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Background Signal transducer and activator of transcription 3 (STAT3) is usually constitutively activated in a variety of malignancies. It directly contributes to tumorigenesis, invasion, and metastasis. The surgical treatment of breast cancer has made no breakthroughs in terms of treatment effect, in spite of its long history. Current biotherapies bring a note of optimism to breast cancer treatment. To explore the possibility of a siRNA targeted STAT3 blocking treatment for over-activated tumor cells, we evaluated the efficacy of a STAT3 siRNA on human breast cancer cells in vitro and in vivo.Methods Three MCF-7 human breast cancer cell lines were tested: control MCF-7 cells, non-specific siRNA transfected MCF-7 cells and STAT3 siRNA transfected MCF-7 cells. Expression of STAT3 in MCF-7 cells was inhibited by RNA interference (RNAi). The STAT3 mRNA and protein levels were detected by semi-quantity RT-PCR and Western blotting. Cell proliferation and apoptosis were determined by MTT method and flow cytometry. The three groups of MCF-7 cells mentioned above were transplanted subcutanuously into nude mice and their tumorgenic ability observed. The STAT3 mRNA and protein levels of the samples from tumors in different groups were determined by semi-quantity RT-PCR and Western blotting and compared.Results In STAT3 siRNA transfected MCF-7 cells, the expressions (STAT3/p-actin) of STAT3 mRNA (0.327±0.020) and protein (0.153±0.006) were significantly lower than that in control MCF-7 cells (mRNA 1.093±0.018, protein 1.374±0.022) and non-specific siRNA transfected MCF-7 cells (mRNA 1.035±0.050, protein 1.320±0.033) (P