The present disclosure relates to the technical field of chelating agents, in particular to a bifunctional macrocyclic chelate, a conjugate, a metal complex, and use thereof. The bifunctional macrocyclic chelate is a compound of following Formula I or an isomer thereof,

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wherein R.sub.1, R.sub.3, R.sub.5, and R.sub.7 are each independently selected from alkyls or long-chain polymer groups, R.sub.2, R.sub.4, R.sub.6, and R.sub.8 are each independently selected from functional groups, R.sub.a, R.sub.b, R.sub.c, and R.sub.d are each independently selected from any one of H, substituted or unsubstituted alkyls, halogens, substituted or unsubstituted cyano groups, substituted or unsubstituted ester groups, substituted or unsubstituted alkoxys, substituted or unsubstituted amines, and substituted or unsubstituted aryls, ring

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The bifunctional macrocyclic chelate can complex most nuclides, and expand use of the bifunctional macrocyclic chelate, and the metal complex chelating different nuclides can realize integration of diagnosis and treatment.

A new class of mass-tag polymers is provided, which include enriched metal isotopes such as zirconium and hafnium mass tags. The chemistry of these new mass tags are different from that of lanthanide mass tags, and opens up new mass channels that can be used in mass cytometry. These polymers may be used for mass cytometry, therapeutic delivery of a radioactive isotope, or screening of a therapeutic isotope. Aspects include a kit, method of making, and method of using a polymer, isotopic composition, or both. A kit may include a polymer. The polymer may include pendant groups that chelate an enriched isotope, such as zirconium and/or hafnium. The kit may include an isotopic composition comprising an enriched zirconium or hafnium isotope. Polymers may be conjugated to a biologically active material. Aspects may also include making a kit. Aspects include use of a kit, such as for mass cytometry.

Compounds comprising a cross-linking moiety and a protecting group are described herein along with their methods of use. The cross-linking moiety may comprise an indoxyl and the protecting group may comprise a sugar (e.g., a glucuronide or glucoside), phosphoester, or sulfoester group. The cross-linking moiety and protecting group may be attached to each other via an oxygen atom, sulfur atom, or linker. In some embodiments, the linker attaching the cross-linking moiety and protecting group is a self-immolative linker. A compound of the present invention may cross-link under physiological conditions and/or in vivo.

Methods are provided for administering and/or assessing a therapeutic agent intraarterially across disrupted blood-brain barrier, systemically or directly to the brain parenchyma in a subject. In a particular aspect, drug infusion parameters can be adjusted based on feedback from real-time MRI and quantitative assessment of brain uptake of the infused therapeutic molecules based on PET imaging.

Provided are compounds and compositions for targeting macrophages and other mannose-binding c-type lectin receptor high expressing cells and methods of treatment and diagnosis using such compounds and compositions.

A polymeric radiation-source with customized geometries to maximize receipt of radiation into treatment areas that is formed from either radioisotopes molecularly bonded to a polymer or radioisotopes encased within a polymer.

The disclosure relates to methods for treating tumors. In particular, the disclosure relates to a method of treating a tumor by ionizing radiations in a subject in need thereof, said method comprising the steps of: (i) injecting a first therapeutically effective amount of high-Z element containing nanoparticles as radiosensitizing agents in said subject in need thereof within a period between 2 and 7 days prior to the first irradiation of the tumor, (ii) injecting a second therapeutically effective amount of the same or different high-Z element containing nanoparticles within a period between 1 hour to 12 hours prior to the first irradiation of the tumor, and, (iii) irradiating the tumor of said subject with a therapeutically efficient dose of radiations;
wherein said high-Z element containing nanoparticles are nanoparticles containing an element with an atomic Z number higher than 40 and said nanoparticles have a mean hydrodynamic diameter below 10 nm.

Disclosed are an rk polypeptide radiopharmaceutical targeting HER2, and a preparation method therefor. The rk polypeptide radiopharmaceutical comprises an rk polypeptide dimer and a radionuclide, wherein the radionuclide marks the rk polypeptide dimer by means of a chelating agent, the rk polypeptide dimer is a polypeptide dimer formed by connecting PKM and rk polypeptide monomers and then dimerizing two rk polypeptide monomers connected to the PKM; each rk polypeptide monomer is a D-type amino acid linear eight-membered polypeptide, and the sequence of the rk polypeptide monomer is as follows: Arg-Asn-Trp-Glu-Leu-Arg-Leu-Lys; and the PKM represents a pharmacokinetic modifying molecule. The radiopharmaceutical is used for imaging diagnosis of HER2-positive tumor patients, and medication guidance and real-time therapeutic effect monitoring of patients treated by monoclonal antibodies of the anti-cancer drug trastuzumab.

The present invention provides certain compounds, or salts or solvates thereof, which can be used as matrix metalloproteinase-targeted inhibitors or imaging agents. ##STR00001##

The present technology provides compounds, as well as compositions including such compounds, useful for imaging and/or treatment of a glioma, a breast cancer, an adrenal cortical cancer, a cervical carcinoma, a vulvar carcinoma, an endometrial carcinoma, a primary ovarian carcinoma, a metastatic ovarian carcinoma, a non-small cell lung cancer, a small cell lung cancer, a bladder cancer, a colon cancer, a primary, gastric adenocarcinoma, a primary colorectal adenocarcinoma, a renal cell carcinoma, and/or a prostate cancer. The compounds are represented by the following formula: (I) or a pharmaceutically acceptable salt thereof. ##STR00001##