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RNA\u2010Seq, luciferase assays, western blot and immunofluorescence assays were conducted to detect the impact of RDp002 on STAT3 signalling. CCK\u20108, cell cycle, apoptosis assays and transwell were utilised to evaluate the anti\u2010tumour activity of RDp002 <jats:italic>in vitro<\/jats:italic>. Xenograft models were used to assess the effectiveness of RDp002 <jats:italic>in vivo<\/jats:italic>. Various inhibitors were utilised to investigate how RDp002 causes tumour cell death. The human ether\u2010\u00e0\u2010go\u2010go\u2010related gene (hERG\/K<jats:sub>v<\/jats:sub>11.1) assays, blood biochemistry and acute toxicity experiments were conducted to explore the toxicity of RDp002.<\/jats:p><\/jats:sec><jats:sec><jats:title>Key results<\/jats:title><jats:p>RDp002 exhibited had strong affinity for STAT3 and impaired the phosphorylation of STAT3 at tyrosine 705 and serine 727 residues. RDp002 suppressed the proliferation, survival, migration, growth and metastasis of TNBC and MM cells. RDp002 inhibited tumour cell viability primarily via lysosome\u2010dependent cell death, which can be weakened by overexpression of STAT3. The toxicity of RDp002 <jats:italic>in vivo<\/jats:italic> was minimal based on results from hERG assays, blood biochemistry analysis and acute toxicity tests.<\/jats:p><\/jats:sec><jats:sec><jats:title>Conclusion and implications<\/jats:title><jats:p>RDp002 is a novel STAT3 inhibitor that exerts potent anti\u2010tumour effects mainly by inducing lysosome\u2010dependent cell death. RDp002 represents a promising therapeutic lead for TNBC and MM.<\/jats:p><\/jats:sec>","DOI":"10.1111\/bph.70071","type":"journal-article","created":{"date-parts":[[2025,5,13]],"date-time":"2025-05-13T03:28:17Z","timestamp":1747106897000},"page":"4041-4057","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":4,"title":["A novel synthesised STAT3 inhibitor exerts potent anti\u2010tumour activity by inducing lysosome\u2010dependent cell death"],"prefix":"10.1111","volume":"182","author":[{"given":"Marvin Xuejun","family":"Xu","sequence":"first","affiliation":[{"name":"Henan Key Laboratory of Small Molecular Anti\u2010cancer Novel Drug, Henan International Joint Lab of Target Anti\u2010cancer Drug, Henan Engineering Research Center of Target Anti\u2010cancer Drug Henan Ruida Bio\u2010tech Medicine Co. 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