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Journal Articles

Abstract CT031: A first-in-human, phase 1a/1b, open-label, dose-escalation and expansion study to investigate the safety, pharmacokinetics, and antitumor activity of the RAF dimer inhibitor BGB-3245 in patients with advanced or refractory tumors

Alison M. Schram, Vivek Subbiah, Ryan Sullivan, Rasha Cosman, Jia Liu, Eric I. Sbar, Thuy Hoang, Jiarong Chen, Mark Johnson, Vincent Amoruccio, Todd Shearer, Adeela Kamal, Jocelyn Lewis, Wenlin Shao, Badreddin Edris, Lusong Luo, Jayesh Desai
Journal: Cancer Research
Cancer Res (2023) 83 (8_Supplement): CT031.
https://doi.org/10.1158/1538-7445.AM2023-CT031
Published: 14 April 2023
View article titled, Abstract CT031: A first-in-human, phase 1a/1b, open-label, dose-escalation and expansion study to investigate the safety, pharmacokinetics, and antitumor activity of the RAF dimer inhibitor BGB-3245 in patients with advanced or refractory tumors
Journal Articles

Abstract CT033: Safety, pharmacokinetics, and antitumor activity findings from a phase 1b, open-label, dose-escalation and expansion study investigating RAF dimer inhibitor lifirafenib in combination with MEK inhibitor mirdametinib in patients with advanced or refractory solid tumors

Benjamin Solomon, Bo Gao, Vivek Subbiah, Michael Millward, Lee Rosen, Jayesh Desai, Eric I. Sbar, Neal Collins, Thuy Hoang, Xi Song, Wenlin Shao, Jaspreet Jaggi, Badreddin Edris, Paraneedharan Ramachandran, Lusong Luo, Michael Friedlander
Journal: Cancer Research
Cancer Res (2023) 83 (8_Supplement): CT033.
https://doi.org/10.1158/1538-7445.AM2023-CT033
Published: 14 April 2023
View article titled, Abstract CT033: Safety, pharmacokinetics, and antitumor activity findings from a phase 1b, open-label, dose-escalation and expansion study investigating RAF dimer inhibitor lifirafenib in combination with MEK inhibitor mirdametinib in patients with advanced or refractory solid tumors
Journal Articles

Abstract 1664: Inhibition of arginase in combination with radiation therapy shows increased immune-activation and anti-tumor activity in syngeneic tumor models

Alwin Schuller, Aatman Doshi, Susan Cantin, Matt Griffin, Maryann San Martin, Theresa Proia, Corinne Reimer, Scott Mlynarski, Ray Finlay, Wenlin Shao
Journal: Cancer Research
Cancer Res (2021) 81 (13_Supplement): 1664.
https://doi.org/10.1158/1538-7445.AM2021-1664
Published: 01 July 2021
View article titled, Abstract 1664: Inhibition of arginase in combination with radiation therapy shows increased immune-activation and anti-tumor activity in syngeneic tumor models
Journal Articles

Abstract 6168: Characterization of ATM inhibitor (AZD1390) distribution and pharmacodynamic changes in brain and glioblastoma in preclinical models to inform on mechanism of action

Lenka Oplustil O'Connor, Gregory Hamm, Maria Udriste, Stephanie Ling, Joanne Wilson, Steve Durant, Gareth Hughes, Sabina Cosulich, Wenlin Shao, Martin Pass, Gemma Jones, Andrew Pierce, Richard Goodwin, Mark O'Connor, Carl Barrett, Elizabeth Harrington
Journal: Cancer Research
Cancer Res (2020) 80 (16_Supplement): 6168.
https://doi.org/10.1158/1538-7445.AM2020-6168
Published: 15 August 2020
View article titled, Abstract 6168: Characterization of ATM inhibitor (AZD1390) distribution and pharmacodynamic changes in brain and glioblastoma in preclinical models to inform on mechanism of action
Journal Articles

Abstract CT168: Clinical pharmacology of AZD4635 (A2ARi): Integration of PK data from cancer patients (CP) and healthy volunteer (HV) clinical trials to provide dosing recommendations

