PF-06463922 is a potent and selective next-generation ROS1/ALK inhibitor capable of blocking crizotinib-resistant ROS1 mutations

Proceedings of the National Academy of Sciences of the United States of America

Volumn 112, Issue 11, 2015, Pages 3493-3498

  Zou, Helen Y ^a   Li, Qiuhua ^a   Engstrom, Lars D ^a   West, Melissa ^a   Appleman, Vicky ^b   Wong, Katy A ^b   McTigue, Michele ^a   Deng, Ya Li ^a   Liu, Wei ^a   Brooun, Alexei ^a   Timofeevski, Sergei ^a   McDonnell, Scott R P ^a   Jiang, Ping ^a   Falk, Matthew D ^a   Lappin, Patrick B ^a   Affolter, Timothy ^a   Nichols, Tim ^a   Hu, Wenyue ^a   Lam, Justine ^a   Johnson, Ted W ^a   Smeal, Tod ^a   Charest, Al ^b,c   Fantin, Valeria R ^a   more..

^a PFIZER INC   (United States)

^b TUFTS MEDICAL CENTER   (United States)

^c TUFTS UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

Kinase inhibitor; PF 06463922; ROS1

Indexed keywords

ALECTINIB; ANTINEOPLASTIC AGENT; CERITINIB; CRIZOTINIB; FORETINIB; PF 06463922; PROTEIN KINASE; PROTEIN KINASE INHIBITOR; ROS1 KINASE; UNCLASSIFIED DRUG; 7-AMINO-12-FLUORO-2,10,16-TRIMETHYL-15-OXO-10,15,16,17-TETRAHYDRO-2H-8,4-(METHENO)PYRAZOLO(4,3-H)(2,5,11)BENZOXADIAZACYCLOTETRADECINE-3-CARBONITRILE; MACROCYCLIC LACTAM; ONCOPROTEIN; PROTEIN TYROSINE KINASE; PYRAZOLE DERIVATIVE; PYRIDINE DERIVATIVE; ROS1 PROTEIN, HUMAN;

3T3 CELL LINE; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANTINEOPLASTIC ACTIVITY; ANTIPROLIFERATIVE ACTIVITY; ARTICLE; AUTOPHOSPHORYLATION; BINDING AFFINITY; BIOLUMINESCENCE; C ROS ONCOGENE 1; CELL GROWTH; CELL LYSATE; CELL PROLIFERATION; COMPARATIVE STUDY; COMPETITIVE BINDING ASSAY; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG BINDING SITE; DRUG PENETRATION; DRUG POTENCY; DRUG SELECTIVITY; ENZYME ACTIVITY; ENZYME ASSAY; ENZYME INHIBITION; GENE FUSION; GENE MUTATION; GLIOBLASTOMA; HISTOPATHOLOGY; HUMAN; HUMAN CELL; HYDROGEN BOND; IC50; MAXIMUM PLASMA CONCENTRATION; MOUSE; NONHUMAN; ONCOGENE; PRIORITY JOURNAL; PROTEIN CONFORMATION; PROTEIN INTERACTION; SEQUENCE HOMOLOGY; STRUCTURAL HOMOLOGY; TUMOR GROWTH; TUMOR REGRESSION; TUMOR VOLUME; WESTERN BLOTTING; ANIMAL; ANTAGONISTS AND INHIBITORS; CARCINOGENESIS; CHEMICAL STRUCTURE; CHEMISTRY; DISEASE MODEL; DRUG EFFECTS; DRUG RESISTANCE; GENETICS; GLIOMA; MUTATION; PATHOLOGY; SIGNAL TRANSDUCTION; X RAY CRYSTALLOGRAPHY;

PYRONIA TITHONUS;

ANIMALS; CARCINOGENESIS; CELL PROLIFERATION; CRYSTALLOGRAPHY, X-RAY; DISEASE MODELS, ANIMAL; DRUG RESISTANCE, NEOPLASM; GLIOMA; HUMANS; LACTAMS, MACROCYCLIC; MICE; MODELS, MOLECULAR; MUTATION; PROTEIN KINASE INHIBITORS; PROTEIN-TYROSINE KINASES; PROTO-ONCOGENE PROTEINS; PYRAZOLES; PYRIDINES; SIGNAL TRANSDUCTION;

EID: 84925307919     PISSN: 00278424     EISSN: 10916490     Source Type: Journal    
DOI: 10.1073/pnas.1420785112     Document Type: Article

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