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Volumn 16, Issue 19, 2006, Pages 5157-5163

Development of a novel albumin-binding prodrug that is cleaved by urokinase-type-plasminogen activator (uPA)

Author keywords

[No Author keywords available]

Indexed keywords

ALBUMIN; DOXORUBICIN; PRODRUG; UROKINASE RECEPTOR; WATER;

EID: 33747339731     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2006.07.023     Document Type: Article
Times cited : (38)

References (32)
  • 19
    • 33747352090 scopus 로고    scopus 로고
    • note
    • +, HPLC (495 nm): >95%.
  • 20
    • 33747329418 scopus 로고    scopus 로고
    • note
    • 2, pH 5.0, containing 0.1% Brij 35). Homogenization was carried out with a micro-dismemberator at 3000 rpm for 3 min with the aid of glass balls, and the samples were then centrifuged at 5000 rpm for 10 min and kept frozen at -78 °C prior to use.
  • 21
    • 33747361080 scopus 로고    scopus 로고
    • note
    • HPLC was performed with a BioLogic Duo Flow System from Bio-Rad (Munich, Germany), which was connected with a Merck F-1050 Fluorescence Spectrophotometer (EX. 490 nm, EM. 540 nm) and a Lambda 1000 visible detector from Bischoff (at λ = 495 nm); UV-detection at 280 nm; column: Waters, 300 Å, Symmetry C18 (4.6 × 250 mm) with precolumn; injection volume: 50 μL.
  • 22
    • 33747348525 scopus 로고    scopus 로고
    • note
    • 3CN, 30% 4 mM sodium phosphate buffer (pH 3.0); gradient: 0-25 min 100% mobile phase A; 25-40 min increase to mobile phase B; 40-50 min 100% mobile phase B; 50-60 min decrease to initial mobile phase.
  • 29
    • 33747349817 scopus 로고    scopus 로고
    • note
    • +.
  • 30
    • 33747347636 scopus 로고    scopus 로고
    • note
    • 3CN, 30% 20 mM potassium phosphate (pH 7.0); gradient: 0-25 min 100% mobile phase A; 25-40 min increase to mobile phase B; 40-50 min 100% mobile phase B; 50-60 min decrease to initial mobile phase.
  • 31
    • 33747332108 scopus 로고    scopus 로고
    • note
    • -1]. The concentration of 1 in the conjugate was adjusted to 500 ± 50 μM by concentrating the sample with CENTRIPREP-10-concentrators from Amicon, FRG (4 °C and 4500 rpm). Samples were kept frozen at -20 °C and thawed prior to use.
  • 32
    • 33747345731 scopus 로고    scopus 로고
    • note
    • In vivo experiment. For the orientating toxicity study of 1 two female NMRI: nude mice were used. Compound 1 was dissolved in 10 mM sodium phosphate/5% d-glucose buffer, pH 7.0, and was administered at a dose of 3 × 59.95 mg/kg (3 × 24 mg/kg doxorubicin equivalents) by intravenous application to two animals with an interval of 7 days (1th, 8th, and 15th day).


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.