Functional characterization of CFI-402257, a potent and selective Mps1/TTK kinase inhibitor, for the treatment of cancer
Bibliographic record
Abstract
Significance At present, microtubule-targeting agents are the most important antimitotic drugs used in the clinic. However, there is an urgent need for the discovery of new approaches to more effectively target tumor cells with less toxicity. Emerging strategies for anticancer therapy include exploiting cell-cycle checkpoint vulnerabilities and genomic instability in cancer cells. The spindle assembly checkpoint (SAC) is important for cell survival, and its inactivation generates lethal genomic instability in cancer cells. Inhibition of SAC signaling through targeting of monopolar spindle 1 (Mps1) has provided an indication of the feasibility of such an approach. We report here the cellular and antitumor effects of CFI-402257, a potent and specific small-molecule inhibitor of Mps1. CFI-402257 is currently in a phase I clinical trial ( ClinicalTrials.gov ID: NCT02792465).
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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) | 0.000 | 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) | 0.000 | 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".