Biomarker-targeted nanocarrier holds promise for early diagnosis and effective therapy of cancer. This work successfully designs and evaluates GPC1-targeted, gemcitabine (GEM)-loaded multifunctional gold nanocarrier for near-infrared fluorescence (NIRF)/MRI and targeted chemotherapy against pancreatic cancer and . Blood biochemical and histological analyses show that the toxicity of GPC1-GEM-nanoparticles (NPs) was negligible. Both and studies demonstrate that GPC1-GEM-NPs can be used as NIRF/MR contrast agent for pancreatic cancer detection. Treatment of xenografted mice with GPC1-GEM-NPs shows a higher tumor inhibitory effect compared with controls. This novel theranostic nanoplatform provides early diagnostic and effective therapeutic potential for pancreatic cancer.