نتایج جستجو برای: PF-04217903

تعداد نتایج: 9619  

Journal: :Molecular cancer therapeutics 2012
Helen Y Zou Qiuhua Li Joseph H Lee Maria E Arango Kristina Burgess Ming Qiu Lars D Engstrom Shinji Yamazaki Max Parker Sergei Timofeevski Jingrong Jean Cui Michele McTigue Gerrit Los Steven L Bender Tod Smeal James G Christensen

The c-Met pathway has been implicated in a variety of human cancers for its critical role in tumor growth, invasion, and metastasis. PF-04217903 is a novel ATP-competitive small-molecule inhibitor of c-Met kinase. PF-04217903 showed more than 1,000-fold selectivity for c-Met compared with more than 150 kinases, making it one of the most selective c-Met inhibitors described to date. PF-04217903 ...

2012
Helen Y. Zou Qiuhua Li Joseph H. Lee Maria E. Arango Kristina Burgess Ming Qiu Lars D. Engstrom Shinji Yamazaki Max Parker Sergei Timofeevski Jingrong Jean Cui Michele McTigue Gerrit Los Steven L. Bender Tod Smeal James G. Christensen

The c-Met pathway has been implicated in a variety of human cancers for its critical role in tumor growth, invasion, andmetastasis. PF-04217903 is a novelATP-competitive small-molecule inhibitor of c-Met kinase. PF04217903 showed more than 1,000-fold selectivity for c-Met compared with more than 150 kinases, making it one of the most selective c-Met inhibitors described to date. PF-04217903 inh...

Journal: :Drug metabolism and disposition: the biological fate of chemicals 2011
Shinji Yamazaki Judith Skaptason David Romero Sylvia Vekich Hannah M Jones Weiwei Tan Keith D Wilner Tatiana Koudriakova

The objective of this study was to assess the physiologically based pharmacokinetic (PBPK) model for predicting plasma concentration-time profiles of orally available cMet kinase inhibitors, (R)-3-[1-(2,6-dichloro-3-fluoro-phenyl)-ethoxy]-5-(1-piperidin-4-yl-1H-pyrazol-4-yl)-pyridin-2-ylamine (PF02341066) and 2-[4-(3-quinolin-6-ylmethyl-3H-[1,2,3]triazolo[4,5-b]pyrazin-5-yl)-pyrazol-1-yl]-ethan...

Journal: :Cancer discovery 2012
Barbara Sennino Toshina Ishiguro-Oonuma Ying Wei Ryan M Naylor Casey W Williamson Vikash Bhagwandin Sebastien P Tabruyn Weon-Kyoo You Harold A Chapman James G Christensen Dana T Aftab Donald M McDonald

UNLABELLED Invasion and metastasis increase after the inhibition of VEGF signaling in some preclinical tumor models. In the present study we asked whether selective VEGF inhibition is sufficient to increase invasion and metastasis and whether selective c-Met inhibition is sufficient to block this effect. Treatment of pancreatic neuroendocrine tumors in RIP-Tag2 mice with a neutralizing anti-VEG...

Journal: :Cancer research 2013
Barbara Sennino Toshina Ishiguro-Oonuma Brian J Schriver James G Christensen Donald M McDonald

Inhibition of VEGF signaling can promote lymph node metastasis in preclinical models, but the mechanism is not fully understood, and successful methods of prevention have not been found. Signaling of hepatocyte growth factor (HGF) and its receptor c-Met can promote the growth of lymphatics and metastasis of some tumors. We sought to explore the contributions of c-Met signaling to lymph node met...

2013
Barbara Sennino Toshina Ishiguro-Oonuma Brian J. Schriver James G. Christensen Donald M. McDonald

Inhibition of VEGF signaling can promote lymph node metastasis in preclinical models, but the mechanism is not fully understood, and successful methods of prevention have not been found. Signaling of hepatocyte growth factor (HGF) and its receptor c-Met can promote the growth of lymphatics and metastasis of some tumors. We sought to explore the contributions of c-Met signaling to lymph node met...

Journal: :Hypertension 2015
Ricardo A Peña-Silva Nohra Chalouhi Lauren Wegman-Points Muhammad Ali Ian Mitchell Gary L Pierce Yi Chu Zuhair K Ballas Donald Heistad David Hasan

Inflammation plays a key role in formation and rupture of intracranial aneurysms. Because hepatocyte growth factor (HGF) protects against vascular inflammation, we sought to assess the role of endogenous HGF in the pathogenesis of intracranial aneurysms. Circulating HGF concentrations in blood samples drawn from the lumen of human intracranial aneurysms or femoral arteries were compared in 16 p...

2015
Iwei Yeh Thomas Botton Eric Talevich A. Hunter Shain Alyssa J. Sparatta Arnaud de la Fouchardiere Thaddeus W. Mully Jeffrey P. North Maria C. Garrido Alexander Gagnon Swapna S. Vemula Timothy H. McCalmont Philip E. LeBoit Boris C. Bastian

Oncogenic gene fusions have been identified in many cancers and many serve as biomarkers or targets for therapy. Here we identify six different melanocytic tumours with genomic rearrangements of MET fusing the kinase domain of MET in-frame to six different N-terminal partners. These tumours lack activating mutations in other established melanoma oncogenes. We functionally characterize two of th...

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