Tracer library / 3-[211At]astato-α-methyl-O-methyl-L-tyrosine
3-[211At]astato-α-methyl-O-methyl-L-tyrosine
Also written as 211At-AAMT-O-Me-L; AAMT-O-Me-L
- Radionuclide
- At-211 t½ 431 min
- Modality
- Therapy
- Production route
- —
- Stage
- Preclinical
- Syntheses indexed
- 2
What it is
- Compound class
- Radiohalogenated amino acid analogue (alpha-methyl-tyrosine derivative, O-methylated), LAT1 substrate
- Target / mechanism
- L-type amino acid transporter 1 (LAT1); developed from a seed compound (3-[211At]astato-α-methyl-L-tyrosine, 211At-AAMT-OH-L) by replacing the phenol OH with a methyl group, which increased tumour retention PMID 39596451
- Clinical application
- Targeted alpha-radionuclide therapy for LAT1-expressing tumours; described as the lead compound from a structure-activity series (OH, methyl, ethyl and propyl analogues compared), selected for uptake speed, high specific radioactivity, stability and therapeutic effect PMID 39596451
- Theranostic pair
- —
Published syntheses
| Module | Cassette | Purification | Yield % | RCP % | Precursor / supplier | Source |
|---|---|---|---|---|---|---|
| — | — | SPE | 81% | 98% | boronic acid or pinacolborane substituted…boronic acid or pinacolborane substituted precursor Kishida Chemical Co., Ltd. | 39596451 2024 Int J Mol Sci |
| Manual synthesis | — | SPE | 81.3% crude, 81% purified | 98% | boronic acid/pinacolborane substituted…boronic acid/pinacolborane substituted precursor for 211At-AAMT-O-Me-L Kishida Chemical Co., Ltd. | 39596451 2024 Int J Mol Sci All precursors were labeled by "Shirakami Reaction" and purified using an HLB column (Waters Corp, Waltham, MA, USA). - 211At-AAMT-O-Me-L in the crude product solution was detected at Rf = 0.80, yielding a radiochemical yield (RCY) of 81.3%. The radiochemical yield and purity of the purified product were 81% and 98%, respectively. |
Precursor
- Common precursor
- —
- Suppliers seen in the literature
- —
- Cited suppliers in indexed syntheses
- Kishida Chemical Co.
- Typical final purification
- —
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Get in touchNotes
Added stage 29 (2026-09-14): replaces the deleted 'at211-astato' fragment row (name was just the element 'astato', no active-ingredient root, 0 parsed syntheses). Its one remaining source, PMID 39596451 ('Development of LAT1-Selective Nuclear Medicine Therapeutics Using Astatine-211'), is a development-program review, but it names concrete compounds rather than describing the program in the abstract only -- quote: 'The seed compound was 3-[211At] Astato-α-methyl-L-tyrosine (211At-AAMT-OH-L)... By changing the OH group of phenol to a methyl group, retention was successfully increased... 211At-AAMT-O-Me-L, which has a simple structure, was clearly superior in terms of uptake speed for several candidate compounds.' This row tracks the named lead compound (AAMT-O-Me-L); the earlier seed compound (AAMT-OH-L) is mentioned here as context, not as its own row -- ask if a separate entry for it is wanted. Distinct from at211-aamp (2-[211At]astato-α-methyl-L-phenylalanine, PMID 32916470) -- different amino acid backbone (tyrosine vs phenylalanine), different source article, not the same compound.