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Article

Discovery of SILA-123 as a Highly Potent FLT3 Inhibitor for the Treatment of Acute Myeloid Leukemia with Various FLT3 Mutations.

Journal of medicinal chemistry - 26 Dec 2024

Wei Tian-Hua, Wang Zi-Xuan, Lu Meng-Yi, Xu Yu-Jing, Yang Jin, Ni Xing-Feng, Cheng Yang, Zhang Meng-Yuan, Liu Jia-Chuan, Li Qing-Qing, Cai Jiao, Chen Zi-Jun, Kang Ji-Bo, Li Nan, Dai Wei-Chen, Ding Ning, Yu Yan-Cheng, Leng Xue-Jiao, Xue Xin, Wang Xiao-Long, Sun Shan-Liang, Yang Ye, Li Nian-Guang, Shi Zhi-Hao

Abstract excerpt

The FLT3-ITD (internal tandem duplication) mutant has been a promising target for acute myeloid leukemia (AML) drug discovery but is now facing the challenge of resistance due to point mutations. Herein, we have discovered a type II FLT3 inhibitor, SILA-123. This inhibitor has shown highly potent inhibitory effects against FLT3-WT (IC50 = 2.1 nM) and FLT3-ITD (IC50 = 1.0 nM), tumor cells with the FLT3-ITD mutant...

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Identifiers

PMID: 39258312
DOI: 10.1021/acs.jmedchem.4c00529

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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