Ganesh Moorthy, Gayle Pageau Pouliot, Lorraine Graham, Chris Wilks, Tinnu Sarvotham, Patrick Mitchell, Lindsey Jung, Yan Li, Wenlin Shao, Ganesh Mugundu
Journal: Cancer Research
Cancer Res (2020) 80 (16_Supplement): CT168.
https://doi.org/10.1158/1538-7445.AM2020-CT168
Published: 15 August 2020
View article titled, Abstract CT168: Clinical pharmacology of AZD4635 (A2ARi): Integration of PK data from cancer patients (CP) and healthy volunteer (HV) clinical trials to provide dosing recommendations
Journal Articles

Abstract 4523: Inhibition of arginase in combination with anti-PDL1 leads to increased infiltration and activation of CD8+ T cells, NK cells, and CD103+ dendritic cells in mouse syngeneic tumor models

Alwin Schuller, Aatman Doshi, Susan Cantin, Michael Secinaro, Yanjun Wang, Laura Prickett, Sharon Tentarelli, Eric Gangl, Horma Ghadially, Kristina Ilieva, Theresa Proia, Scott Mlynarski, Ray Finlay, Wenlin Shao
Journal: Cancer Research
Cancer Res (2020) 80 (16_Supplement): 4523.
https://doi.org/10.1158/1538-7445.AM2020-4523
Published: 15 August 2020
View article titled, Abstract 4523: Inhibition of arginase in combination with anti-PDL1 leads to increased infiltration and activation of CD8+ T cells, NK cells, and CD103+ dendritic cells in mouse syngeneic tumor models
Journal Articles

Abstract 2500: Transient CDK9 inhibition with AZD4573 modulates Bfl-1 in preclinical lymphoma models

Scott Boiko, Theresa Proia, Maryann San Martin, Lisa Drew, Wenlin Shao, Justin Cidado
Journal: Cancer Research
Cancer Res (2019) 79 (13_Supplement): 2500.
https://doi.org/10.1158/1538-7445.AM2019-2500
Published: 01 July 2019
View article titled, Abstract 2500: Transient CDK9 inhibition with AZD4573 modulates Bfl-1 in preclinical lymphoma models
Journal Articles

Abstract LB-192: The A2AR antagonist AZD4635 prevents adenosine-mediated immunosuppression of CD103+ dendritic cells

Christine M. Barbon, Alexandra Borodovsky, Yanjun Wang, Laura Prickett, Kris Sachsenmeier, Alwin Schuller, Wenlin Shao, Carl Barrett, Stephen Fawell, Deanna A. Mele
Journal: Cancer Research
Cancer Res (2019) 79 (13_Supplement): LB-192.
https://doi.org/10.1158/1538-7445.AM2019-LB-192
Published: 01 July 2019
View article titled, Abstract LB-192: The A2AR antagonist AZD4635 prevents adenosine-mediated immunosuppression of CD103+ dendritic cells
Journal Articles

Abstract CT026: Evidence of immune activation in the first-in-human Phase Ia dose escalation study of the adenosine 2a receptor antagonist, AZD4635, in patients with advanced solid tumors

Johanna Bendell, Todd Bauer, Manish Patel, Gerald Falchook, Janet L. Karlix, Emerson Lim, Ganesh Mugundu, Patrick D. Mitchell, Gayle P. Pouliot, Ganesh Moorthy, Bolan Linghu, Lara McGrath, Bryony Harrop, Wenlin Shao, Charles G. Drake, Kris Sachsenmeier, Melinda S. Merchant
Journal: Cancer Research
Cancer Res (2019) 79 (13_Supplement): CT026.
https://doi.org/10.1158/1538-7445.AM2019-CT026
Published: 01 July 2019
View article titled, Abstract CT026: Evidence of immune activation in the first-in-human Phase Ia dose escalation study of the adenosine 2a receptor antagonist, AZD4635, in patients with advanced solid tumors
Journal Articles

Abstract DDT01-04: Pharmacological profile and anti-tumor properties of LXH254, a highly selective RAF kinase inhibitor

