DOTA tris(TBE)-Amido-dPEG®-broomoacetamide-50mg

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DOTA-tris(TBE)-amido-dPEG®23-bromoacetamide, product number QBD-11153, combines the macrocycle 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) through a single molecular weight, discrete polyethylene glycol (dPEG®) linker to a thiol-reactive bromoacetyl group that couples to the dPEG® linker via an amide bond. The dPEG® linker contains 75 atoms and is 85.2 Å long from the terminal amide adjacent to the DOTA moiety to the methylene group adjacent to the bromine atom. This product is useful in radioimaging and radiotherapeutic applications. The bromoacetate moiety (present as the bromoacetamide in QBD-11153) reacts chemoselectively, but not chemospecifically, with free thiol groups to form stable thioether bonds. The rate and specificity of bromoacetate for free thiols depends upon the pH of the reaction and the relative availability (compared to thiols) of other groups with which the bromoacetate moiety can react (for example, surface-accessible amines). DOTA is a highly popular bifunctional chelator used in a variety of diagnostic and therapeutic applications for the delivery of radionuclides, particularly lanthanide radionuclides and certain rare earth radioisotopes such as yttrium. DOTA is the preferred ligand for treatments using trivalent lanthanides because it binds the metal ions to form thermodynamically stable, kinetically inert complexes. Importantly, this product has the DOTA group protected by three tert-butyl ester groups and cannot chelate metals until those protecting groups are removed (using, for example, trifluoroacetic acid). However, this compound can be introduced at an early stage in a drug development process and left protected until the final step before chelation. This allows users to extensively manipulate and develop the product without putting the DOTA moiety's performance at risk. The long, flexible, single molecular weight dPEG® linker between the DOTA and the bromoacetate groups serves many purposes. First, each ethylene glycol unit in the dPEG® chain acquires up to three molecules of water through hydrogen bonding resulting in improved water solubility for conjugate molecules. Second, in aqueous environments such as blood, dPEG® increases the hydrodynamic volume of dPEG® conjugates. With larger hydrodynamic volumes, conjugates are less susceptible to renal excretion, meaning that lower doses of the diagnostic or therapeutic agent are needed for the efficacious performance of the conjugate. Third, dPEG® is non-immunogenic, and its large hydrodynamic volume helps reduce the immunogenicity of conjugated molecules.
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品牌介绍

Click Chemistry Tools（CCT）公司位于美国亚利桑那州斯科茨代尔（Scottsdale,AZ）。自公司成立以来，一致致力于不断开发和扩展一系列连接产品。他们利用特别新的研究成果研发生产出新颖的交联和标记试剂。产品被广泛用于药物研发、癌症治疗以及各类诊断技术等。此外，CCT还可以提供个性化的定制产品，已满足不同用户的需求。目前CCT的产品线主要包括：Azides（Biotin-Azides）试剂、Bis-sulfone交联试剂、DBCO试剂、TCO试剂、Terminal Alkyne试剂、Tetrazine试剂、标记试剂盒以及分选用底物等。 Fluoroprobes公司位于美国亚利桑那州斯科茨代尔(Scottsdale, AZ)，自成立以来，一直致力于不断开发一系列的连接(linker)产品。利用特别新的研究成果研发生产出各类新颖的交联和标记试剂。其产品被广泛用于药物研发与筛选、疾病治疗方法和诊断技术等领域。此外，Fluoroprobes还可以根据客户的个性化需求提供各类定制连接产品。代表产品有Classic Fluorescent Dyes, AZDye, Cyanine Dyes, IR Dyes, MB dyes以及一些标记试剂盒等。 Quanta Biodesign公司位于美国中部的俄亥俄州，成立于1997年。也是专注于生产研发各类标记产品的品牌之一。其研发的产品与dPEG技术相结合，生产出他们独有的专利产品dPEG Building Blocks and Linkers，被广泛用于细胞治疗和分子诊断等研究领域。另外，还可为广大科研工作者提供多种化学修饰试剂以及传统Liner等。 目前上述三个品牌都已被被Vectorlabs收购并整合到Vectorlabs产品中

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