A Novel <sup>68</sup>Ga‐Labeled 2‐Azabicyclo[3.1.0]Hexane‐3‐Carbonitrile‐Based Fibroblast Activation Protein‐Targeted Tracer for Cancer Imaging With Positron Emission Tomography
Bibliographic record
Abstract
ABSTRACT Most of the reported small molecule‐based fibroblast activation protein (FAP)‐targeted radioligands are derived from UAMC1110 and contain a 4‐difluoro‐2‐cyanopyrrolidine moiety. In this study, we investigated the effect of replacing the 4‐difluoro‐2‐cyanopyrrolidine moiety of [ 68 Ga]Ga‐FAPI‐04 with 2‐azabicyclo[3.1.0]hexane‐3‐carbonitrile on the in vitro /vivo FAP‐targeting capability. The newly derived 68 Ga‐labeled FAP‐targeted tracer, [ 68 Ga]Ga‐JC02076, was obtained in 43.5 ± 10.4% decay‐corrected radiochemical yield within 33.5 ± 5.8 min ( n = 4). The radiochemical purity and molar activity were 97.2 ± 3.4% and 411.6 ± 232.5 GBq/μmol, respectively. Ga‐JC02076 showed good binding affinity for FAP (IC 50 = 29.7 ± 3.5 nM). Most importantly, [ 68 Ga]Ga‐JC02076 enabled clear visualization of HEK293T:hFAP tumor xenografts in PET images and had good tumor uptake (7.17 ± 2.19 %ID/g) and excellent tumor‐to‐bone (17.3 ± 6.99) and tumor‐to‐muscle (32.3 ± 12.5) uptake ratios at 1 h post‐injection. Our data suggest that N ‐(4‐quinolinoyl)‐Gly‐(2‐azabicyclo[3.1.0]hexane‐3‐carbonitrile) is a promising pharmacophore for the design of FAP‐targeted tracers.
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How this classification was reachedexpand
Full frame distilled prediction
Teacher imitationNot calibrated prevalence, not ground truth. Human validation pending. Learned from the 10,348 direct Codex labels and 10,348 direct Gemma labels. Candidate is the union of thresholded teacher heads; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels or direct frontier model labels.
Codex and Gemma teacher scores by category
| Category | Codex | Gemma |
|---|---|---|
| Metaresearch | 0.000 | 0.000 |
| Meta-epidemiology (narrow) | 0.000 | 0.000 |
| Meta-epidemiology (broad) | 0.001 | 0.000 |
| Bibliometrics | 0.001 | 0.001 |
| Science and technology studies | 0.000 | 0.000 |
| Scholarly communication | 0.000 | 0.000 |
| Open science | 0.000 | 0.000 |
| Research integrity | 0.000 | 0.001 |
| Insufficient payload (model declined to judge) | 0.000 | 0.000 |
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 teacher head, 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".