Tracers / [18F]ICMT-11

[18F]ICMT-11

Also written as [18F]ICMT-11; [F-18]ICMT-11; F-18 ICMT-11; F-18 ICMT11; ICMT-11; ICMT11; isatin-5-sulfonamide
Radionuclide
F-18 t½ 109.7 min
Modality
PET
Production route
Cyclotron liquid target
Stage
Clinical research
Syntheses indexed
3

What it is

Compound class
Isatin sulfonamide
Target / mechanism
Activated caspase-3 (apoptosis); isatin-5-sulfonamide caspase-3 inhibitor PMID 22575271 / DOI 10.1016/j.nucmedbio.2012.03.004; PMID 19805307 / DOI 10.1073/pnas.0901310106
Clinical application
Imaging of tumour apoptosis / early treatment response PMID 19805307 / DOI 10.1073/pnas.0901310106; PMID 30259091 / DOI 10.1007/s00259-018-4098-9
Theranostic pair

Regulatory status

FDA
No Drugs@FDA / openFDA drug registry — no approved application found; search: https://www.accessdata.fda.gov/scripts/cder/daf/index.cfm?event=BasicSearch.process&searchTerm=ICMT-11
EMA (centralised)
Other approvals
Brand names

Clinical use

Typical injected activity
~150-160 MBq in healthy volunteers (159 +/- 3 MBq); ~330 MBq in patient studies PMID 23949910 / DOI 10.2967/jnumed.112.118760; PMID 30259091 / DOI 10.1007/s00259-018-4098-9
Uptake time
Dynamic PET ~60-65 min from injection; whole-body scans acquired up to 4 h post-injection PMID 23949910 / DOI 10.2967/jnumed.112.118760; PMID 30259091 / DOI 10.1007/s00259-018-4098-9

Reported in the literature. Not a dosing recommendation.

Published syntheses

ModuleCassettePurificationYield %RCP %Precursor / supplierSource
HPLC15.4 ± 0.1%
no
97.5 ± 0.1%acetal protected tosylate precursor40148277
2025 Nat Commun
22030029
2011 Bioorg Med Chem Lett
>98%22575271
2012 Nucl Med Biol
the process was transferred onto a fully automated GE FASTlab synthesis platform for further development and optimisation

Precursor

Common precursor
Acetal-protected tosylate precursor (SN2 [18F]fluorination, then acid-mediated deprotection and HPLC) PMID 32232626 / DOI 10.1007/s11307-020-01494-9
Suppliers seen in the literature
Typical final purification
HPLC

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Quality control Preliminary — inferred from compound class

Ph. Eur. monograph
USP monograph
AppearancepHRCP HPLCRCP TLCHPLC UVRadionuclidic (HPGe)Half-lifeActivityEndotoxins (LAL)SterilityFilter integrity
How this set was arrived at. base set per Ph. Eur. general monograph 0125 (rule); organic-phase radiosynthesis assumed from isotope/compound class, no synthesis data confirming it -> GC residual solvents (preliminary); conventional nucleophilic 18F-fluorination assumed from isotope/compound class, no synthesis data confirming K222 use -> Kryptofix test (preliminary)

Tests listed by reference only. Monograph texts are copyrighted and are not reproduced here. How these are derived

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