Identification of NVP-TNKS656: The Use of Structure–Efficiency Relationships To Generate a Highly Potent, Selective, and Orally Active Tankyrase Inhibitor von Shultz, Michael D, Cheung, Atwood K, Kirby, Christina A, Firestone, Brant, Fan, Jianmei, Chen, Christine Hiu-Tung, Chen, Zhouliang, Chin, Donovan N, DiPietro, Lucian, Fazal, Aleem, Feng, Yun, Fortin, Pascal D, Gould, Ty, Lagu, Bharat, Lei, Huangshu, Lenoir, Francois, Majumdar, Dyuti, Ochala, Etienne, Palermo, M. G, Pham, Ly, Pu, Minying, Smith, Troy, Stams, Travis, Tomlinson, Ronald C, Touré, B. Barry, Visser, Michael, Wang, Run Ming, Waters, Nigel J, Shao, Wenlin

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In vitro and in vivo anticancer activities of synthetic macrocyclic ketone analogues of halichondrin B von TOWLE, Murray J, SALVATO, Kathleen A, HABGOOD, Gregory J, SINGER, Lori A, DIPIETRO, Lucian V, YUAN WANG, CHEN, Jack J, QUINCY, David A, DAVIS, Ashley, YOSHIMATSU, Kentaro, KISHI, Yoshito, YU, Melvin J, BUDROW, Jacqueline, LITTLEFIELD, Bruce A, WELS, Bruce F, KUZNETSOV, Galina, AALFS, Kimberley K, WELSH, Susan, WANJUN ZHENG, SELETSKY, Boris M, PALME, Monica H

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The Role of the Acidity of N‑Heteroaryl Sulfonamides as Inhibitors of Bcl‑2 Family Protein–Protein Interactions von Touré, B. Barry, Miller-Moslin, Karen, Yusuff, Naeem, Perez, Lawrence, Doré, Michael, Joud, Carol, Michael, Walter, DiPietro, Lucian, van der Plas, Simon, McEwan, Michael, Lenoir, Francois, Hoe, Madelene, Karki, Rajesh, Springer, Clayton, Sullivan, John, Levine, Kymberly, Fiorilla, Catherine, Xie, Xiaoling, Kulathila, Raviraj, Herlihy, Kara, Porter, Dale, Visser, Michael

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Evaluation of Protein Kinase cAMP-Activated Catalytic Subunit Alpha as a Therapeutic Target for Fibrolamellar Carcinoma von Schalm, Stefanie S., O’Hearn, Erin, Wilson, Kevin, LaBranche, Timothy P., Silva, Grace, Zhang, Zhuo, DiPietro, Lucian, Bifulco, Neil, Woessner, Richard, Stransky, Nicolas, Sappal, Darshan, Campbell, Robert, Lobbardi, Riadh, Palmer, Michael, Kim, Joseph, Ye, Chaoyang, Dorsch, Marion, Lengauer, Christoph, Guzi, Timothy, Kadambi, Vivek, Garner, Andrew, Hoeflich, Klaus P.

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Precision Targeted Therapy with BLU-667 for RET -Driven Cancers von Subbiah, Vivek, Gainor, Justin F, Rahal, Rami, Brubaker, Jason D, Kim, Joseph L, Maynard, Michelle, Hu, Wei, Cao, Qiongfang, Sheets, Michael P, Wilson, Douglas, Wilson, Kevin J, DiPietro, Lucian, Fleming, Paul, Palmer, Michael, Hu, Mimi I, Wirth, Lori, Brose, Marcia S, Ou, Sai-Hong Ignatius, Taylor, Matthew, Garralda, Elena, Miller, Stephen, Wolf, Beni, Lengauer, Christoph, Guzi, Timothy, Evans, Erica K

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Structurally simplified macrolactone analogues of halichondrin B von Seletsky, Boris M., Wang, Yuan, Hawkins, Lynn D., Palme, Monica H., Habgood, Gregory J., DiPietro, Lucian V., Towle, Murray J., Salvato, Kathleen A., Wels, Bruce F., Aalfs, Kimberley K., Kishi, Yoshito, Littlefield, Bruce A., Yu, Melvin J.