Darrin D. Stuart, Wenlin Shao, Yuji Mishina, Yun Feng, Giordano Caponigro, Vesselina G. Cooke, Stacey Rivera, Fang Shen, Joshua Korn, Lesley A. Mathews Griner, Giselle Nishiguchi, Benjamin Taft, Lifeng Wan, Sharadha Subramanian, Yan Lou, Lina Setti, Matthew Burger, Victor Tamez, Alice Rico, Robert Aversa, John Tellew, Jacob R. Haling, Valery Polyakov, Amy Lambert, Richard Zang, Ann Van Abbema, Mohamad Hekmat-Nejad, Payman Amiri, Mallika Singh, Nicholas Keen, Michael P. Dillon, Emma Lees, William R. Sellers, Savithri Ramurthy
Journal: Cancer Research
Cancer Res (2018) 78 (13_Supplement): DDT01-04.
https://doi.org/10.1158/1538-7445.AM2018-DDT01-04
Published: 01 July 2018
View article titled, Abstract DDT01-04: Pharmacological profile and anti-tumor properties of LXH254, a highly selective RAF kinase inhibitor
Journal Articles

Abstract 306: A mechanistic rationale for combining acalabrutinib with CDK9 inhibitor, AZD4573, in ABC-DLBCL

Scott Boiko, Theresa Proia, Maryann San Martin, Justin Cidado, Wenlin Shao, Lisa Drew
Journal: Cancer Research
Cancer Res (2018) 78 (13_Supplement): 306.
https://doi.org/10.1158/1538-7445.AM2018-306
Published: 01 July 2018
View article titled, Abstract 306: A mechanistic rationale for combining acalabrutinib with CDK9 inhibitor, AZD4573, in ABC-DLBCL
Journal Articles

Abstract 1650: Discovery of AZD4573, a potent and selective inhibitor of CDK9 that enables transient target engagement for the treatment of hematologic malignancies

Bernard Barlaam, Chris De Savi, Lisa Drew, Andrew D. Ferguson, Douglas Ferguson, Chungang Gu, Janet Hawkins, Alexander W. Hird, Michelle L. Lamb, Nichole O'Connell, Kurt Pike, Theresa Proia, Maryann San Martin, Melissa M. Vasbinder, Jeff Varnes, Jianyan Wang, Wenlin Shao
Journal: Cancer Research
Cancer Res (2018) 78 (13_Supplement): 1650.
https://doi.org/10.1158/1538-7445.AM2018-1650
Published: 01 July 2018
View article titled, Abstract 1650: Discovery of AZD4573, a potent and selective inhibitor of CDK9 that enables transient target engagement for the treatment of hematologic malignancies
Journal Articles

Abstract 297: AZD4573: Mechanistic PKPD model linking CDK9 inhibition to Mcl1 depletion and induction of apoptosis in preclinical AML model

Douglas Ferguson, Theresa Proia, Justin Cidado, Scott Boiko, Maryann San Martin, Steven Criscione, Wenlin Shao, Lisa Drew
Journal: Cancer Research
Cancer Res (2018) 78 (13_Supplement): 297.
https://doi.org/10.1158/1538-7445.AM2018-297
Published: 01 July 2018
View article titled, Abstract 297: AZD4573: Mechanistic PKPD model linking CDK9 inhibition to Mcl1 depletion and induction of apoptosis in preclinical AML model
Journal Articles

Abstract 310: AZD4573, a novel CDK9 inhibitor, rapidly induces cell death in hematological tumor models through depletion of Mcl1

Justin Cidado, Theresa Proia, Scott Boiko, Maryann San Martin, Steven Criscione, Douglas Ferguson, Wenlin Shao, Lisa Drew
Journal: Cancer Research
Cancer Res (2018) 78 (13_Supplement): 310.
https://doi.org/10.1158/1538-7445.AM2018-310
Published: 01 July 2018
View article titled, Abstract 310: AZD4573, a novel CDK9 inhibitor, rapidly induces cell death in hematological tumor models through depletion of Mcl1
Journal Articles

Antitumor Properties of RAF709, a Highly Selective and Potent Inhibitor of RAF Kinase Dimers, in Tumors Driven by Mutant RAS or BRAF

Wenlin Shao, Yuji M. Mishina, Yun Feng, Giordano Caponigro, Vesselina G. Cooke, Stacy Rivera, Yingyun Wang, Fang Shen, Joshua M. Korn, Lesley A. Mathews Griner, Gisele Nishiguchi, Alice Rico, John Tellew, Jacob R. Haling, Robert Aversa, Valery Polyakov, Richard Zang, Mohammad Hekmat-Nejad, Payman Amiri, Mallika Singh, Nicholas Keen, Michael P. Dillon, Emma Lees, Savithri Ramurthy, William R. Sellers, Darrin D. Stuart
Journal: Cancer Research
Cancer Res (2018) 78 (6): 1537–1548.
https://doi.org/10.1158/0008-5472.CAN-17-2033
Published: 14 March 2018
View article titled, Antitumor Properties of RAF709, a Highly Selective and Potent Inhibitor of RAF Kinase Dimers, in Tumors Driven by Mutant RAS or BRAF
Open the PDF for Antitumor Properties of RAF709, a Highly Selective and Potent Inhibitor of RAF Kinase Dimers, in Tumors Driven by Mutant RAS or BRAF in another window
Includes: Supplementary data
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

