Discovery of 3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), A Potent and Selective Inhibitor of the Fibroblast Growth Factor Receptor Family of Receptor Tyrosine Kinase
Guagnano, Vito, Furet, Pascal, Spanka, Carsten, Bordas, Vincent, Le Douget, Mickaël, Stamm, Christelle, Brueggen, Josef, Jensen, Michael R, Schnell, Christian, Schmid, Herbert, Wartmann, Markus, Berghausen, Joerg, Drueckes, Peter, Zimmerlin, Alfred, Bussiere, Dirksen, Murray, Jeremy, Graus Porta, Diana
Published in Journal of medicinal chemistry (27.10.2011)
Published in Journal of medicinal chemistry (27.10.2011)
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FGFR genetic alterations predict for sensitivity to NVP-BGJ398, a selective pan-FGFR inhibitor
Guagnano, Vito, Kauffmann, Audrey, Wöhrle, Simon, Stamm, Christelle, Ito, Moriko, Barys, Louise, Pornon, Astrid, Yao, Yao, Li, Fang, Zhang, Yun, Chen, Zhi, Wilson, Christopher J, Bordas, Vincent, Le Douget, Mickaël, Gaither, L Alex, Borawski, Jason, Monahan, John E, Venkatesan, Kavitha, Brümmendorf, Thomas, Thomas, David M, Garcia-Echeverria, Carlos, Hofmann, Francesco, Sellers, William R, Graus-Porta, Diana
Published in Cancer discovery (01.12.2012)
Published in Cancer discovery (01.12.2012)
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FGF receptors control vitamin D and phosphate homeostasis by mediating renal FGF‐23 signaling and regulating FGF‐23 expression in bone
Wöhrle, Simon, Bonny, Olivier, Beluch, Noemie, Gaulis, Swann, Stamm, Christelle, Scheibler, Marcel, Müller, Matthias, Kinzel, Bernd, Thuery, Anne, Brueggen, Joseph, Hynes, Nancy E, Sellers, William R, Hofmann, Francesco, Graus‐Porta, Diana
Published in Journal of bone and mineral research (01.10.2011)
Published in Journal of bone and mineral research (01.10.2011)
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Fibroblast growth factor receptors as novel therapeutic targets in SNF5-deleted malignant rhabdoid tumors
Wöhrle, Simon, Weiss, Andreas, Ito, Moriko, Kauffmann, Audrey, Murakami, Masato, Jagani, Zainab, Thuery, Anne, Bauer-Probst, Beatrice, Reimann, Flavia, Stamm, Christelle, Pornon, Astrid, Romanet, Vincent, Guagnano, Vito, Brümmendorf, Thomas, Sellers, William R, Hofmann, Francesco, Roberts, Charles W M, Graus Porta, Diana
Published in PloS one (2013)
Published in PloS one (2013)
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Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4
Fairhurst, Robin A, Knoepfel, Thomas, Buschmann, Nicole, Leblanc, Catherine, Mah, Robert, Todorov, Milen, Nimsgern, Pierre, Ripoche, Sebastien, Niklaus, Michel, Warin, Nicolas, Luu, Van Huy, Madoerin, Mario, Wirth, Jasmin, Graus-Porta, Diana, Weiss, Andreas, Kiffe, Michael, Wartmann, Markus, Kinyamu-Akunda, Jacqueline, Sterker, Dario, Stamm, Christelle, Adler, Flavia, Buhles, Alexandra, Schadt, Heiko, Couttet, Philippe, Blank, Jutta, Galuba, Inga, Trappe, Jörg, Voshol, Johannes, Ostermann, Nils, Zou, Chao, Berghausen, Jörg, Del Rio Espinola, Alberto, Jahnke, Wolfgang, Furet, Pascal
Published in Journal of medicinal chemistry (12.11.2020)
Published in Journal of medicinal chemistry (12.11.2020)
