Tracer library / [225Ac]Ac(MacropaSq-hG250)

[225Ac]Ac(MacropaSq-hG250)

Also written as [Ac-225]Ac(MacropaSq-hG250)
Radionuclide
Ac-225 t½ 14284.8 min
Modality
Therapy
Production route
—
Stage
Preclinical
Syntheses indexed
1

What it is

Compound class
Radiolabeled monoclonal antibody (girentuximab) conjugated with macrocyclic diazacrown ether chelator (Macropa-type), targeting carbonic anhydrase IX
Target / mechanism
Binds carbonic anhydrase IX (CAIX), overexpressed on clear cell renal cell carcinoma cells PMID 38425522
Clinical application
Alpha particle radioimmunotherapy targeting CAIX-expressing tumors, evaluated in mouse xenograft model PMID 38425522
Theranostic pair
—

Published syntheses

ModuleCassettePurificationYield %RCP %Precursor / supplierSource
Manual synthesis——quantitative97.8%H2MacropaSq-hG25038425522
2024 Chem Sci
Neutralized [225Ac]AcIII (370 kBq) was reacted with H2MacropaSq-hG250 (10 μg) with a final antibody concentration of 1.5 μM. - quantitative radiolabeling was achieved within 1 minute

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Notes

Added at stage 22: promoted from 'Reported once' (single-article, no diagnostic pair at discovery) because a full-text synthesis with extracted data exists in parsed-therapy.xlsx -- PMID(s): 38425522. Target/mechanism, clinical application, indications, approval and precursor fields still need per-agent research and are intentionally left empty. Stage set/updated at stage 23 from PMID 38425522: 'Evaluation of [225Ac]Ac(MacropaSq-hG250) in a mouse xenograft model, that overexpresses carbonic anhydrase IX, demonstrated a highly significant therapeutic response.'. | Stage 26: Name corrected from '[225Ac]Ac-Ac(MacropaSq-hG250' to '[225Ac]Ac(MacropaSq-hG250)' -- matches the verbatim quote already on file from PMID 38425522 ('Evaluation of [225Ac]Ac(MacropaSq-hG250) in a mouse xenograft model...'): source used a single 'Ac' with no hyphen and a closing parenthesis.
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