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Radiosynthesis of t...
Radiosynthesis of the iodine-124 labeled Hsp90 inhibitor PU-H71
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- Taldone, Tony (författare)
- Mem Sloan Kettering Cancer Centre, NY 10065 USA
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- Zatorska, Danuta (författare)
- Mem Sloan Kettering Cancer Centre, NY 10065 USA
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- Ochiana, Stefan O. (författare)
- Mem Sloan Kettering Cancer Centre, NY 10065 USA
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- Smith-Jones, Peter (författare)
- Mem Sloan Kettering Cancer Centre, NY 10065 USA; Stony Brook School Med, NY USA; Stony Brook School Med, NY USA
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- Koziorowski, Jacek (författare)
- Department of Radiology, Memorial Sloan Kettering Cancer Center, New York,NY, USA
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- Dunphy, Mark P. (författare)
- Mem Sloan Kettering Cancer Centre, NY 10065 USA
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- Zanzonico, Pat (författare)
- Mem Sloan Kettering Cancer Centre, NY 10065 USA
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- Bolaender, Alexander (författare)
- Mem Sloan Kettering Cancer Centre, NY 10065 USA
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- Lewis, Jason S. (författare)
- Mem Sloan Kettering Cancer Centre, NY 10065 USA; Mem Sloan Kettering Cancer Centre, NY 10065 USA
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- Larson, Steven M. (författare)
- Mem Sloan Kettering Cancer Centre, NY 10065 USA; Mem Sloan Kettering Cancer Centre, NY 10065 USA
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- Chiosis, Gabriela (författare)
- Mem Sloan Kettering Cancer Centre, NY 10065 USA
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- Vara Kishore Pillarsetty, Naga (författare)
- Mem Sloan Kettering Cancer Centre, NY 10065 USA
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(creator_code:org_t)
- 2016-01-25
- 2016
- Engelska.
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Ingår i: Journal of labelled compounds & radiopharmaceuticals. - : WILEY-BLACKWELL. - 0362-4803 .- 1099-1344. ; 59:3, s. 129-132
- Relaterad länk:
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https://europepmc.or...
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https://urn.kb.se/re...
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https://doi.org/10.1...
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Abstract
Ämnesord
Stäng
- Heat shock protein 90 (Hsp90) is an ATP dependent molecular chaperone protein whose function is critical for maintaining several key proteins involved in survival and proliferation of cancer cells. PU-H71 (1), is a potent purine-scaffold based ATP pocket binding Hsp90 inhibitor which has been shown to have potent activity in a broad range of in vivo cancer models and is currently in Phase I clinical trials in patients with advanced solid malignancies, lymphomas, and myeloproliferative neoplasms. In this report, we describe the radiosynthesis of [I-124]-PU-H71(5); this was synthesized from the corresponding Boc-protected stannane precursor 3 by iododestannylation with [I-124]-NaI using chloramine-T as an oxidant for 2min, followed by Boc deprotection with 6 N HCl at 50 degrees C for 30min to yield the final compound. The final product 5 was purified using HPLC and was isolated with an overall yield of 55 +/- 6% (n=6, isolated) from 3, and >98% purity and an average specific activity of 980mCi/mu mol. Our report sets the stage for the introduction of [I-124]-PU-H71 as a potential non-invasive probe for understanding biodistribution and pharmacokinetics of PU-H71 in living subjects using positron emission tomography imaging.
Ämnesord
- MEDICIN OCH HÄLSOVETENSKAP -- Klinisk medicin (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Clinical Medicine (hsv//eng)
Nyckelord
- iodine-124; PU-H71; purine; heat shock protein 90; PET; radiotracer; cancer; iododestannylation
Publikations- och innehållstyp
- ref (ämneskategori)
- art (ämneskategori)
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Till lärosätets databas
- Av författaren/redakt...
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Taldone, Tony
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Zatorska, Danuta
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Ochiana, Stefan ...
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Smith-Jones, Pet ...
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Koziorowski, Jac ...
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Dunphy, Mark P.
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visa fler...
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Zanzonico, Pat
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Bolaender, Alexa ...
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Lewis, Jason S.
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Larson, Steven M ...
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Chiosis, Gabriel ...
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Vara Kishore Pil ...
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- MEDICIN OCH HÄLSOVETENSKAP
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MEDICIN OCH HÄLS ...
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och Klinisk medicin
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Journal of label ...
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Linköpings universitet