Scott D. Wardwell

发表

SAR of Carbon‐Linked, 2‐Substituted Purines: Synthesis and Characterization of AP23451 as a novel Bone‐Targeted Inhibitor of Src Tyrosine Kinase With In Vivo Anti‐Resorptive Activity

R. Bohacek, L. Xing, B. Boyce, 2008, Chemical biology & drug design.

Pharmacologically regulated in vivo selection in a large animal.

C. von Kalle, A. Gown, T. Clackson, 2002, Blood.

Abstract 1794: AP26113 is a dual ALK/EGFR inhibitor: Characterization against EGFR T790M in cell and mouse models of NSCLC

T. Clackson, R. Anjum, V. Rivera, 2012 .

The Potent ALK Inhibitor Brigatinib (AP26113) Overcomes Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in Preclinical Models

T. Clackson, R. Anjum, V. Rivera, 2016, Clinical Cancer Research.

Potent Antitumor Activity of AP24534, An Orally Active Inhibitor of Bcr-Abl, Flt3 and Other Kinases, in Both in Vitro and in Vivo Models of Acute Myeloid Leukemia (AML)

T. Clackson, L. Berk, V. Rivera, 2008 .

Potent Antitumor Activity of AP24534, an Orally Active Inhibitor of Bcr-Abl Variants Including T315I, in In Vitro and In Vivo Models of Chronic Myeloid Leukemia (CML).

T. Clackson, B. Druker, A. Corbin, 2007 .

Abstract LB-298: AP26113, a potent ALK inhibitor, overcomes mutations in EML4-ALK that confer resistance to PF-02341066 (PF1066)

T. Clackson, R. Anjum, V. Rivera, 2010 .

Abstract #3738: Discovery of potent and selective orally active inhibitors of anaplastic lymphoma kinase (ALK)

T. Clackson, R. Anjum, V. Rivera, 2009 .

Ponatinib Inhibits Polyclonal Drug-Resistant KIT Oncoproteins and Shows Therapeutic Potential in Heavily Pretreated Gastrointestinal Stromal Tumor (GIST) Patients

J. Fletcher, T. Clackson, M. Heinrich, 2014, Clinical Cancer Research.

AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance.

T. Clackson, B. Druker, A. Corbin, 2009, Cancer cell.

Potent Preclinical Activity of Ponatinib in Germinal Center B-Cell-like Diffuse Large B-Cell Lymphoma (GCB-DLBCL) Models

V. Rivera, Youngchul Song, J. Gozgit, 2015 .

1048. Long-Term Regulated Gene Expression in Non-Human Primates Using a Single Non-Recombinogenic AAV Vector

T. Clackson, James M. Wilson, L. Berk, 2004 .

Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including the T315I gatekeeper mutant.

Wei-Sheng Huang, Jan Romero, Shuangying Liu, 2010, Journal of medicinal chemistry.

Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase.

T. Clackson, R. Anjum, V. Rivera, 2016, Journal of medicinal chemistry.

Potent Activity of Ponatinib (AP24534) in Models of FLT3-Driven Acute Myeloid Leukemia and Other Hematologic Malignancies

T. Clackson, B. Druker, J. Tyner, 2011, Molecular Cancer Therapeutics.

Preclinical Development Potent Activity of Ponatinib ( AP 24534 ) in Models of FLT 3-Driven Acute Myeloid Leukemia and Other Hematologic Malignancies

T. Clackson, B. Druker, J. Tyner, 2011 .

Mobocertinib (TAK-788): A Targeted Inhibitor of EGFR Exon 20 Insertion Mutants in Non-Small Cell Lung Cancer.

Kwok-Kin Wong, T. Clackson, A. Gould, 2021, Cancer discovery.

Mice deficient in IL-1β-converting enzyme are defective in production of mature IL-1β and resistant to endotoxic shock

R. Kamen, Ping Li, Subhashish Banerjee, 1995, Cell.

Crizotinib-Resistant Mutants of EML4-ALK Identified Through an Accelerated Mutagenesis Screen

T. Clackson, R. Anjum, V. Rivera, 2011, Chemical biology & drug design.

Antitumor Activity of Ridaforolimus and Potential Cell-Cycle Determinants of Sensitivity in Sarcoma and Endometrial Cancer Models

T. Clackson, V. Rivera, D. Clapham, 2011, Molecular Cancer Therapeutics.

Ridaforolimus (AP23573; MK-8669), a Potent mTOR Inhibitor, Has Broad Antitumor Activity and Can Be Optimally Administered Using Intermittent Dosing Regimens

T. Clackson, L. Berk, V. Rivera, 2011, Molecular Cancer Therapeutics.

Ponatinib (AP24534), a Multitargeted Pan-FGFR Inhibitor with Activity in Multiple FGFR-Amplified or Mutated Cancer Models

