<i>p</i>-NO<sub>2</sub>–Bn–H<sub>4</sub>neunpa and H<sub>4</sub>neunpa–Trastuzumab: Bifunctional Chelator for Radiometalpharmaceuticals and <sup>111</sup>In Immuno-Single Photon Emission Computed Tomography Imaging
Bibliographic record
Abstract
Potentially nonadentate (N 5 O 4 ) bifunctional chelator p -SCN–Bn–H 4 neunpa and its immunoconjugate H 4 neunpa–trastuzumab for 111 In radiolabeling are synthesized. The ability of p -SCN–Bn–H 4 neunpa and H 4 neunpa–trastuzumab to quantitatively radiolabel 111 InCl 3 at an ambient temperature within 15 or 30 min, respectively, is presented. Thermodynamic stability determination with In 3+, Bi 3+, and La 3+ resulted in high conditional stability constant ( p M) values. In vitro human serum stability assays have demonstrated both 111 In complexes to have high stability over 5 days. Mouse biodistribution of [ 111 In][In( p -NO 2 –Bn–neunpa)] −, compared to that of [ 111 In][In( p -NH 2 –Bn–CHX-A″–diethylenetriamine pentaacetic acid (DTPA))] 2–, at 1, 4, and 24 h shows fast clearance of both complexes from the mice within 24 h. In a second mouse biodistribution study, the immunoconjugates 111 In-neunpa–trastuzumab and 111 In–CHX-A″–DTPA–trastuzumab demonstrate a similar distribution profile but with slightly lower tumor uptake of 111 In-neunpa–trastuzumab compared to that of 111 In–CHX-A″–DTPA–trastuzumab. These results were also confirmed by immuno-single photon emission computed tomography (immuno-SPECT) imaging in vivo. These initial investigations reveal the acyclic bifunctional chelator p -SCN–Bn–H 4 neunpa to be a promising chelator for 111 In (and other radiometals) with high in vitro stability and also show H 4 neunpa–trastuzumab to be an excellent 111 In chelator with promising biodistribution in mice.
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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 | 0.001 | 0.000 |
| Meta-epidemiology (narrow) | 0.001 | 0.001 |
| Meta-epidemiology (broad) | 0.001 | 0.000 |
| Bibliometrics | 0.000 | 0.000 |
| Science and technology studies | 0.001 | 0.001 |
| Scholarly communication | 0.000 | 0.000 |
| Open science | 0.001 | 0.000 |
| Research integrity | 0.001 | 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".