A CB-TE2A bifunctional chelate applicable to immunoPET with 64Cu
Bibliographic record
Abstract
129 Objectives CB-TE2A is a highly stable chelate for 64Cu which shows improved background clearance. In this work we synthesized and evaluated 1, a side-arm functionalized version of CB-TE2A which yields a six coordinate uncharged Cu complex. The unanticipated room-temperature labeling of 1 allowed evaluation of this bifunctional chelate (BFC) for imaging with antibodies. Methods 1 and Cu(1) complexes were synthesized and characterized using standard techniques. Radiolabeling was optimized for pH, temperature, time and BFC concentration. 1 was conjugated to trastuzumab and used for 64Cu PET imaging RAG2M mice bearing HER2+ or HER2- tumor xenografts. Results The synthesis of 1 yielded two conformational isomers separable by chromatography, 1a and 1b. Cu(1a) and Cu(1b) were fully characterized, including structural determination by X-ray crystallography. 1a and 1b had significantly different 64Cu radiolabeling properties. 1b required radiolabeling conditions similar to the conditions reported for CB-TE2A (pH >6, 90°C, 1 h). Unexpectedly, 1a could be radiolabeled with 64Cu in >95% radiochemical yield under mild conditions (pH 6, Conclusions The conformational isomer 1a containing the superior Cu chelating CB-TE2A core was discovered and shown to be applicable to 64Cu immunoPET. 1a should also be useful for immunotherapy with 67Cu
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How this classification was reachedexpand
Full frame machine prediction
Teacher imitationNot calibrated prevalence, not ground truth. Human validation pending. The Gemma side is a direct model label for every work in the frame, read from the title-only record. The Codex side is a classifier learned from the 10,348 direct Codex labels and calibrated to design-weighted sample rates; fields without enough sample support carry no Codex call. Candidate is the union of the two sides; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels.
Distilled classifier scores by category (both heads)
| Category | Codex | Gemma |
|---|---|---|
| Metaresearch | 0.000 | 0.000 |
| Meta-epidemiology (narrow) | 0.000 | 0.000 |
| Meta-epidemiology (broad) | 0.000 | 0.000 |
| Bibliometrics | 0.000 | 0.000 |
| Science and technology studies | 0.000 | 0.000 |
| Scholarly communication | 0.000 | 0.000 |
| Open science | 0.000 | 0.000 |
| Research integrity | 0.000 | 0.000 |
| Insufficient payload (model declined to judge) | 0.001 | 0.001 |
Machine scores (provisional)
The two teacher heads of the student model, read on this work. A score orders the frame for review; it never asserts a category, and the validation status ships verbatim with every row.
Baseline scores from an immature model (maturity gate not passed, 7 training rounds). Scores rank; they never assert a category.
score_only:v0-immature-baseline · verbatim from the scoring run: score_only means the number may rank works, and no category label ships from itClassification
machine, unvalidatedMachine predicted; a candidate call from one source (direct Gemma or distilled Codex), not a consensus.
How this classification was reached, model by model and score by score, is at the end of the page under "How this classification was reached".