Abstract: The present disclosure provides, inter alia, novel compounds targeting cholecystokinin-2 receptor (CCK2R) expressed on the surface of cancer cells. Also provided are methods for imaging, diagnosing, and/or treating cancers using the same.

Abstract: Systems and methods for generating radionuclides, such as radium-224. Systems herein may include a first cartridge having a first opening, a second opening, and a chamber therebetween having a first resin having affinity for thorium-228 and bismuth-212; a second cartridge having a first opening, a second opening, and a chamber therebetween having a second resin having affinity for thorium-228 and bismuth-212, a third cartridge having a first opening, a second opening, and a chamber therebetween comprising a third resin having affinity for thorium-228 and bismuth-212, a fourth cartridge having a first opening, a second opening, and a chamber therebetween having a third resin having affinity for lead-212; wherein a continuous flow path is formed from a top of the first cartridge though the second cartridge, through the third cartridge, and to a bottom of the fourth cartridge during system use.

Abstract: Systems and methods for generating radionuclides, such as radium-224. Systems herein may include a first cartridge having a first opening, a second opening, and a chamber therebetween having a first resin having affinity for thorium-228 and bismuth-212; a second cartridge having a first opening, a second opening, and a chamber therebetween having a second resin having affinity for thorium-228 and bismuth-212, a third cartridge having a first opening, a second opening, and a chamber therebetween comprising a third resin having affinity for thorium-228 and bismuth-212, a fourth cartridge having a first opening, a second opening, and a chamber therebetween having a third resin having affinity for lead-212; wherein a continuous flow path is formed from a top of the first cartridge though the second cartridge, through the third cartridge, and to a bottom of the fourth cartridge during system use.

Abstract: The present invention relates to a fibroblast activation protein alpha (FAP)-targeting peptides A-[Z-AA1-AA2-AA3-AA4-AA5-AA6-AA7-Z]-B. A is N-terminal structure. B is C-terminal structure, and each of the Z, AA1, AA2, AA3, AA4, AA5, AA6, AA7 is a residue of an amino acid. The peptides can be linear or cyclized.

Abstract: The present invention provides in certain embodiments a carcinoma-targeting conjugate comprising Formula I wherein T is a SST2R targeting ligand, L is a linker, and X is a chelator, for the therapeutic treatment of cancer, and methods of use thereof.

Abstract: Systems and methods for generating radionuclides, such as radium-224, are disclosed herein. Systems herein may include a first cartridge having a first opening, a second opening, and a chamber therebetween having a first resin having affinity for thorium-228 and bismuth-212; a second cartridge having a first opening, a second opening, and a chamber therebetween having a second resin having affinity for thorium-228, a third cartridge having a first opening, a second opening, and a chamber therebetween comprising a third resin having affinity for thorium-228 and bismuth-212, and a fourth cartridge having a first opening, a second opening, and a chamber therebetween having a fourth resin having affinity for lead-212; wherein a continuous flow path is formed from a top of the first cartridge though the second cartridge, through the third cartridge, and to a bottom of the fourth cartridge during system use.

Abstract: Systems and methods for generating radionuclides, such as radium-224. Systems herein may include a first cartridge having a first opening, a second opening, and a chamber therebetween having a first resin having affinity for thorium-228 and bismuth-212; a second cartridge having a first opening, a second opening, and a chamber therebetween having a second resin having affinity for thorium-228 and bismuth-212, a third cartridge having a first opening, a second opening, and a chamber therebetween comprising a third resin having affinity for thorium-228 and bismuth-212, a fourth cartridge having a first opening, a second opening, and a chamber therebetween having a third resin having affinity for lead-212; wherein a continuous flow path is formed from a top of the first cartridge though the second cartridge, through the third cartridge, and to a bottom of the fourth cartridge during system use.

Abstract: A method for separating a lead radioisotope from a mixture comprising the lead radioisotope and a radioisotope of radium or thorium is provided, along with a system comprising a plurality of chromatographic columns. The system can include a first cartridge having a lead-complexing media that preferentially binds the lead radioisotope over radioisotopes of radium or thorium, and a second cartridge having a weak cationic exchange media, where a pH of a loading solution used to load the second cartridge is pH2L, and a pH of an eluent used to elute the lead radioisotope from the second cartridge is pH2E, and pH2L is greater than pH2E. The system can also comprise further third and fourth cartridges with chromatographic media to extract and purify the lead radioisotope, to provide a purified solution of lead radioisotope that can be used for medical and other purposes, such as in the labeling of radiopharmaceutical compounds.

Abstract: The present invention provides in certain embodiments a carcinoma-targeting conjugate comprising Formula I: T-L-X wherein T is a SSTR2 targeting ligand, L is a linker, and X is a chelator, for the therapeutic treatment of cancer, and methods of use thereof.

Abstract: The present invention relates to a fibroblast activation protein alpha (FAP)-targeting peptides A-[Z-AA1-AA2-AA3-AA4-AA5-AA6-AA7-Z]—B. A is N-terminal structure. B is C-terminal structure, and each of the Z, AA1, AA2, AA3, AA4, AA5, AA6, AA7 is a residue of an amino acid. The peptides can be linear or cyclized.

