In this review, the author summarizes the potential targeting strategies underlying tyrosine kinase inhibitors, mTOR inhibitors, interleukins, CSC marker inhibitors, bone morphogenetic protein-2 (BMP-2), antibody drug conjugates (ADCs), and nanomedicine that can target renal cancer cells and renal CSCs to treat RCC more efficiently. Here, BMP2 is linked to renal cell carcinoma.