T. Clackson, V. Rivera, W. Shakespeare, 2012, Molecular Cancer Therapeutics.

Synergistic activity of the mTOR inhibitor ridaforolimus and the antiandrogen bicalutamide in prostate cancer models

T. Clackson, V. Rivera, Frank Y Wang, 2012, International journal of oncology.

Preclinical Development Ridaforolimus ( AP 23573 ; MK-8669 ) , a Potent mTOR Inhibitor , Has Broad Antitumor Activity and Can Be Optimally Administered Using Intermittent Dosing Regimens

T. Clackson, L. Berk, V. Rivera, 2011 .

Discovery of Mobocertinib, a Potent, Oral Inhibitor of EGFR Exon 20 Insertion Mutations in Non-Small Cell Lung Cancer.

T. Clackson, A. Gould, V. Rivera, 2022, Bioorganic & medicinal chemistry letters.

9-(Arenethenyl)purines as dual Src/Abl kinase inhibitors targeting the inactive conformation: design, synthesis, and biological evaluation.

G. Daley, T. Clackson, M. Azam, 2009, Journal of medicinal chemistry.

Orally Active Inhibitors of the Imatinib Resistant Bcr-Abl Mutant T315I.

T. Clackson, B. Druker, A. Corbin, 2006 .

RET fusions observed in lung and colorectal cancers are sensitive to ponatinib

J. Pritchard, H. Edgren, Tzu-Hsiu Chen, 2018, Oncotarget.

Combined targeting of FGFR2 and mTOR by ponatinib and ridaforolimus results in synergistic antitumor activity in FGFR2 mutant endometrial cancer models

T. Clackson, V. Rivera, M. Wongchenko, 2013, Cancer Chemotherapy and Pharmacology.

Activity in Multiple FGFR-Amplified or Mutated Cancer Models Ponatinib ( AP 24534 ) , a Multitargeted Pan-FGFR Inhibitor with Updated

V. Rivera, W. Shakespeare, N. Narasimhan, 2012 .

Preclinical Development Ponatinib ( AP 24534 ) , aMultitargeted Pan-FGFR Inhibitorwith Activity in Multiple FGFR-Ampli fi ed or Mutated Cancer Models

T. Clackson, V. Rivera, W. Shakespeare, 2012 .

Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.

Wei-Sheng Huang, Jan Romero, Shuangying Liu, 2011, Bioorganic & medicinal chemistry letters.

Novel N9-arenethenyl purines as potent dual Src/Abl tyrosine kinase inhibitors.

T. Clackson, T. Sawyer, W. Shakespeare, 2008, Bioorganic & medicinal chemistry letters.

AP23848 against activation loop mutants of Kit In vitro and in vivo activity of ATP-based kinase inhibitors AP23464 and

B. Druker, M. Heinrich, T. Sawyer, 2013 .

In vitro and in vivo activity of ATP-based kinase inhibitors AP23464 and AP23848 against activation-loop mutants of Kit.

B. Druker, M. Heinrich, A. Corbin, 2005, Blood.

Abstract 781: The potent ALK inhibitor AP26113 can overcome mechanisms of resistance to first- and second-generation ALK TKIs in preclinical models

J. Hodgson, V. Rivera, Scott D. Wardwell, 2015 .

Abstract 1262: BLU-701 is a highly potent, brain-penetrant and WT-sparing next-generation EGFR TKI for the treatment of sensitizing (ex19del, L858R) and C797S resistance mutations in metastatic NSCLC

S. Kazmirski, Ayşegül Özen, K. Hoeflich, 2021, Experimental and Molecular Therapeutics.

Abstract 3623: Efficacy and pharmacodynamic analysis of AP26113, a potent and selective orally active inhibitor of Anaplastic Lymphoma Kinase (ALK)

Juan J. Miret, Wei-Sheng Huang, Shuangying Liu, 2010 .

Abstract 3560: Ponatinib (AP24534), a potent pan-FGFR inhibitor with activity in multiple FGFR-driven cancer models

T. Clackson, V. Rivera, W. Shakespeare, 2011 .

Abstract 2644: AP32788, a potent, selective inhibitor of EGFR and HER2 oncogenic mutants, including exon 20 insertions, in preclinical models

V. Rivera, T. Zhou, M. Greenfield, 2016 .

The value of nucleolar organizer regions in uveal melanoma. The Collaborative Ocular Melanoma Study Group.

D. Albert, D. Marcus, J. B. Minkovitz, 1990, American journal of ophthalmology.

Abstract 2827: Discovery of AP26113, a potent, orally active inhibitor of anaplastic lymphoma kinase and clinically relevant mutants

T. Clackson, V. Rivera, W. Shakespeare, 2015 .