메뉴 건너뛰기




Volumn 18, Issue 17, 2008, Pages 4789-4793

An osteoclast-targeting agent for imaging and therapy of bone metastasis

Author keywords

Bifunctional chelator; Bisphosphonate; Bone metastasis; Imaging agent; Indium 111; Osteoclast

Indexed keywords

1,4,7,10 TETRAAZACYCLOTETRADECANE N,N',N'',N''' TETRAACETIC ACID BIPHOSPHONATE CONJUGATE; INDIUM 111; UNCLASSIFIED DRUG;

EID: 49949087770     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.07.092     Document Type: Article
Times cited : (17)

References (36)
  • 8
    • 0034660553 scopus 로고    scopus 로고
    • Body J.J. Cancer 88 (2000) 3054
    • (2000) Cancer , vol.88 , pp. 3054
    • Body, J.J.1
  • 24
    • 49949094097 scopus 로고    scopus 로고
    • note
    • Chemical synthesis and characterization data.(a) General methods.All chemicals, solvents, and reagents were purchased from Sigma-Aldrich (St. Louis, MO) and used directly without further purification unless otherwise noted. 1,4,7,10-Tetraazacyclododecane-1,4,7-tris-(t-butyl acetate) (DO3A-t-Bu-ester) was obtained from Macrocylic Inc. (Dallas, TX). Silica gel 60 (70-230 mesh) used for column chromatography was obtained from Sigma-Aldrich. Analytical thin-layer chromatography (TLC) was performed using Merck 60 F254 silica gel (precoated sheets, 0.2 mm thick) (Lawrence, KS) and Whatman MCK 18F reversed-phase plates (Maidstone, Kent, UK).
  • 27
    • 49949088125 scopus 로고    scopus 로고
    • note
    • 111In-DO3A-BP was determined by adding 5 μL of the complex to a solution containing 500 μL of Milli-Q water and 500 μL of octanol (obtained from a saturated octanol/water solution) (n = 10). The sample vials were shaken for 1 h at room temperature. From each vial, aliquots of 100 μL each were removed from the octanol phase and the water phase, respectively, and counted separately. The partition coefficient was calculated as the ratio of counts in the octanol fraction to the counts in the water fraction. An average of log P value was obtained from the 10 samples.
  • 32
    • 49949093597 scopus 로고    scopus 로고
    • note
    • 111In-DO3A-BP was measured by counting the cell lysates in a γ-counter. The protein concentration in each lysate was determined using the Bio-Rad Protein Assay. The assay was repeated 5 times, and all data were pooled for analysis.
  • 33
    • 49949091992 scopus 로고    scopus 로고
    • note
    • 111In-DO3A-BP was diluted with PBS (10 mM) to prepare the injection doses. Each mouse was injected with ca. 5 μCi of radioactivity in 100 μL via the tail vein. The mice were anesthetized prior to sacrifice at each time point (1, 4, 24, and 48 h; n = 4 per time point). Organs of interest were removed, weighed, and counted by a γ-counter. Standards were prepared and counted along with the samples to calculate the percent injected dose per gram (%ID/g) and percent injected dose per organ (%ID/organ). The animals of the last time point groups were housed in metabolic cages (4 mice per cage) to collect urine and feces at 1, 4, 24, and 48 h pi to evaluate the excretion route and stability of the compound.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.