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Abstract LB194: Discovery and characterization of a mutant selective PI3Kα^H1047Xinhibitor with a best-in-class profile

Leonard Buckbinder, David J. St. Jean, Trang Tieu, Weixue Wang, Gregory Kryukov, Philip Jonsson, Jacob Alltucker, Samantha Manimala, Brendon Ladd, Angel Guzman-Perez, Darrin Stuart

Cancer Res (2022) 82 (12_Supplement): LB194.

DOI: https://doi.org/10.1158/1538-7445.AM2022-LB194

Published: 15 June 2022

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Journal Articles

Abstract LB-114: RAF inhibitor LXH254 effectively inhibits B-and-CRAF, but not ARAF

Kelli-Ann Monaco, Scott Delach, Paul Fordjour, Salonee Parikh, Yun Feng, Mariela Jaskelioff, Darrin Stuart, Giordano Caponigro

Cancer Res (2019) 79 (13_Supplement): LB-114.

DOI: https://doi.org/10.1158/1538-7445.AM2019-LB-114

Published: 01 July 2019

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Journal Articles

Abstract 4769: Gene expression profiling of response to short- and long-term treatment of LSZ102 in MCF7 cells

Choi Lai Tiong Yip, Joshua Korn, David Ruddy, Daniel Rakiec, Darrin Stuart, Alex Gaither

Cancer Res (2019) 79 (13_Supplement): 4769.

DOI: https://doi.org/10.1158/1538-7445.AM2019-4769

Published: 01 July 2019

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Journal Articles

Abstract 2155: Modeling therapeutic response in BRAF V600-mutant melanoma using patient-derived xenografts

Tianshu Feng, Javad Golji, Ailing Li, Xiamei Zhang, David Ruddy, Darrin Stuart, Matthew Meyer

Cancer Res (2018) 78 (13_Supplement): 2155.

DOI: https://doi.org/10.1158/1538-7445.AM2018-2155

Published: 01 July 2018

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Journal Articles

Abstract 395: Activation mechanisms of cancer associated MEK1 mutants

Yijun Gao, Matthew T. Chang, Daniel McKay, Rona D. Yaeger, Merna Torres, Keven Muniz, Drosten Matthias, Omar I. Abdel-Wahab, Mariano Barbacid, Giordano Caponigro, Darrin Stuart, David Solit, Barry S. Taylor, Zhan Yao, Neal Rosen

Cancer Res (2017) 77 (13_Supplement): 395.

DOI: https://doi.org/10.1158/1538-7445.AM2017-395

Published: 01 July 2017

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Journal Articles

Abstract 330: Development of a highly selective B/CRAF kinase inhibitor that exhibits antitumor activities in RAS and BRAF mutant tumors with minimal paradoxical activation

Cancer Res (2016) 76 (14_Supplement): 330.

DOI: https://doi.org/10.1158/1538-7445.AM2016-330

Published: 15 July 2016

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Journal Articles

Abstract 1610: MAPK inhibitor resistance leads to ligand-independent Ephrin A2 receptor signaling and the formation of new melanoma metastases

Kim H. T. Paraiso, Meghna Das Thakur, Jobin K. John, Bin Fang, John M. Koomen, Inna V. Fedorenko, Hensin Tsao, Keith T. Flaherty, Jane L. Messina, Elena M. Pasquale, Alejandro Villagra, John M. Kirkwood, Friedegund Meier, Sarah Sloot, Geoffrey T. Gibney, Darrin Stuart, Hussein Tawbi, Keiran S.M. Smalley

Cancer Res (2014) 74 (19_Supplement): 1610.

DOI: https://doi.org/10.1158/1538-7445.AM2014-1610

Published: 01 October 2014

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Journal Articles

Abstract LB-121: Dissecting MAPK pathway in BRAF^mut melanoma: Intricacies of ERK1 and ERK2

Tatiana Zavorotinskaya, Upasana Mehra, Yumin Dai, Michel Faure, Ken Crawford, Karen Yu, Jan Marie Cheng, Xiaolei Ma, Jan Xuan, Kelly Yan, Mohammad Hekmat-Nejad, Hanne Merritt, Darrin Stuart, Charles Voliva

Cancer Res (2014) 74 (19_Supplement): LB-121.

