The present invention provides a novel radioactive compound for imaging malignant melanoma and a use thereof as a contrast agent for PET imaging.

Provided is a composition containing a buffer to be used at the time of labeling of a chelated targeting agent with .sup.90Y, .sup.153Sm, .sup.165Dy, .sup.165Er, .sup.166Ho, or .sup.177Lu. At least one kind of buffer selected from the group consisting of benzoic acid, maleic acid, fumaric acid, succinic acid, and salts thereof is incorporated in a composition containing a chelated targeting agent.

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).

Provided herein are compounds of Formula (I) or a pharmaceutically acceptable salt thereof. Also provided are compositions including a compound of Formula (I) together with a pharmaceutically acceptable carrier, and methods for imaging prostate cancer cells.

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The present invention provides a targeted prodrug enzyme fusion carrier comprising a targeted molecule and a prodrug enzyme. The targeted prodrug enzyme fusion carrier can effectively identify and bind to tumor cells and tumor-induced tumor angiogenesis. The targeted prodrug enzyme fusion carrier also has a targeted prodrug enzyme fusion protein and a theranostic system utilizing the method of in vivo nuclear medicine for the clinical diagnosis and treatment of individual patients with tumors.

Ultrasound imaging is a non-invasive, non-radioactive, and low cost technology for diagnosis and identification of implantable medical devices in real time. Developing new ultrasound activated coatings is important to broaden the utility of in vivo marking by ultrasound imaging. Ultrasound responsive macro-phase segregated micro-composite thin films were developed to be coated on medical devices composed of multiple materials and with multiple shapes and varying surface area. The macro-phase segregated in films having silica micro-shells in polycyanoacrylate produces strong color Doppler signals with the use of a standard clinical ultrasound transducer. Electron microscopy showed a macro-phase separation during slow curing of the cyanoacrylate adhesive, as air-filled silica micro-shells were driven to the surface of the film. The air sealed in the hollow space of the silica shells acted as an ultrasound contrast agent and echo decorrelation of air exposed to ultrasound waves produces color Doppler signals.

Provided is a composition containing a buffer to be used at the time of labeling of a chelated targeting agent with .sup.90Y, .sup.153Sm, .sup.165Dy, .sup.165Er, .sup.166Ho, or .sup.177Lu. At least one kind of buffer selected from the group consisting of benzoic acid, maleic acid, fumaric acid, succinic acid, and salts thereof is incorporated in a composition containing a chelated targeting agent.

The present invention discloses indicator fluids, reference indicator fluid, and usage thereof, and systems and methods for assessing movement of molecular substances within, to or from a cerebrospinal fluid, brain or spinal cord compartment of a human cranio-spinal cavity. Indicator fluid moving from the cerebrospinal fluid compartment enables measurements of levels of indicator fluid in blood or urine and assessment of the cranio-spinal cavity's ability to remove molecular substances. The indicator fluids may be contrast agents used for imaging, such as by computed tomography imaging, and magnetic resonance imaging, or imaging utilizing radioactive substances by positron emission tomography, single-photon emission computed tomography or scintigraphy. Using these imaging modalities, the invention describes indicator fluids, systems and methods enabling assessment of movement of substances within, to or from a cerebrospinal fluid, brain or spinal cord compartment of a cranio-spinal cavity, and from the human cranio-spinal cavity to lymphatic pathways or kidneys.

Provided is a composition containing a buffer to be used at the time of labeling of a chelated targeting agent with .sup.90Y, .sup.153Sm, .sup.165Dy, .sup.165Er, .sup.166Ho, or .sup.177Lu. At least one kind of buffer selected from the group consisting of benzoic acid, maleic acid, fumaric acid, succinic acid, and salts thereof is incorporated in a composition containing a chelated targeting agent.

Provided herein are radiopharmaceutical compositions, conjugates and uses thereof. In one aspect, provided herein are covalently modified KRAS proteins comprising a radiolabeled compound or conjugate. In some embodiments, the radiolabeled compound described herein comprises a covalently bound radioisotope. In some embodiments, the radiolabeled conjugate comprises a targeting ligand and a metal chelator configured to bind a radionuclide. The radiolabeled compound or conjugate described herein can form a covalent bond with a cysteine residue (such as G12C) in the mutated KRAS protein. Further provided herein are methods of treating and diagnosing cancer by administering the described radiolabeled compounds, conjugates, and compositions to a subject, thereby forming the covalently modified KRAS G12C protein.