Abstract: The present invention relates to a fibroblast activation protein alpha (FAP)-targeting peptides A-[Z-AA1-AA2-AA3-AA4-AA5-AA6-AA7-Z]-B. A is N-terminal structure. B is C-terminal structure, and each of the Z, AA1, AA2, AA3, AA4, AA5, AA6, AA7 is a residue of an amino acid. The peptides can be linear or cyclized.

Abstract: The present invention relates to a fibroblast activation protein alpha (FAP)-targeting conjugate comprising Formula I: Y-L-X, wherein Y is a chelator or cytotoxic drug, L is a linker, and X is a molecule comprising a cyclic peptide of formula A-[Z-AA1-AA2-AA3-AA4-AA5-AA6-AA7-Z]-B A is N-terminal structure. B is C-terminal structure, and each of the Z, AA1, AA2, AA3, AA4, AA5, AA6, AA7 is a residue of an amino acid.

Abstract: A method for separating a lead radioisotope from a mixture comprising the lead radioisotope and a radioisotope of radium or thorium is provided, along with a system comprising a plurality of chromatographic columns. The system can include a first cartridge having a lead-complexing media that preferentially binds the lead radioisotope over radioisotopes of radium or thorium, and a second cartridge having a weak cationic exchange media, where a pH of a loading solution used to load the second cartridge is pH2L, and a pH of an eluent used to elute the lead radioisotope from the second cartridge is pH2E, and pH2L is greater than pH2E. The system can also comprise further third and fourth cartridges with chromatographic media to extract and purify the lead radioisotope, to provide a purified solution of lead radioisotope that can be used for medical and other purposes, such as in the labeling of radiopharmaceutical compounds.

Abstract: The invention provides compositions, kits and methods to treat a hyperproliferative disorder with an agent that increases expression of MCR1 and an MCR1 ligand. The invention also provides a method of treating drug-resistant melanoma, comprising administering an MCR1 ligand to a patient in need thereof. The present invention also provides in certain embodiments a melanoma-targeting conjugate comprising Formula I. T-L-X wherein T is a MCR1 ligand, L is a linker, and X an anti-cancer composition, for the therapeutic treatment of a hyperproliferative disorder. The present invention also provides methods, kits, and uses of the conjugate of Formula I.

Abstract: A method for separating a lead radioisotope from a mixture comprising the lead radioisotope and a radioisotope of radium or thorium is provided, along with a system comprising a plurality of chromatographic columns. The system can include a first cartridge having a lead-complexing media that preferentially binds the lead radioisotope over radioisotopes of radium or thorium, and a second cartridge having a weak cationic exchange media, where a pH of a loading solution used to load the second cartridge is pH2L, and a pH of an eluent used to elute the lead radioisotope from the second cartridge is pH2E, and pH2L is greater than pH2E. The system can also comprise further third and fourth cartridges with chromatographic media to extract and purify the lead radioisotope, to provide a purified solution of lead radioisotope that can be used for medical and other purposes, such as in the labeling of radiopharmaceutical compounds.

Abstract: A method of performing a chelating reaction comprising contacting a divalent metal with a compound of Formula (I): or a salt thereof wherein: each of R1-R4 is independently selected from the group consisting of CH2COORa and CH2C(?O)NHRa; each of R5-R12 is independently selected from the group consisting of II and -L-X; each Ra is independently selected from the group consisting of H and -L-X; each L is independently selected from the group consisting of absent and a linking group; and each X is a biological agent; and wherein the contacting occurs at a temperature below about 40° C. to form a chelated composition.

Abstract: The invention provides compositions, kits and methods to treat a hyperproliferative disorder with an agent that increases expression of MCR1 and an MCR1 ligand. The invention also provides a method of treating drug-resistant melanoma, comprising administering an MCR1 ligand to a patient in need thereof. The present invention also provides in certain embodiments a melanoma-targeting conjugate comprising Formula I: T-L-X wherein T is a MCR1 ligand, L is a linker, and X an anti-cancer composition, for the therapeutic treatment of a hyperproliferative disorder. The present invention also provides methods, kits, and uses of the conjugate of Formula I.

Abstract: The present invention provides in certain embodiments a carcinoma-targeting conjugate comprising Formula I: T-L-X wherein T is a SSTR2 targeting ligand, L is a linker, and X is a chelator, for the therapeutic treatment of cancer, and methods of use thereof.

Abstract: A method of performing a chelating reaction comprising contacting a divalent metal with a compound of Formula (I): or a salt thereof wherein: each of R1-R4 is independently selected from the group consisting of CH2COORa and CH2C(?O)NHRa; each of R5-R12 is independently selected from the group consisting of H and -L-X; each Ra is independently selected from the group consisting of H and -L-X; each L is independently selected from the group consisting of absent and a linking group; and each X is a biological agent; and wherein the contacting occurs at a temperature below about 40° C. to form a chelated composition.

Abstract: The present invention relates to a process of removing free-unlabeled radionuclides from a radiopharmaceutical prior to administering the radiopharmaceutical to the patient using size-exclusion or ion-exchange mechanisms.