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FGF401, A First-In-Class Highly Selective and Potent FGFR4 Inhibitor for the Treatment of FGF19-Driven Hepatocellular Cancer
Weiss, Andreas, Adler, Flavia, Buhles, Alexandra, Stamm, Christelle, Fairhurst, Robin A, Kiffe, Michael, Sterker, Dario, Centeleghe, Mario, Wartmann, Markus, Kinyamu-Akunda, Jacqueline, Schadt, Heiko S, Couttet, Philippe, Wolf, Armin, Wang, Youzhen, Barzaghi-Rinaudo, Patrizia, Murakami, Masato, Kauffmann, Audrey, Knoepfel, Thomas, Buschmann, Nicole, Leblanc, Catherine, Mah, Robert, Furet, Pascal, Blank, Jutta, Hofmann, Francesco, Sellers, William R, Graus Porta, Diana
Published in Molecular cancer therapeutics (01.12.2019)
Published in Molecular cancer therapeutics (01.12.2019)
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Integrated CRISPR screening and drug profiling identifies combination opportunities for EGFR, ALK, and BRAF/MEK inhibitors
Tiedt, Ralph, King, Frederick J., Stamm, Christelle, Niederst, Matthew J., Delach, Scott, Zumstein-Mecker, Sabine, Meltzer, Jodi, Mulford, Iain J., Labrot, Emma, Engstler, Barbara Schacher, Baltschukat, Sabrina, Kerr, Grainne, Golji, Javad, Wyss, Daniel, Schnell, Christian, Ainscow, Edward, Engelman, Jeffrey A., Sellers, William R., Barretina, Jordi, Caponigro, Giordano, Porta, Diana Graus
Published in Cell reports (Cambridge) (25.04.2023)
Published in Cell reports (Cambridge) (25.04.2023)
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Rescue screens with secreted proteins reveal compensatory potential of receptor tyrosine kinases in driving cancer growth
Harbinski, Fred, Craig, Vanessa J, Sanghavi, Sneha, Jeffery, Douglas, Liu, Lijuan, Sheppard, Kelly Ann, Wagner, Sabrina, Stamm, Christelle, Buness, Andreas, Chatenay-Rivauday, Christian, Yao, Yao, He, Feng, Lu, Chris X, Guagnano, Vito, Metz, Thomas, Finan, Peter M, Hofmann, Francesco, Sellers, William R, Porter, Jeffrey A, Myer, Vic E, Graus-Porta, Diana, Wilson, Christopher J, Buckler, Alan, Tiedt, Ralph
Published in Cancer discovery (01.10.2012)
Published in Cancer discovery (01.10.2012)
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Abstract 2098: NVP-FGF401, a first-in-class highly selective and potent FGFR4 inhibitor for the treatment of HCC
Porta, Diana Graus, Weiss, Andreas, Fairhurst, Robin A., Wartmann, Markus, Stamm, Christelle, Reimann, Flavia, Buhles, Alexandra, Kinyamu-Akunda, Jaqueline, Sterker, Dario, Murakami, Masato, Wang, Youzhen, Engelman, Jeffrey, Hofmann, Francesco, Sellers, William R.
Published in Cancer research (Chicago, Ill.) (01.07.2017)
Published in Cancer research (Chicago, Ill.) (01.07.2017)
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Abstract 2103: NVP-FGF401: Cellular and in vivo profile of a novel highly potent and selective FGFR4 inhibitor for the treatment of FGF19/FGFR4/KLB+ tumors
Weiss, Andreas, Porta, Diana Graus, Reimann, Flavia, Buhles, Alexandra, Stamm, Christelle, Fairhurst, Robin A., Kinyamu-Akunda, Jacqueline, Sterker, Dario, Murakami, Masato, Wartmann, Markus, Wang, Youzhen, Engelman, Jeffrey A., Hofmann, Francesco, Sellers, Wiliam R.