DOI: https://doi.org/10.1158/1538-7445.AM2014-LB-121

Published: 01 October 2014

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Journal Articles

Vemurafenib Cooperates with HPV to Promote Initiation of Cutaneous Tumors

Matthew Holderfield, Edward Lorenzana, Ben Weisburd, Lisa Lomovasky, Lise Boussemart, Ludovic Lacroix, Gorana Tomasic, Michel Favre, Stephan Vagner, Caroline Robert, Majid Ghoddusi, Dylan Daniel, Nancy Pryer, Frank McCormick, Darrin Stuart

Cancer Res (2014) 74 (8): 2238–2245.

DOI: https://doi.org/10.1158/0008-5472.CAN-13-1065-T

Published: 15 April 2014

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Includes: Supplementary data

Journal Articles

Abstract LB-54: Identification of a RAF inhibitory auto-phosphorylation site.

Matthew Holderfield, Hanne Merritt, Julie Lin, Zenhai Gao, Darrin Stuart, Frank McCormick

Cancer Res (2013) 73 (8_Supplement): LB-54.

DOI: https://doi.org/10.1158/1538-7445.AM2013-LB-54

Published: 15 April 2013

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Journal Articles

Abstract LB-61: Vemurafenib promotes RAS wild-type tumor formation in a mouse model of HPV-driven cutaneous squamous cell carcinoma.

Matthew Holderfield, Edward Lorenzana, Ben Weisburd, Lisa Lomovasky, Majid Ghoddusi, Dylan Daniel, Nancy Pryer, Frank McCormick, Darrin Stuart

Cancer Res (2013) 73 (8_Supplement): LB-61.

DOI: https://doi.org/10.1158/1538-7445.AM2013-LB-61

Published: 15 April 2013

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Journal Articles

Abstract SY17-03: Targeting BRAF and PI3′-kinase signaling for therapy of melanoma.

Martin McMahon, Meghna Das Thakur, Victoria Marsh, Jillian Silva, Allison Landman, Marian Deuker, Fernando Salangsang, Nancy Pryer, Wayne Phillips, Mitchell Levesque, Reinhard Dummer, Marcus Bosenberg, William R. Sellers, Darrin Stuart

Cancer Res (2013) 73 (8_Supplement): SY17-03.

DOI: https://doi.org/10.1158/1538-7445.AM2013-SY17-03

Published: 15 April 2013

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Journal Articles

Abstract LB-144: Modeling vemurafenib resistance in melanoma reveals a strategy to forestall drug resistance.

Meghna Das Thakur, Rosalie Fisher, Fernando Salangsang, Allison Landman, William Sellers, Nancy Pryer, Mitchell Paul Levesque, Reinhard Dummer, Martin Gore, James Larkin, Martin McMahon, Darrin Stuart

Cancer Res (2013) 73 (8_Supplement): LB-144.

DOI: https://doi.org/10.1158/1538-7445.AM2013-LB-144

Published: 15 April 2013

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Journal Articles

Abstract 5592: Modeling the evolution of resistance to RAF inhibitors in clinically relevant melanoma models

Meghna Das Thakur, Fernando Salangsang, Nancy Pryer, Darrin Stuart, Martin McMahon

Cancer Res (2012) 72 (8_Supplement): 5592.

DOI: https://doi.org/10.1158/1538-7445.AM2012-5592

Published: 15 April 2012

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Journal Articles

Abstract 20: Raf kinase inhibitors can induce Raf dimerization, downstream signaling, and cell growth

Tobi Nagel, Kevin Shoemaker, Nanxin Li, Marco Wallroth, Hanne Merritt, John Chan, Susan Kaufman, Brent Appleton, Yongjin Xu, Matthew Holderfield, Daniel Poon, John Tellew, Darrin Stuart

Cancer Res (2010) 70 (8_Supplement): 20.

