SERP
Comments:
The compound appears to be selective vs Plk4 and therefore should be suitable for dosing above 100 nM, which only represents 2x above it's cellular IC50. I would anticipate dosing up to at least IC90 / 10x above IC50 to get a meaningful dose response.
In the cited publication, the authors describe low doses for the oral and iv PK studies to determine overall PK profiles, btu these doses are unlikely to be adequate for any efficacy studies. The literature suggests doses of 20mg/kg would be more realistic for such studies. From the same publication, I really do not understand the use of chow-dosing in the efficacy study, which gives no robust control over actual dose delivered, and would strongly advocate against this dosing route.
(last updated:
5 Jun 2025 )
