In:
Radiochimica Acta, Walter de Gruyter GmbH, Vol. 103, No. 11 ( 2015-11-28), p. 777-787
Abstract:
Cladribine, a purine analogue antimetabolite, was radioiodinated with 125 I via direct electrophilic substitution
reaction. The maximum radiochemical yield (92.5 ± 0.8%) was obtained when the reaction was done at ambient temperature for 30 min using 100 μg of Cladribine and 10 μg N-chlorosuccinamide (NCS) in
150 μL of 0.2 M phosphate buffer, pH 7. In vitro stability studies of HPLC purified 125 I-Cladribine sample dissolved in 0.5 ml of 0.2 M phosphate buffer pH 7 at ambient temperature
showed that 125 I-Cladribine is stable up to 12 h post labeling. Biodistribution results revealed excretion of 125 I-Cladribine mainly by kidneys. The uptake of 125 I-Cladribine in the induced Ehrlich Ascites Carcinoma was
2.8 ± 0.4 %ID/g at 1 h post injection with maximum tumor/muscle ratio of 5.5. The good uptake of 125 I-Cladribine confirms the molecular docking studies results which indicate that iodinated Cladribine binds with
polymerase enzyme with a good –CDOCKER energy. As a result, radioiodinated Cladribine may be used as a valuable agent for tumor diagnosis and therapy.
Type of Medium:
Online Resource
ISSN:
0033-8230
,
2193-3405
DOI:
10.1515/ract-2014-2357
Language:
English
Publisher:
Walter de Gruyter GmbH
Publication Date:
2015
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