生物活性

• 靶点

  EGFR IC50:4nM

  ERBB3 IC50:4nM

  HER2 IC50:3nM

• 描述AZD8931 shows different potency to NSCLC and SCCHN cell lines. AZD8931 has high sensitivity to PC-9 cells (EGFR activating mutation) with GI50 of 0.1 nM and low activity to NCI-1437 cells with GI50 above 10 μM. AZD8931 exhibits more potency against phospho-EGFR, phospho-erbB2 and phospho-erbB3 than either lapatinib or gefitinib in PE/CA-PJ41, PE/CA-PJ49, DOK and FaDu cells.
• 细胞研究
• Cell Data

  Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
  human KB cells	-	Function assay	-	Inhibition of EGF-stimulated EGFR phosphorylation in human KB cells, IC50=4 nM	24900741
  human MCF7 cells	-	Function assay	-	Inhibition of heregulin-stimulated HER2 phosphorylation in human MCF7 cells, IC50=3 nM	24900741
  human MCF7 cells	-	Function assay	-	Inhibition of heregulin-stimulated HER3 phosphorylation in human MCF7 cells, IC50=4 nM	24900741

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• 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
  NCT01862003	Metastatic Colorectal Cancer ... more >> Recurrent Colorectal Cancer Collapse <<	Phase 2	Active, not recruiting	December 2020	United Kingdom ... more >> Barts Health NHS Trust London, United Kingdom Guy's and St Thomas' NHS Foundation Trust London, United Kingdom University College London Hospital NHS Foundation Trust London, United Kingdom The Christie NHS Foundation Trust Manchester, United Kingdom Collapse <<
  NCT02117167	Non-small Cell Lung Cancer Met... more >>astatic Collapse <<	Phase 2	Recruiting	February 2022	France ... more >> 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 Collapse <<
  NCT01151215	Neoplasms Bre... more >>ast Neoplasms Breast Cancer Collapse <<	Phase 2	Terminated(Futility)	-	-

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