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Abstract P5-16-10: RLY-2608: The first allosteric mutant- and isoform-selective inhibitor of PI3Kα, is efficacious as a single agent and drives regressions in combination with stan... von Pazolli, Ermira, Kipp, Randy, Boezio, Alessandro, Gunaydin, Hakan, Iskandar, Amanda, Zubrowski, Matthew, Williams, Bret, Shortsleeves, Kelley, Larivee, Alexandre, McLean, Tom, Michelsen, Klaus, Zeng, Hongtao, LaRochelle, Jonathan, Manna, Joe, DiPietro, Lucian, Lescarbeau, Andre, Mader, Mary, Bennet, Bindu, Wilbur, Jeremy, Wang, Qi, Pierce, Levi, Martin, Iain, Watters, James, Fortin, Pascal, Bergstrom, Donald

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Abstract P251: Discovery and characterization of RLY-2608: The first allosteric, mutant, and isoform-selective inhibitor of PI3Kα von Pazolli, Ermira, Kipp, Randy, Boezio, Alessandro, Gunaydin, Hakan, Iskandar, Amanda, Zubrowski, Matthew, Williams, Bret, Shortsleeves, Kelley, Larivee, Alexandre, McLean, Tom, Michelsen, Klaus, Zeng, Hongtao, LaRochelle, Jonathan, Manna, Joe, DiPietro, Lucian, Mader, Mary, Bennet, Bindu, Wilbur, Jeremy, Wang, Qi, Pierce, Levi, Martin, Iain, Watters, James, Fortin, Pascal, Bergstrom, Donald

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Abstract B01: BLU-667: A highly selective RET inhibitor to target RET-driven NSCLC von Rahal, Rami, Maynard, Michelle, Hu, Wei, Brubaker, Jason, Cao, Qiangfang, Kim, Joseph L., Sheets, Michael P., Wilson, Douglas P., Wilson, Kevin J., DiPietro, Lucian, LaBranche, Timothy, Wolf, Beni, Guzi, Timothy, Lengauer, Christoph, Evans, Erica K.

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Abstract B127: Evaluating PRKACA as a therapeutic target for Fibrolamellar Carcinoma von Schalm, Stefanie S, O’Hearn, Erin, Wilson, Kevin, LaBranche, Timothy, Silva, Grace, DiPietro, Lucian, Bifulco, Neil, Woessner, Richard, Stransky, Nicolas, Sappal, Darshan, Shutes, Adam, Campbell, Robert, Lobbardi, Riadh, Palmer, Michael, Kim, Joseph, Miller, Stephen, Dorsch, Marion, Lengauer, Christoph, Guzi, Timothy, Kadambi, Vivek, Garner, Andrew, Hoeflich, Klaus P

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Abstract B151: BLU-667 is a potent and highly selective RET inhibitor being developed for RET -driven cancers von Rahal, Rami, Maynard, Michelle, Hu, Wei, Brubaker, Jason, Cao, Qiongfang, Kim, Joseph L., Sheets, Michael P., Wilson, Douglas P., Wilson, Kevin J., DiPietro, Lucian, Fleming, Paul, LaBranche, Timothy P., Wolf, Beni, Guzi, Timothy, Lengauer, Christoph, Evans, Erica K.

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Design, Synthesis, and Evaluation of Orally Active Benzimidazoles and Benzoxazoles as Vascular Endothelial Growth Factor-2 Receptor Tyrosine Kinase Inhibitors von Potashman, Michele H, Bready, James, Coxon, Angela, DeMelfi, Thomas M, DiPietro, Lucian, Doerr, Nicholas, Elbaum, Daniel, Estrada, Juan, Gallant, Paul, Germain, Julie, Gu, Yan, Harmange, Jean-Christophe, Kaufman, Stephen A, Kendall, Rick, Kim, Joseph L, Kumar, Gondi N, Long, Alexander M, Neervannan, Seshadri, Patel, Vinod F, Polverino, Anthony, Rose, Paul, van der Plas, Simon, Whittington, Douglas, Zanon, Roger, Zhao, Huilin

