Discovery of CJ-2360 as a Potent and Orally Active Inhibitor of Anaplastic Lymphoma Kinase Capable of Achieving Complete Tumor Regression

Journal of Medicinal Chemistry ◽

10.1021/acs.jmedchem.0c01550 ◽

2020 ◽

Vol 63 (22) ◽

pp. 13994-14016

Author(s):

Jianyong Chen ◽

Yunlong Zhou ◽

Xuyuan Dong ◽

Liu Liu ◽

Longchuan Bai ◽

...

Keyword(s):

Anaplastic Lymphoma Kinase ◽

Tumor Regression ◽

Active Inhibitor ◽

Complete Tumor Regression ◽

Anaplastic Lymphoma ◽

Orally Active ◽

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

Journal of Medicinal Chemistry ◽

10.1021/acs.jmedchem.6b00306 ◽

2016 ◽

Vol 59 (10) ◽

pp. 4948-4964 ◽

Author(s):

Wei-Sheng Huang ◽

Shuangying Liu ◽

Dong Zou ◽

Mathew Thomas ◽

Yihan Wang ◽

...

Keyword(s):

Phosphine Oxide ◽

Anaplastic Lymphoma Kinase ◽

Active Inhibitor ◽

Anaplastic Lymphoma ◽

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Structure-based discovery of a highly potent and orally active small-molecule inhibitor of embryonic ectoderm development (EED) capable of achieving complete tumor regression

10.1021/scimeetings.0c02817 ◽

2020 ◽

Author(s):

Rohan Kalyan Rej

Keyword(s):

Small Molecule ◽

Tumor Regression ◽

Small Molecule Inhibitor ◽

Complete Tumor Regression ◽

Molecule Inhibitor ◽

Embryonic Ectoderm Development ◽

Orally Active ◽

Embryonic Ectoderm ◽

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Structure-based discovery of a highly potent and orally active small-molecule inhibitor of embryonic ectoderm development (EED) capable of achieving complete tumor regression

10.1021/scimeetings.0c02819 ◽

2020 ◽

Author(s):

Rohan Kalyan Rej

Keyword(s):

Small Molecule ◽

Tumor Regression ◽

Small Molecule Inhibitor ◽

Complete Tumor Regression ◽

Molecule Inhibitor ◽

Embryonic Ectoderm Development ◽

Orally Active ◽

Embryonic Ectoderm ◽

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

10.1158/1538-7445.am2015-2827 ◽

2015 ◽

Author(s):

Wei-Sheng Huang ◽

Feng Li ◽

Lisi Cai ◽

Yongjin Xu ◽

Sen Zhang ◽

...

Keyword(s):

Anaplastic Lymphoma Kinase ◽

Active Inhibitor ◽

Anaplastic Lymphoma ◽

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

10.1158/1538-7445.am10-3623 ◽

2010 ◽

Author(s):

Victor M. Rivera ◽

Rana Anjum ◽

Frank Wang ◽

Sen Zhang ◽

Jeffrey Keats ◽

...

Keyword(s):

Anaplastic Lymphoma Kinase ◽

Active Inhibitor ◽

Anaplastic Lymphoma ◽

Pharmacodynamic Analysis ◽

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Abstract 3574: Identification and preclinical characterization of CEP-28122, a highly potent and selective orally active inhibitor of anaplastic lymphoma kinase, in lymphoma and non-small cell lung cancer models

10.1158/1538-7445.am2011-3574 ◽

2011 ◽

Author(s):

Mangeng Cheng ◽

Matthew R. Quail ◽

Diane E. Gingrich ◽

Gregory R. Ott ◽

Lihui Lu ◽

...

Keyword(s):

Lung Cancer ◽

Small Cell Lung Cancer ◽

Anaplastic Lymphoma Kinase ◽

Small Cell Lung ◽

Active Inhibitor ◽

Anaplastic Lymphoma ◽

Cancer Models ◽

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CEP-28122, a Highly Potent and Selective Orally Active Inhibitor of Anaplastic Lymphoma Kinase with Antitumor Activity in Experimental Models of Human Cancers

Molecular Cancer Therapeutics ◽

10.1158/1535-7163.mct-11-0776 ◽

2011 ◽

Vol 11 (3) ◽

pp. 670-679 ◽

Author(s):

Mangeng Cheng ◽

Matthew R. Quail ◽

Diane E. Gingrich ◽

Gregory R. Ott ◽

Lihui Lu ◽

...

Keyword(s):

Antitumor Activity ◽

Anaplastic Lymphoma Kinase ◽

Experimental Models ◽

Active Inhibitor ◽

Anaplastic Lymphoma ◽

Human Cancers ◽

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Faculty Opinions recommendation of Structure-based discovery of BM-957 as a potent small-molecule inhibitor of Bcl-2 and Bcl-xL capable of achieving complete tumor regression.

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature ◽

10.3410/f.717959626.793462957 ◽

2012 ◽

Author(s):

Mark Searcey

Keyword(s):

Small Molecule ◽

Tumor Regression ◽

Small Molecule Inhibitor ◽

Complete Tumor Regression ◽

Molecule Inhibitor ◽

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IL-12/PULSE IL-2 INDUCES ENDOTHELIAL INJURY, INHIBITS TUMOR NEOVASCULARIZATION, AND INDUCES COMPLETE TUMOR REGRESSION VIA MECHANISMS DEPENDENT ON CD8 T CELLS AND FAS-L

Journal of Immunotherapy ◽

10.1097/00002371-199909000-00074 ◽

1999 ◽

Vol 22 (5) ◽

pp. 470

Author(s):

J M Wigginton ◽

J W Park ◽

T C Back ◽

L Gieselhart ◽

T A Wiltrout ◽

...

Keyword(s):

T Cells ◽

Cd8 T Cells ◽

Tumor Regression ◽

Endothelial Injury ◽

Complete Tumor Regression ◽

Tumor Neovascularization ◽

Fas L ◽

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Abstract B14: Hsp90-inhibitor drug conjugate STA-12-8666 demonstrates complete tumor regression in preclinical models of pediatric sarcoma

10.1158/1538-7445.pedca15-b14 ◽

2016 ◽

Author(s):

Christine M. Heske ◽

Arnulfo Mendoza ◽

Choh Yeung ◽

David A. Proia ◽

Len Neckers ◽

...

Keyword(s):

Tumor Regression ◽

Hsp90 Inhibitor ◽

Preclinical Models ◽

Complete Tumor Regression ◽

Drug Conjugate ◽

Pediatric Sarcoma ◽

Inhibitor Drug ◽

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