Discovery of 3‑(3-(4-(1-Aminocyclobutyl)phenyl)-5-phenyl‑3H‑imidazo[4,5‑b]pyridin-2-yl)pyridin-2-amine (ARQ 092): An Orally Bioavailable, Selective, and Potent Allosteric AKT Inhibitor
Lapierre, Jean-Marc, Eathiraj, Sudharshan, Vensel, David, Liu, Yanbin, Bull, Cathy O, Cornell-Kennon, Susan, Iimura, Shin, Kelleher, Eugene W, Kizer, Darin E, Koerner, Steffi, Makhija, Sapna, Matsuda, Akihisa, Moussa, Magdi, Namdev, Nivedita, Savage, Ronald E, Szwaya, Jeff, Volckova, Erika, Westlund, Neil, Wu, Hui, Schwartz, Brian
Published in Journal of medicinal chemistry (14.07.2016)
Published in Journal of medicinal chemistry (14.07.2016)
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Journal Article
Discovery and Optimization of a Series of 3-(3-Phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amines: Orally Bioavailable, Selective, and Potent ATP-Independent Akt Inhibitors
Ashwell, Mark A, Lapierre, Jean-Marc, Brassard, Christopher, Bresciano, Karen, Bull, Cathy, Cornell-Kennon, Susan, Eathiraj, Sudharshan, France, Dennis S, Hall, Terence, Hill, Jason, Kelleher, Eoin, Khanapurkar, Sampada, Kizer, Darin, Koerner, Steffi, Link, Jeff, Liu, Yanbin, Makhija, Sapna, Moussa, Magdi, Namdev, Nivedita, Nguyen, Khanh, Nicewonger, Robert, Palma, Rocio, Szwaya, Jeff, Tandon, Manish, Uppalapati, Uma, Vensel, David, Volak, Laurie P, Volckova, Erika, Westlund, Neil, Wu, Hui, Yang, Rui-Yang, Chan, Thomas C. K
Published in Journal of medicinal chemistry (14.06.2012)
Published in Journal of medicinal chemistry (14.06.2012)
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Abstract A169: Assessment of genotype-correlated sensitivity to the investigational PI3Kα selective inhibitor MLN1117 in preclinical models
Iartchouk, Natasha, Koenig, Erik, Shah, Pooja, Szwaya, Jeff, Fitzgerald, Michael, Zhang, Dong Mei, Cao, Yueying, Song, Keli, Brake, Rachael
Published in Molecular cancer therapeutics (01.11.2013)
Published in Molecular cancer therapeutics (01.11.2013)
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Abstract C176: The combination of mTORC1/2 and PI3Kα inhibition alleviates PI3K pathway reactivation and leads to significant antitumor activity in multiple preclinical xenograft models
Brake, Rachael L., Fabrey, Robyn, Szwaya, Jeff, Fitzgerald, Michael, Iartchouk, Natasha, Guo, Xin, Kuida, Keisuke, Zohren, Fabian, Manfredi, Mark
Published in Molecular cancer therapeutics (01.11.2013)
Published in Molecular cancer therapeutics (01.11.2013)
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Journal Article
Discovery of 3-(3-(4-(1-Aminocyclobutyl)phenyl)-5-phenyl-3 H -imidazo[4,5- b ]pyridin-2-yl)pyridin-2-amine (ARQ 092): An Orally Bioavailable, Selective, and Potent Allosteric AKT Inhibitor
Lapierre, Jean-Marc, Eathiraj, Sudharshan, Vensel, David, Liu, Yanbin, Bull, Cathy O., Cornell-Kennon, Susan, Iimura, Shin, Kelleher, Eugene W., Kizer, Darin E., Koerner, Steffi, Makhija, Sapna, Matsuda, Akihisa, Moussa, Magdi, Namdev, Nivedita, Savage, Ronald E., Szwaya, Jeff, Volckova, Erika, Westlund, Neil, Wu, Hui, Schwartz, Brian
Published in Journal of medicinal chemistry (14.07.2016)
Published in Journal of medicinal chemistry (14.07.2016)
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Abstract 3571: Exploratory biomarker discovery for clinical development of ARQ 087, a potent pan-FGFR kinase inhibitor
Yu, Yi, Gu, Xiubin, Nakuci, Enkelada, Zhao, Xiaolan, Chang, Edward, Szwaya, Jeff, Castro, Jenn, Cousens, Laura, Bull, Cathy, Wang, Yunxia, Savage, Ron, Waghorne, Carol, Chen, Chang-Rung, France, Dennis S., Clark, Edwin, Chan, Thomas C.K.
Published in Cancer research (Chicago, Ill.) (15.04.2011)
Published in Cancer research (Chicago, Ill.) (15.04.2011)
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Abstract LB-1: Discovery and optimization of orally bioavailable, selective and potent ATP-independent Akt inhibitors
Chan, Thomas C.K., Ashwell, Mark A., Lapierre, Jean-Marc, Brassard, Christopher, Bull, Cathy, Cornell-Kennon, Susan, Eathiraj, Sudharshan, France, Dennis S., Hill, Jason, Koerner, Steffi, Kelleher, Eoin, Kizer, Darin, Liu, Yanbin, Link, Jeff, Makhija, Sapna, Moussa, Magdi, Namdev, Nivedita, Nicewonger, Robert, Uppalapati, Uma, Palma, Rocio, Szwaya, Jeff, Tandon, Manish, Vensel, David, Volak, Laurie, Volckova, Erika, Westland, Neil, Wu, Hui, Yang, Rui-Yang
Published in Cancer research (Chicago, Ill.) (15.04.2012)
Published in Cancer research (Chicago, Ill.) (15.04.2012)
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