In these cell lines with high LRRFIP1/GCF2 expression, the down-regulated of RhoA, and the disrupted actin-filament network were observed, and then the membrane-transporter multidrug resistance protein 1 (MRP1), which facilitates efflux of anti-cancer drugs from cytoplasm, was internalized from membrane to cytoplasm, leading to inefficient efflux and increased accumulation of doxorubicin and vincristine, and subsequent therapeutic effects. This evidence concerns the gene LRRFIP1 and cancer.