间变性淋巴瘤激酶
碱性抑制剂
化学
IC50型
效力
淋巴瘤
酶抑制剂
激酶
癌症研究
体外
药理学
生物化学
内科学
医学
恶性胸腔积液
胸腔积液
作者
Jianyong Chen,Yunlong Zhou,Xuyuan Dong,Liu Liu,Longchuan Bai,Donna McEachern,Sally Przybranowski,Chao‐Yie Yang,Jeanne A. Stuckey,Xiaoqin Li,Bo Wen,Ting C. Zhao,Siwei Sun,Duxin Sun,Lingling Jiao,Yu Jing,Ming‐Lei Guo,Dajun Yang,Shaomeng Wang
标识
DOI:10.1021/acs.jmedchem.0c01550
摘要
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.
科研通智能强力驱动
Strongly Powered by AbleSci AI