Abstract: The present disclosure relates to the fields of nuclear medicine and molecular imaging, and specifically relates to a dual-targeting compound and a preparation method and application thereof. The dual-targeting compound has the following structure shown in Formula (I). The present disclosure also provides a dual-targeting compound capable of being labeled with a radionuclide, and the compound has the following structure shown in Formula (I-1) or Formula (1-2). The dual-targeting compound of the present disclosure has high affinity for an FAP target and an integrin ?v?3 target, can realize synergistic targeting of the FAP target and the integrin ?v?3 target in tumors, and has high uptake in tumors and long retention time in tumors.

Abstract: The present disclosure provides a truncated Evans Blue modified fibroblast activation protein inhibitor compound. The compound is formed by connecting truncated Evans Blue, a fibroblast activation protein inhibitor and a nuclide chelating group by means of connecting groups L1, L2, L3, L4 and X. The compound has the following structure shown in Formula (I), where R1 is a fibroblast activation protein inhibitor; L1 is lysine, glutamic acid, or a derivative structure thereof; L2 is —(CH2)n—, n is an integer from 0 to 30, and each —CH2— may be individually substituted or unsubstituted with —O—, —NH—, —(CO)—, —NH(CO)—, or —(CO)—NH—; L3 is —(CH2)m—, m is an integer from 0 to 30, and each —CH2— may be individually substituted or unsubstituted with —O— or —(CO)—; L4 is —(CH2)p—, p is an integer from 0 to 30, and each —CH2— may be individually substituted or unsubstituted with —O—, —NH—, —(CO)—, —NH(CO)—, or —(CO)—NH—; X is selected from N, C, O, S, or and R2 is a nuclide chelating group.

Abstract: The present disclosure provides a compound targeting prostate specific membrane antigen (PSMA), wherein the compound has the following structure shown in Formula (I); R1 is a compound structure targeting prostate specific membrane antigen; L1 is -(X)n-(CH2)m-(Y)q-, X and Y are independently selected from lysine, glutamic acid or a derivative structure containing lysine and glutamic acid, n is an integer from 0 to 12, m is an integer from 0 to 60, q is an integer from 0 to 12, and each CH2 may be individually substituted with —O—, —NH(CO)—, or —(CO)—NH—; L2 is -(CH2)p-, p is an integer from 0 to 30, and each CH2 may be individually substituted with —O—, —NH(CO)—, or —(CO)—NH—; and R2 is a nuclide chelating group. The present disclosure also provides a radiolabeled complex based on the structure of the compound.