DOI: https://doi.org/10.1158/1538-7445.AM10-20

Published: 15 April 2010

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Journal Articles

Abstract 1802: Correlating flow-cytometric and ¹⁹F-NMR changes in fluorodeoxyglucose signal in response to the Raf-inhibitor RAF265

Andrzej Dzik-Jurasz, Melissa Lin, Kathleen Dohoney, Jason McCormick, Mary Ising, Darrin Stuart, Diana Jespersen

Cancer Res (2010) 70 (8_Supplement): 1802.

DOI: https://doi.org/10.1158/1538-7445.AM10-1802

Published: 15 April 2010

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Journal Articles

RAF265 is a potent Raf kinase inhibitor with selective anti-proliferative activity in vitro and in vivo

Darrin Stuart, Kimberly Aardalen, Eleni Venetsanakos, Tobi Nagel, Marco Wallroth, David Batt, Savithri Ramurthy, Daniel Poon, Michel Faure, Edward Lorenzana, Fernando Salangsang, Jeff Dove, Evelyn Garrett, Mina Aikawa, Angelo Kaplan, Payman Amiri, Paul Renhowe

Cancer Res (2008) 68 (9_Supplement): 4876.

Published: 01 May 2008

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Journal Articles

The melanoma inhibitory activity (MIA) protein is an early indicator for therapeutic response in preclinical melanoma models

Nguyen Tan, Eleni Venetsanakos, Kimberly Aardalen, Darrin Stuart, Debbie Swinarski, Katherine Rendahl, Dirk Mendel, Bahija Jallal, Carla Heise, Michel Faure

Cancer Res (2007) 67 (9_Supplement): 5464.

Published: 01 May 2007

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Journal Articles

CHIR-265, a novel inhibitor that targets B-Raf and VEGFR, shows efficacy in a broad range of preclinical models

Eleni Venetsanakos, Darrin Stuart, Nguyen Tan, Helen Ye, Fernando Salangsang, Kimberley Aardalen, Michel Faure, Carla Heise, Dirk Mendel, Bahija Jallal

Cancer Res (2006) 66 (8_Supplement): 1140.

Published: 15 April 2006

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NARROW

Abstract LB194: Discovery and characterization of a mutant selective PI3Kα^H1047Xinhibitor with a best-in-class profile

Abstract LB-114: RAF inhibitor LXH254 effectively inhibits B-and-CRAF, but not ARAF

Abstract 4769: Gene expression profiling of response to short- and long-term treatment of LSZ102 in MCF7 cells

Abstract 2155: Modeling therapeutic response in BRAF V600-mutant melanoma using patient-derived xenografts

Abstract 395: Activation mechanisms of cancer associated MEK1 mutants

Abstract 330: Development of a highly selective B/CRAF kinase inhibitor that exhibits antitumor activities in RAS and BRAF mutant tumors with minimal paradoxical activation

Abstract 1610: MAPK inhibitor resistance leads to ligand-independent Ephrin A2 receptor signaling and the formation of new melanoma metastases

Abstract LB-121: Dissecting MAPK pathway in BRAF^mut melanoma: Intricacies of ERK1 and ERK2

Vemurafenib Cooperates with HPV to Promote Initiation of Cutaneous Tumors

Abstract LB-54: Identification of a RAF inhibitory auto-phosphorylation site.

Abstract LB-61: Vemurafenib promotes RAS wild-type tumor formation in a mouse model of HPV-driven cutaneous squamous cell carcinoma.

Abstract SY17-03: Targeting BRAF and PI3′-kinase signaling for therapy of melanoma.

Abstract LB-144: Modeling vemurafenib resistance in melanoma reveals a strategy to forestall drug resistance.

Abstract 5592: Modeling the evolution of resistance to RAF inhibitors in clinically relevant melanoma models

Abstract 20: Raf kinase inhibitors can induce Raf dimerization, downstream signaling, and cell growth

Abstract 1802: Correlating flow-cytometric and ¹⁹F-NMR changes in fluorodeoxyglucose signal in response to the Raf-inhibitor RAF265

RAF265 is a potent Raf kinase inhibitor with selective anti-proliferative activity in vitro and in vivo

The melanoma inhibitory activity (MIA) protein is an early indicator for therapeutic response in preclinical melanoma models

CHIR-265, a novel inhibitor that targets B-Raf and VEGFR, shows efficacy in a broad range of preclinical models

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