170908-81-3Relevant articles and documents
Preparation, quality control and biodistribution studies of two [ 111In]-rituximab immunoconjugates
Jalilian, Amir R.,Sardari, Darush,Kia, Leila,Rowshanfarzad, Pejman,Garousi, Javad,Akhlaghi, Mehdi,Shanehsazzadeh, Saeed,Mirzaii, Mohammad
, p. 151 - 170 (2008)
In order to use Auger-electron therapeutic effects in CD20 antigen targeting in lymphomas, Mabthera (rituximab) was successively labeled with [111In]-indium chloride (185 MBq) after conjugation with freshly prepared macrocyclic bifunctional chelating agent, N-succinimidyl-1,4,7,10- tetraazacyclododecane-1,4,7,10-tetra-acetic acid (DOTA-NHS) and ccDTPA separately. Conjugated-Rituximab was obtained by the addition of 1 ml of a rituximab pharmaceutical solution (5 mg/ml, in phosphate buffer, pH=7.8) to a glass tube pre-coated with freshly prepared DOTA-NHS or ccDTPA (0.01-0.1 mg) at 25°C. Radiolabeling was performed at 37°C in 3h and room temperature for one hour for DOTA-conjugate and DTPA-conjugate respectively. HPLC showed an overall radiochemical purity of 97.5 and 95% for DOTA and DTPA-conjugates respectively (Specific activity =2800-5600 GBq/mM). The final isotonic 111In-rituximab complexes were checked by gel electrophoresis for radiolysis. Preliminary biodistribution studies in normal rat model performed to determine radioimmunoconjugates distribution of up to 48h. Oesterreichische Apotheker-Verlagsgesellschaft m. b. H.
Gd3+ cFLFLFK conjugate for MRI: A targeted contrast agent for FPR1 in inflammation
Stasiuk, Graeme J.,Smith, Helen,Wylezinska-Arridge, Marzena,Tremoleda, Jordi L.,Trigg, William,Luthra, Sajinder Kaur,Iveson, Veronique Morisson,Gavins, Felicity N. E.,Long, Nicholas J.
, p. 564 - 566 (2013)
Formyl Peptide Receptors (FPRs) are vital in the host inflammatory response, playing an important regulatory role in multiple diseases. A Gd(iii) DOTA conjugate of cFLFLFK has been synthesised which targets and visualises FPR1 upon leukocytes in the inflammatory response via magnetic resonance imaging for the first time.
Development of 170Tm-DOTA-cetuximab for radioimmunotherapy
Shirvani-Arani, Simindokht,Bahrami-Samani, Ali,Jalilian, Amir Reza,Shirvani-Arani, Amirsaleh,Ghannadi-Maragheh, Mohammad
, p. 103 - 107 (2012)
Thulium-170 [T1/2=128.4days, Eβ(max)=968keV, Eγ=84keV (3.26%)] has radionuclidic properties suitable for use in therapy. 170Tm can be produced by a relatively feasible route involving thermal neutron bombardment on natural Tm(NO3)3 (100% 169Tm) in medium flux research reactors. The combination of beta-particle emission of Tm-170 with therapeutic properties of C225 monoclonal antibody (cetuximab) as well as optimization studies for future Tm-167 labeling was targeted in this study. Conjugated cetuximab was obtained by the addition of 0.5ml of a cetuximab pharmaceutical solution (1mg, in phosphate buffer, pH7.8) to a glass tube pre-coated with in situ prepared 1,4,7,10-tetraazacyclododecane- N,N,N,N-tetraacetic acid mono-(N-hydroxysuccinimidyl) ester (DOTA-NHS) (～5mg) at 25°C. Cetuximab was labeled with 170Tm-Thulium chloride (100MBq) after conjugation with DOTA-NHS in 2-3h (radiochemical purity >99%, instant thin-layer chromatography, specific activity=77-385TBq/mmol). Biodistribution studies in wild-type rats for free Tm-170 and the radioimmunoconjugate were performed to determine the distribution up to 72h. A comparative time-frame study was performed for critical organs for both radiochemical species. The major organs of accumulation were shown to be the lung, liver, and spleen, respectively.
Conjugates of the B-subunit of shiga toxin for use as contrasting agents for imaging and therapy
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, (2014/06/24)
Multivalent conjugates comprising the following formula: (STxB-linker A-S)x-GNS-(S-linker B-T)y wherein STxB is the B-subunit of Shiga toxin; linker A is a noncleavable linker; linker B is a cleavable linker used to release at least
CONJUGATES OF THE B-SUBUNIT OF SHIGA TOXIN FOR USE AS CONTRASTING AGENTS FOR IMAGING AND THERAPY
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, (2014/06/24)
Multivalent conjugates comprising the following formula: (STxB-linker A-S)x-GNS-(S-linker B-T)y wherein STxB is the B-subunit of Shiga toxin; linker A is a noncleavable linker; linker B is a cleavable linker used to release at least
Multimodal image-guided enzyme/prodrug cancer therapy
Li, Cong,Winnard Jr., Paul T.,Takagi, Tomoyo,Artemov, Dmitri,Bhujwalla, Zaver M.
, p. 15072 - 15073 (2007/10/03)
The conjugate of bacterial cytosine deaminase (bCD) and poly-l-lysine (PLL) that was functionalized with biotin, rhodamine, and Gd3+-DOTA was synthesized and characterized. It demonstrated high relaxivity, improved enzymatic specificity to prodrug 5-fluorocytosine, low cytotoxicity, efficient cell uptake, and high enzymatic stability in fresh mouse serum and human breast cancer cell culture. Copyright
Process for making a chelating agent for labeling biomolecules using preformed active esters
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Page column 10-11, (2008/06/13)
The present invention is directed, in general, to a method for making high yields of functionalized cyclic or acyclic tertiary amine-containing compounds, termed active esters, the functionalized compounds themselves, and diagnostic or therapeutic systems incorporating such compounds. Ester groups are attached to all but one of its Nitrogen atoms of the tertiary amine-containing compound. Therefore, an active agent, in the presence of coupling agent, attaches to the remaining amine via a carboxylate group attached to the amine, to produce high yields of the active ester. The active ester is then combined with a biomolecule, to produce high yields of a bioconjugated product. A metal ion may be chelated to the bioconjugated product to produce a chelating agent for use in either diagnostic or therapeutic applications.
