Radiosynthesis and evaluation of IGF1R PET ligand [11C]GSK1838705A

Kiran Kumar Solingapuram Sai; Jaya Prabhakaran; Anirudh Sattiraju; J. John Mann; Akiva Mintz; J. S.Dileep Kumar

doi:10.1016/j.bmcl.2017.04.085

Radiosynthesis and evaluation of IGF1R PET ligand [¹¹C]GSK1838705A

Kiran Kumar Solingapuram Sai, Jaya Prabhakaran, Anirudh Sattiraju, J. John Mann, Akiva Mintz, J. S.Dileep Kumar

Research output: Contribution to journal › Article › peer-review

9 Scopus citations

Abstract

Radiosynthesis and evaluation of [¹¹C]GSK1838705A in mice using microPET and determination of specificity in human GBM UG87MR cells are described herein. The radioligand was synthesized by reacting desmethyl-GSK1838705A with [¹¹C]CH₃I using GE FX2MeI module in ∼5% yield (EOS), >95% radiochemical purity and a specific activity of 2.5 ± 0.5 Ci/μmol. MicroPET imaging in mice indicated that [¹¹C]GSK1838705A penetrated blood brain barrier (BBB) and showed retention of radiotracer in brain. The radioligand exhibited high uptake in U87MG cells with >70% specific binding to IGF1R. Our experiments suggest that [¹¹C]GSK-1838705A can be a potential PET radiotracer for the in vivo quantification of IGF1R expression in GBM and other brain tumors.

Original language	English
Pages (from-to)	2895-2897
Number of pages	3
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	27
Issue number	13
DOIs	https://doi.org/10.1016/j.bmcl.2017.04.085
State	Published - 2017
Externally published	Yes

Keywords

Growth factor
IGF1R
Micropet
Radiotracer

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10.1016/j.bmcl.2017.04.085

Cite this

@article{1b5cc934880745e9840b420d9dc207c7,

title = "Radiosynthesis and evaluation of IGF1R PET ligand [11C]GSK1838705A",

abstract = "Radiosynthesis and evaluation of [11C]GSK1838705A in mice using microPET and determination of specificity in human GBM UG87MR cells are described herein. The radioligand was synthesized by reacting desmethyl-GSK1838705A with [11C]CH3I using GE FX2MeI module in ∼5% yield (EOS), >95% radiochemical purity and a specific activity of 2.5 ± 0.5 Ci/μmol. MicroPET imaging in mice indicated that [11C]GSK1838705A penetrated blood brain barrier (BBB) and showed retention of radiotracer in brain. The radioligand exhibited high uptake in U87MG cells with >70% specific binding to IGF1R. Our experiments suggest that [11C]GSK-1838705A can be a potential PET radiotracer for the in vivo quantification of IGF1R expression in GBM and other brain tumors.",

keywords = "Growth factor, IGF1R, Micropet, Radiotracer",

author = "{Solingapuram Sai}, {Kiran Kumar} and Jaya Prabhakaran and Anirudh Sattiraju and Mann, {J. John} and Akiva Mintz and Kumar, {J. S.Dileep}",

note = "Publisher Copyright: {\textcopyright} 2017 Elsevier Ltd",

year = "2017",

doi = "10.1016/j.bmcl.2017.04.085",

language = "English",

volume = "27",

pages = "2895--2897",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier Ltd.",

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TY - JOUR

T1 - Radiosynthesis and evaluation of IGF1R PET ligand [11C]GSK1838705A

AU - Solingapuram Sai, Kiran Kumar

AU - Prabhakaran, Jaya

AU - Sattiraju, Anirudh

AU - Mann, J. John

AU - Mintz, Akiva

AU - Kumar, J. S.Dileep

PY - 2017

Y1 - 2017

N2 - Radiosynthesis and evaluation of [11C]GSK1838705A in mice using microPET and determination of specificity in human GBM UG87MR cells are described herein. The radioligand was synthesized by reacting desmethyl-GSK1838705A with [11C]CH3I using GE FX2MeI module in ∼5% yield (EOS), >95% radiochemical purity and a specific activity of 2.5 ± 0.5 Ci/μmol. MicroPET imaging in mice indicated that [11C]GSK1838705A penetrated blood brain barrier (BBB) and showed retention of radiotracer in brain. The radioligand exhibited high uptake in U87MG cells with >70% specific binding to IGF1R. Our experiments suggest that [11C]GSK-1838705A can be a potential PET radiotracer for the in vivo quantification of IGF1R expression in GBM and other brain tumors.

AB - Radiosynthesis and evaluation of [11C]GSK1838705A in mice using microPET and determination of specificity in human GBM UG87MR cells are described herein. The radioligand was synthesized by reacting desmethyl-GSK1838705A with [11C]CH3I using GE FX2MeI module in ∼5% yield (EOS), >95% radiochemical purity and a specific activity of 2.5 ± 0.5 Ci/μmol. MicroPET imaging in mice indicated that [11C]GSK1838705A penetrated blood brain barrier (BBB) and showed retention of radiotracer in brain. The radioligand exhibited high uptake in U87MG cells with >70% specific binding to IGF1R. Our experiments suggest that [11C]GSK-1838705A can be a potential PET radiotracer for the in vivo quantification of IGF1R expression in GBM and other brain tumors.

KW - Growth factor

KW - IGF1R

KW - Micropet

KW - Radiotracer

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DO - 10.1016/j.bmcl.2017.04.085

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SN - 0960-894X

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SP - 2895

EP - 2897

JO - Bioorganic and Medicinal Chemistry Letters

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IS - 13