Literature DB >> 33185101

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

Jianyong Chen1,2, Yunlong Zhou2, Xuyuan Dong1, Liu Liu1, Longchuan Bai1, Donna McEachern1, Sally Przybranowski1, Chao-Yie Yang1, Jeanne Stuckey3, Xiaoqin Li4, Bo Wen4, Ting Zhao4, Siwei Sun4, Duxin Sun4, Lingling Jiao2, Yu Jing2, Ming Guo2, Dajun Yang2, Shaomeng Wang1.   

Abstract

We report herein the discovery of a class of potent small-molecule inhibitors of anaplastic lymphoma kinase (ALK) containing a fused indoloquinoline scaffold. The most promising compound CJ-2360 has an IC50 value of 2.2 nM against wild-type ALK and low-nanomolar potency against several clinically reported ALK mutants. This compound is capable of achieving complete tumor regression in the ALK-positive KARPAS-299 xenograft model with oral administration in mice. CJ-2360 represents a promising ALK inhibitor for advanced preclinical development.

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Year:  2020        PMID： 33185101      PMCID： PMC8855370          DOI： 10.1021/acs.jmedchem.0c01550

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  35 in total

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2.  Development and validation of a genetic algorithm for flexible docking.

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5.  ALK, the chromosome 2 gene locus altered by the t(2;5) in non-Hodgkin's lymphoma, encodes a novel neural receptor tyrosine kinase that is highly related to leukocyte tyrosine kinase (LTK)

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Journal:  Oncogene       Date:  1997-05-08       Impact factor: 9.867

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Journal:  Cancer Res       Date:  2012-05-08       Impact factor: 12.701

10.  First-in-human, open-label dose-escalation and dose-expansion study of the safety, pharmacokinetics, and antitumor effects of an oral ALK inhibitor ASP3026 in patients with advanced solid tumors.

Authors:  Tianhong Li; Patricia LoRusso; Michael L Maitland; Sai-Hong Ignatius Ou; Erkut Bahceci; Howard A Ball; Jung Wook Park; Geoffrey Yuen; Anthony Tolcher
Journal:  J Hematol Oncol       Date:  2016-03-10       Impact factor: 17.388
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2.  Deciphering the Mechanism of Gilteritinib Overcoming Lorlatinib Resistance to the Double Mutant I1171N/F1174I in Anaplastic Lymphoma Kinase.

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  2 in total

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