Detail of "105047-45-8"

CAS Number:
105047-45-8
Name:
L-Lysine,N2-[(9H-fluoren-9-ylmethoxy)carbonyl]-
Superlist Name:
Fmoc-L-lysine
Molecular Structure:
Formula:
C₂₁H₂₄N₂O₄
Molecular Weight:
368.43
Synonyms:
(2S)-6-Amino-2-[[[(9H-fluoren-9-yl)methoxy]carbonyl]amino]hexanoicacid;N-a-(Fmoc)-N-e-(NH2)-L-Lysine-OH;Na-(9-Fluorenylmethoxycarbonyl)lysine;a-N-(9-Fluorenylmethyloxycarbonyl)lysine;
Density:
1.245 g/cm³
Boiling Point:
607.6 °C at 760 mmHg
Flash Point:
321.3 °C

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Reference

Tumor targeting by an aptamer: All Rights Reserved. Tumor targeting by an aptamer. Hicke, Brian J.; Stephens, Andrew W.; Gould, Ty; Chang, Ying-Fon; Lynott, Cynthia K.; Heil, James; Borkowski, Sandra; Hilger, Christoph-Stephan; Cook, Gary; Warren, Stephen; Schmidt, Paul G. ( NeXstar Pharmaceuticals, Boulder, CO, USA). Journal of Nuclear Medicine, 47(4), 668-678 (English) 2006 Society of Nuclear Medicine. CODEN: JNMEAQ. ISSN: 0161-5505. DOCUMENT TYPE: Journal CA Section: 63 (Pharmaceuticals) Section cross-reference(s): 1, 8 Aptamers are small oligonucleotides that are selected to bind tightly and specifically to a target mol. The authors sought to det. whether aptamers have potential for in vivo delivery of radioisotopes or cytotoxic agents. TTA1, an aptamer to the extracellular matrix protein tenascin-C, was prepd. in fluorescent and radiolabeled forms. After in vivo administration, uptake and tumor distribution of Rhodamine Red-X-labeled aptamer was studied by fluorescence microscopy. In glioblastoma (U251) and breast cancer (MDA-MB-435) tumor xenografts, biodistribution and imaging studies were performed using TTA1 radiolabeled with 99mTc. Tenascin-C levels and tumor uptake were studied in a variety of addnl. human tumor xenografts. To assess the effect of radio-metal chelate on biodistribution, mercapto-acetyl diglycine (MAG2) was compared with diethylenetriaminepentaacetic acid and with MAG2-3400-mol.-wt. 919788-21-9 and 105047-45-8 which are cas registry numbers are also used here. PEG (PEG3,400). I.v. injection of fluorescent aptamer TTA1 produced bright perivascular fluorescence in a xenografted human tumor within 10 min. In the ensuing 3 h, fluorescence diffused throughout the tumor. Labeled with 99mTc, TTA1 displayed rapid blood clearance, a half-life of less than 2 min, and rapid tumor penetration: 6% injected dose (%ID)/g at 10 min. Tumor retention was durable, with 2.7%ID/g at 60 min and a long-lived phase that stabilized at 1%ID/g. Rapid tumor uptake and blood clearance yielded a tumor-to-blood ratio of 50 within 3 h. Both renal and hepatic clearance pathways were obsd. Using the 99mTc-labeled aptamer, images of glioblastoma and breast tumors were obtained by planar scintigraphy. Aptamer uptake, seen in several different human tumors, required the presence of the target protein, human tenascin-C. Modification of the MAG2 radiometal chelator dramatically altered the uptake and clearance patterns. TTA1 is taken up by a variety of solid tumors including breast, glioblastoma, lung, and colon. Rapid uptake by tumors and rapid clearance from the blood and other nontarget tissues enables clear tumor imaging. As synthetic mols., aptamers are readily modified in a site-specific manner. A variety of aptamer conjugates accumulate in tumors, suggesting imaging and potentially therapeutic applications. .

Detail of "105047-45-8"

L-Lysine,N2-[(9H-fluoren-9-ylmethoxy)carbonyl]-

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