Radioiodination and biological evaluation of Cladribine as potential agent for tumor imaging and therapy
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Noha Anwer Bayoumi
,
Abeer M. Amin
Abstract
Cladribine, a purine analogue antimetabolite, was radioiodinated with 125I 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 125I-Cladribine sample dissolved in 0.5 ml of 0.2 M phosphate buffer pH 7 at ambient temperature showed that 125I-Cladribine is stable up to 12 h post labeling. Biodistribution results revealed excretion of 125I-Cladribine mainly by kidneys. The uptake of 125I-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 125I-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.
©2015 Walter de Gruyter Berlin/Boston
Artikel in diesem Heft
- Frontmatter
- Radiochemical determination of 129I and 36Cl in MEGAPIE, a proton irradiated lead-bismuth eutectic spallation target
- Production of no-carrier-added 135La at an 18 MeV cyclotron and its purification for investigations at a concentration range down to 10−15 mol/L
- New estradiol based 111In complex towards the estrogen receptor
- Radioiodination and biological evaluation of Cladribine as potential agent for tumor imaging and therapy
- Production, quality control, biodistribution assessment and preliminary dose evaluation of 166Ho-alendronate as a bone marrow ablative agent
- Synthesis and evaluation of boron folates for Boron-Neutron-Capture-Therapy (BNCT)
- Plutonium 241Pu in tissues and organs of Cervidae from Northern Poland
Artikel in diesem Heft
- Frontmatter
- Radiochemical determination of 129I and 36Cl in MEGAPIE, a proton irradiated lead-bismuth eutectic spallation target
- Production of no-carrier-added 135La at an 18 MeV cyclotron and its purification for investigations at a concentration range down to 10−15 mol/L
- New estradiol based 111In complex towards the estrogen receptor
- Radioiodination and biological evaluation of Cladribine as potential agent for tumor imaging and therapy
- Production, quality control, biodistribution assessment and preliminary dose evaluation of 166Ho-alendronate as a bone marrow ablative agent
- Synthesis and evaluation of boron folates for Boron-Neutron-Capture-Therapy (BNCT)
- Plutonium 241Pu in tissues and organs of Cervidae from Northern Poland
