasms - drug therapy | Carcinoma, Squamous Cell - genetics | Carcinoma, Squamous Cell - metabolism | Genomics | Humans | Lung Neoplasms - metabolism | Lung Neoplasms - pathology | Antineoplastic Agents - therapeutic use | Molecular Targeted Therapy | Clinical Trials, Phase III as Topic - methods | Carcinoma, Non-Small-Cell Lung - secondary | Biomarkers, Tumor - metabolism | Precision Medicine | Lung Neoplasms - genetics | Genetic Predisposition to Disease | Carcinoma, Non-Small-Cell Lung - genetics | Carcinoma, Non-Small-Cell Lung - metabolism | Phenotype | Carcinoma, Squamous Cell - drug therapy | Signal Transduction - drug effects | Carcinoma, Squamous Cell - secondary | Biomarkers, Tumor - genetics | Carcinoma, Non-Small-Cell Lung - drug therapy | Clinical Trials, Phase II as Topic - methods | Research Design | Squamous cell carcinoma | Usage | Oncology, Experimental | Clinical trials | Research | Drug therapy | Cancer
AZD4547 | 1ST-LINE TREATMENT | THERAPY | PHASE-II | PHARMACOLOGY & PHARMACY | MUTATIONS | INHIBITOR | CANCER | CHEMOTHERAPY | EGFR | Lung Neoplasms - drug therapy | Carcinoma, Squamous Cell - genetics | Carcinoma, Squamous Cell - metabolism | Genomics | Humans | Lung Neoplasms - metabolism | Lung Neoplasms - pathology | Antineoplastic Agents - therapeutic use | Molecular Targeted Therapy | Clinical Trials, Phase III as Topic - methods | Carcinoma, Non-Small-Cell Lung - secondary | Biomarkers, Tumor - metabolism | Precision Medicine | Lung Neoplasms - genetics | Genetic Predisposition to Disease | Carcinoma, Non-Small-Cell Lung - genetics | Carcinoma, Non-Small-Cell Lung - metabolism | Phenotype | Carcinoma, Squamous Cell - drug therapy | Signal Transduction - drug effects | Carcinoma, Squamous Cell - secondary | Biomarkers, Tumor - genetics | Carcinoma, Non-Small-Cell Lung - drug therapy | Clinical Trials, Phase II as Topic - methods | Research Design | Squamous cell carcinoma | Usage | Oncology, Experimental | Clinical trials | Research | Drug therapy | Cancer
Journal Article