Discovery of (10R)-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 (PF-06463922), a Macrocyclic Inhibitor of Anaplastic Lymphoma Kinase (ALK) and c-ros Oncogene 1 (ROS1) with Preclinical Brain Exposure and Broad-Spectrum Potency against ALK-Resistant Mutations
Johnson, Ted W., Richardson, Paul F., Bailey, Simon, Brooun, Alexei, Burke, Benjamin J., Collins, Michael R., Cui, J. Jean, Deal, Judith G., Deng, Ya-Li, Dinh, Dac, Engstrom, Lars D., He, Mingying, Hoffman, Jacqui, Hoffman, Robert L., Huang, Qinhua, Kania, Robert S., Kath, John C., Lam, Hieu, Lam, Justine L., Le, Phuong T., Lingardo, Laura, Liu, Wei, McTigue, Michele, Palmer, Cynthia L., Sach, Neal W., Smeal, Tod, Smith, Graham L., Stewart, Albert E., Timofeevski, Sergei, Zhu, Huichun, Zhu, Jinjiang, Zou, Helen Y., Edwards, Martin P.
Published in Journal of medicinal chemistry (12.06.2014)
Published in Journal of medicinal chemistry (12.06.2014)
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Epithelial tissue hyperplasia induced by the RAF inhibitor PF-04880594 is attenuated by a clinically well-tolerated dose of the MEK inhibitor PD-0325901
Torti, Vince R, Wojciechowicz, Donald, Hu, Wenyue, John-Baptiste, Annette, Evering, Winston, Troche, Gabriel, Marroquin, Lisa D, Smeal, Tod, Yamazaki, Shinji, Palmer, Cynthia L, Burns-Naas, Leigh Ann, Bagrodia, Shubha
Published in Molecular cancer therapeutics (01.10.2012)
Published in Molecular cancer therapeutics (01.10.2012)
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Design of Potent and Selective Inhibitors to Overcome Clinical Anaplastic Lymphoma Kinase Mutations Resistant to Crizotinib
Huang, Qinhua, Johnson, Ted W, Bailey, Simon, Brooun, Alexei, Bunker, Kevin D, Burke, Benjamin J, Collins, Michael R, Cook, Andrew S, Cui, J. Jean, Dack, Kevin N, Deal, Judith G, Deng, Ya-Li, Dinh, Dac, Engstrom, Lars D, He, Mingying, Hoffman, Jacqui, Hoffman, Robert L, Johnson, Patrick S, Kania, Robert S, Lam, Hieu, Lam, Justine L, Le, Phuong T, Li, Qiuhua, Lingardo, Laura, Liu, Wei, Lu, Melissa West, McTigue, Michele, Palmer, Cynthia L, Richardson, Paul F, Sach, Neal W, Shen, Hong, Smeal, Tod, Smith, Graham L, Stewart, Albert E, Timofeevski, Sergei, Tsaparikos, Konstantinos, Wang, Hui, Zhu, Huichun, Zhu, Jinjiang, Zou, Helen Y, Edwards, Martin P
Published in Journal of medicinal chemistry (27.02.2014)
Published in Journal of medicinal chemistry (27.02.2014)
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Abstract PR10: Is CNS availability for oncology a no-brainer? Discovery of PF-06463922, a novel small molecule inhibitor of ALK/ROS1 with preclinical brain availability and broad spectrum potency against ALK-resistant mutations
Johnson, Ted W., Bailey, Simon, Burke, Benjamin J., Collins, Michael R., Cui, J. Jean, Deal, Judy, Deng, Ya-Li, Edwards, Martin P., He, Mingying, Hoffman, Jacqui, Hoffman, Robert L., Huang, Qinhua, Kania, Robert S., Le, Phuong, McTigue, Michele, Palmer, Cynthia L., Richardson, Paul F., Sach, Neal W., Smith, Graham L., Engstrom, Lars, Hu, Wenyue, Lam, Hieu, Lam, Justine L., Smeal, Tod, Zou, Helen Y.
Published in Molecular cancer therapeutics (01.11.2013)
Published in Molecular cancer therapeutics (01.11.2013)
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Journal Article
Discovery of (10R)‑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 (PF-06463922), a Macrocyclic Inhibitor of Anaplastic Lymphoma Kinase (ALK) and c-ros Oncogene 1 (ROS1) with Preclinical Brain Exposure and Broad-Spectrum Potency against ALK-Resistant Mutations
Johnson, Ted W, Richardson, Paul F, Bailey, Simon, Brooun, Alexei, Burke, Benjamin J, Collins, Michael R, Cui, J. Jean, Deal, Judith G, Deng, Ya-Li, Dinh, Dac, Engstrom, Lars D, He, Mingying, Hoffman, Jacqui, Hoffman, Robert L, Huang, Qinhua, Kania, Robert S, Kath, John C, Lam, Hieu, Lam, Justine L, Le, Phuong T, Lingardo, Laura, Liu, Wei, McTigue, Michele, Palmer, Cynthia L, Sach, Neal W, Smeal, Tod, Smith, Graham L, Stewart, Albert E, Timofeevski, Sergei, Zhu, Huichun, Zhu, Jinjiang, Zou, Helen Y, Edwards, Martin P
Published in Journal of medicinal chemistry (12.06.2014)
Published in Journal of medicinal chemistry (12.06.2014)
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Journal Article