Abstract: Objective: To evaluate the effects of ¹²⁵I-labeled antisense oligonucleotide(¹²⁵I-A-SODNs) targeting Ki-67 gene on the proliferation and apoptosis of human renal carcinoma cell line invitro and in vivo. Methods: Antisense oligonucleotides (ASODNs) was coupled with ¹²⁵I. Human renal carcinoma cell line 786-0 cells and implanted tumor mice were treated with ¹²⁵I-ASODNs. The Ki-67 expression was detected using immunohistochemical technique and Western blot method, respectively.Apoptosis of 786-0 cells was detected by TUNEL assay. Results: The Ki-67 positive expression rateand Ki-67 protein rate were low, but the rate of apoptosis was high. The tumor volume was signifi cantlysmall. Conclusion: Effects of ASODNs targeting Ki67 gene on the proliferation and apoptosis of humanrenal carcinoma cells are augmented when ASODNs coupled with ¹²⁵I.