Published in Cancer research (Chicago, Ill.) (01.07.2017)
Published in Cancer research (Chicago, Ill.) (01.07.2017)
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Direct and selective pharmacological disruption of the YAP-TEAD interface by IAG933 inhibits Hippo-dependent and RAS-MAPK-altered cancers
Chapeau, Emilie A, Sansregret, Laurent, Galli, Giorgio G, Chène, Patrick, Wartmann, Markus, Mourikis, Thanos P, Jaaks, Patricia, Baltschukat, Sabrina, Barbosa, Ines A M, Bauer, Daniel, Brachmann, Saskia M, Delaunay, Clara, Estadieu, Claire, Faris, Jason E, Furet, Pascal, Harlfinger, Stefanie, Hueber, Andreas, Jiménez Núñez, Eloísa, Kodack, David P, Mandon, Emeline, Martin, Typhaine, Mesrouze, Yannick, Romanet, Vincent, Scheufler, Clemens, Sellner, Holger, Stamm, Christelle, Sterker, Dario, Tordella, Luca, Hofmann, Francesco, Soldermann, Nicolas, Schmelzle, Tobias
Published in Nature cancer (01.07.2024)
Published in Nature cancer (01.07.2024)
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Abstract 3575: Dovitinib (TKI258), a dual inhibitor of FGFR and VEGFR, induces tumor growth suppression in xenograft models of human bladder cancer
Shi, Michael M., Linnartz, Ronald, Versace, Richard, Brueggen, Joseph, Chatenay-Rivauday, Christian, Stamm, Christelle, Dugan, Margaret, Porta, Diana Graus
Published in Cancer research (Chicago, Ill.) (15.04.2011)
Published in Cancer research (Chicago, Ill.) (15.04.2011)
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Journal Article
Abstract B246: NVP-BGJ398: A potent and selective inhibitor of the fibroblast growth factor receptor family
Guagnano, Vito, Porta, Diana Graus, Bordas, Vincent, Douget, Mickael Le, Stamm, Christelle, Furet, Pascal, Spanka, Carsten, Wartmann, Markus, Schmid, Herbert, Brueggen, Josef, Drueckes, Peter, Bussiere, Dirksen, Abrams, Tinya, Rendahl, Katherine, Bernard-Pierrot, Isabelle, Radvanyi, Francois
Published in Molecular cancer therapeutics (12.11.2011)
Published in Molecular cancer therapeutics (12.11.2011)
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Abstract 854: Patient stratification strategies for NVP-BGJ398, a selective pan-FGFR inhibitor in phase I clinical trials
Porta, Diana Graus, Guagnano, Vito, Stamm, Christelle, Woehrle, Simon, Kauffmann, Audrey, Yao, Yao, Brümmendorf, Thomas, Bordas, Vincent, Douget, Mickaël Le, Zhang, Yun, Chen, Zhi, Ito, Moriko, Li, Fang, Monahan, John, Gaither, Alex, Borawski, Jason, Wilson, Christopher J., Venkatesan, Kavitha, Hofmann, Francesco, Sellers, William
Published in Cancer research (Chicago, Ill.) (15.04.2012)
Published in Cancer research (Chicago, Ill.) (15.04.2012)
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Abstract C193: FGFR genetic alterations predict for sensitivity to NVP-BGJ398, a novel orally bioavailable, selective, and potent FGFR inhibitor
Porta, Diana Graus, Guagnano, Vito, Yao, Yao, Kauffmann, Audrey, Stamm, Christelle, Chen, Zhi, Zhang, Yun, Bordas, Vincent, Douget, Mickael Le, Ito, Moriko, Li, Fang, Monahan, John, Gaither, Alex, Borawski, Jason, Wilson, Christopher J., Venkatesan, Kavitha, Bruemmendorf, Thomas, Hofmann, Francesco, Sellers, William R.
Published in Molecular cancer therapeutics (12.11.2011)
Published in Molecular cancer therapeutics (12.11.2011)
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Biotinylated phosphotyrosine containing peptides: A valuable tool for studies on phosphopeptide interactions with SH2 and PTB domains
García-Echeverría, Carlos, Stamm, Christelle, Wille, Roman, Arz, Dorothee, Gay, Brigitte
Published in Letters in Peptide Science (01.03.1997)
Published in Letters in Peptide Science (01.03.1997)
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