Metastasis　currently　remains　the　predominant　cause　of　breast　carcinoma　treatment　failure.　The　effective　targeting　of　metastasis-related-pathways　in　cancer　holds　promise　for　a　new　generation　of　therapeutics.　In　this　study,　we　developed　an　novel　Asp-UA　conjugate,　which　was　composed　of　classical　＂old　drug＂　aspirin　and　low　toxicity　natural　product　ursolic　acid　for　targeting　breast　cancer　metastasis.　Our　results　showed　that　Asp-UA　could　attenuate　the　adhesion,　migration　and　invasion　of　breast　cancer　MCF-7　and　MDA-MB-231　cells　in　a　more　safe　and　effective　manner　in　vitro.　Molecular　and　cellular　study　demonstrated　that　Asp-UA　significantly　downregulated　the　expression　of　cell　adhesion　and　invasion　molecules　including　integrin　a6β1,　CD44,　MMP-2,　MMP-9,　COX-2,　EGFR　and　ERK　proteins,　and　up-regulated　the　epithelial　markers　＂E-cadherin＂　and　＂β-catenin＂,　and　PTEN　proteins.　Furthermore,　Asp-UA　(80　mg/kg)　reduced　lung　metastasis　in　a　4T1　murine　breast　cancer　metastasis　model　more　efficiently,　which　was　associated　with　a　decrease　in　the　expression　of　CD44.　More　importantly,　we　did　not　detect　side　effects　with　Asp-UA　in　mice　such　as　weight　loss　and　main　viscera　tissues　toxicity.　Overall,　our　research　suggested　that　codrug　Asp-UA　possessed　potential　metastasis　chemoprevention　abilities　via　influencing　EMT　and　EGFR-mediated　pathways　and　could　be　a　more　promising　drug　candidate　for　the　prevention　and/or　treatment　of　breast　cancer　metastasis.