Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib.

doi:10.1021/jm301581y

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Article

Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib.

Journal of medicinal chemistry - 14 Feb 2013

Ren Xiaomei, Pan Xiaofen, Zhang Zhang, Wang Deping, Lu Xiaoyun, Li Yupeng, Wen Donghai, Long Huoyou, Luo Jinfeng, Feng Yubing, Zhuang Xiaoxi, Zhang Fengxiang, Liu Jianqi, Leng Fang, Lang Xingfen, Bai Yang, She Miaoqin, Tu Zhengchao, Pan Jingxuan, Ding Ke

Abstract excerpt

Bcr-Abl(T315I) mutation-induced imatinib resistance remains a major challenge for clinical management of chronic myelogenous leukemia (CML). Herein, we report GZD824 (10a) as a novel orally bioavailable inhibitor against a broad spectrum of Bcr-Abl mutants including T315I. It tightly bound to Bcr-Abl(WT) and Bcr-Abl(T315I) with K(d) values of 0.32 and 0.71 nM, respectively, and strongly inhibited the kinase...

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PMID: 23301703
DOI: 10.1021/jm301581y

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 6 Sept 2026. Manifest publication-graph-cohort-2026-09-06.1.

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