Wenlin Shao, Yuji Mishina, Yun Feng, Giordano Caponigro, Savithri Ramurthy, Vesselina Cooke, Lesley Griner, Gisele Nishiguchi, Alice Rico, Ben Taft, Matthew Burger, Huw Tanner, Valery Polyakov, Brent Appleton, John Tellew, Richard Zang, Mohammad Hekmat-Nejad, Payman Amiri, Mallika Singh, Darrin Stuart
Journal: Cancer Research
Cancer Res (2016) 76 (14_Supplement): 330.
https://doi.org/10.1158/1538-7445.AM2016-330
Published: 15 July 2016
View article titled, 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
Journal Articles

Abstract LB-107: Inhibiting TNKS sensitizes KRAS mutant cancer cells to MEK inhibitors by suppressing FGFR2 feedback signaling

Wenlin Shao, Marie Schoumacher, Kristen Hurov, Joseph Lehar, Yan Yan-Neale, Yuji Mishina, Dmitriy Sonkin, Joshua Korn, Daisy Flemming, Michael Jones, Brandon Antonakos, Vessilina Cooke, Mark Stump, Nika Danial, William Sellers
Journal: Cancer Research
Cancer Res (2014) 74 (19_Supplement): LB-107.
https://doi.org/10.1158/1538-7445.AM2014-LB-107
Published: 01 October 2014
View article titled, Abstract LB-107: Inhibiting TNKS sensitizes KRAS mutant cancer cells to MEK inhibitors by suppressing FGFR2 feedback signaling
Journal Articles

Inhibiting Tankyrases Sensitizes KRAS-Mutant Cancer Cells to MEK Inhibitors via FGFR2 Feedback Signaling

Marie Schoumacher, Kristen E. Hurov, Joseph Lehár, Yan Yan-Neale, Yuji Mishina, Dmitriy Sonkin, Joshua M. Korn, Daisy Flemming, Michael D. Jones, Brandon Antonakos, Vesselina G. Cooke, Janine Steiger, Jebediah Ledell, Mark D. Stump, William R. Sellers, Nika N. Danial, Wenlin Shao
Journal: Cancer Research
Cancer Res (2014) 74 (12): 3294–3305.
https://doi.org/10.1158/0008-5472.CAN-14-0138-T
Published: 12 June 2014
View article titled, Inhibiting Tankyrases Sensitizes KRAS-Mutant Cancer Cells to MEK Inhibitors via FGFR2 Feedback Signaling
Open the PDF for Inhibiting Tankyrases Sensitizes KRAS-Mutant Cancer Cells to MEK Inhibitors via FGFR2 Feedback Signaling in another window
Includes: Supplementary data
Journal Articles

Abstract LB-34: Investigating novel biological functions of tankyrases in cancer

Marie Schoumacher, Yun Feng, Yuji Mishina, Wenlin Shao
Journal: Cancer Research
Cancer Res (2012) 72 (8_Supplement): LB-34.
https://doi.org/10.1158/1538-7445.AM2012-LB-34
Published: 15 April 2012
View article titled, Abstract LB-34: Investigating novel biological functions of tankyrases in cancer
Journal Articles

Potent anticancer activity of a pan-deacetylase inhibitor panobinostat (LBH589) as a single agent in in vitro and in vivo tumor models

Wenlin Shao, Joseph Growney, Yun Feng, Ping Wang, Yan Yan-Neale, Gregory O'Connor, Paul Kwon, Yung-mae Yao, Stephen Fawell, Peter Atadja
Journal: Cancer Research
Cancer Res (2008) 68 (9_Supplement): 735.
Published: 01 May 2008
View article titled, Potent anticancer activity of a pan-deacetylase inhibitor panobinostat (LBH589) as a single agent in <em>in vitro</em> and <em>in vivo</em> tumor models