Discovery and efficacy study of an ALK inhibitor AMX6001 in anaplastic large cell lymphoma Karpas299 mice models
Year: 2024
Type: article
Abstract: Anaplastic lymphoma kinase (ALK) is an attractive therapeutic target for the treatment of anaplastic large cell lymphoma (ALCL). We identified novel deuterated 2,4-diarylamino pyrimidine compounds as potent ALK inhibitors . The compound 9 ( AMX6001 ) showed better in vitro activity against ALK and NPM-ALK kinase and significantly inhibited proliferation of Karpas299 and SU-DHL-1 cell lines. In vivo efficacy of compound 9 was better than reference standard ceritinib in ALCL Karpas299 mice models. Daily oral treatment of compound 9 (25 mg/kg) induced tumor suppression TGI up to 95.8 % in ALCL models.
Authors: Debasis Das, Lingzhi Xie, Dandan Qiao, Yuxi Cao, Jianhe Jia, Yong Li, Jian Hong
Language: English
Subfield: Pulmonary and Respiratory Medicine
Field: Medicine
Domain: Health Sciences
Open Access status: gold
Estimated APC paid: $1,500
Funder: China Pharmaceutical University
OpenAlex ID: W4402037413