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Abstract LB-324: First isoform selective inhibitor of FGFR4 for the treatment of genomically defined patients with hepatocellular carcinoma von Hagel, Margit, Miduturu, Chandra, Sheets, Mike, Weng, Weifan, Rubin, Nooreen, Bifulco, Neil, DiPietro, Lucian, Kim, Joseph, Brooijmans, Natasja, Stransky, Nicolas, Winter, Christopher, Lengauer, Christoph, Guzi, Timothy

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Abstract 2641: The development of potent, selective RET inhibitors that target both wild-type RET and prospectively identified resistance mutations to multi-kinase inhibitors von Rahal, Rami, Evans, Erica K., Hu, Wei, Maynard, Michelle, Fleming, Paul, DiPietro, Lucian, Kim, Joseph L., Sheets, Michael P., Wilson, Doug P., Wilson, Kevin J., Stransky, Nicolas, Brubaker, Jason D., Guzi, Timothy, Kohl, Nancy E., Lengauer, Christoph

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A precision therapy against cancers driven by KIT/PDGFRA mutations von Evans, Erica K, Gardino, Alexandra K, Kim, Joseph L, Hodous, Brian L, Shutes, Adam, Davis, Alison, Zhu, Xing Julia, Schmidt-Kittler, Oleg, Wilson, Doug, Wilson, Kevin, DiPietro, Lucian, Zhang, Yulian, Brooijmans, Natasja, LaBranche, Timothy P, Wozniak, Agnieszka, Gebreyohannes, Yemarshet Kelemework, Schöffski, Patrick, Heinrich, Michael C, DeAngelo, Daniel J, Miller, Stephen, Wolf, Beni, Kohl, Nancy, Guzi, Timothy, Lydon, Nicholas, Boral, Andy, Lengauer, Christoph

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Identification of Potent and Selective Amidobipyridyl Inhibitors of Protein Kinase D von Meredith, Erik L, Beattie, Kimberly, Burgis, Robin, Capparelli, Michael, Chapo, Joseph, DiPietro, Lucian, Gamber, Gabriel, Enyedy, Istvan, Hood, David B, Hosagrahara, Vinayak, Jewell, Charles, Koch, Keith A, Lee, Wendy, Lemon, Douglas D, McKinsey, Timothy A, Miranda, Karl, Pagratis, Nikos, Phan, Dillon, Plato, Craig, Rao, Chang, Rozhitskaya, Olga, Soldermann, Nicolas, Springer, Clayton, van Eis, Maurice, Vega, Richard B, Yan, Wanlin, Zhu, Qingming, Monovich, Lauren G

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Naphthamides as Novel and Potent Vascular Endothelial Growth Factor Receptor Tyrosine Kinase Inhibitors: Design, Synthesis, and Evaluation von Harmange, Jean-Christophe, Weiss, Matthew M, Germain, Julie, Polverino, Anthony J, Borg, George, Bready, James, Chen, Danlin, Choquette, Deborah, Coxon, Angela, DeMelfi, Tom, DiPietro, Lucian, Doerr, Nicholas, Estrada, Juan, Flynn, Julie, Graceffa, Russell F, Harriman, Shawn P, Kaufman, Stephen, La, Daniel S, Long, Alexander, Martin, Matthew W, Neervannan, Sesha, Patel, Vinod F, Potashman, Michele, Regal, Kelly, Roveto, Phillip M, Schrag, Michael L, Starnes, Charlie, Tasker, Andrew, Teffera, Yohannes, Wang, Ling, White, Ryan D, Whittington, Douglas A, Zanon, Roger

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INHIBITORS OF RET von BRUBAKER, Jason, WILSON, Kevin, WILSON, Douglas, KIM, Joseph, DIPIETRO, Lucian

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INHIBITORS OF RET von BRUBAKER, Jason, WILSON, Kevin, WILSON, Douglas, KIM, Joseph, DIPIETRO, Lucian

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INHIBITORS OF RET von BRUBAKER, Jason, WILSON, Kevin, WILSON, Douglas, KIM, Joseph, DIPIETRO, Lucian

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