SERP
Comments:
The use of this compound as a cellular probe should take into account the nearly equipotent activity on ALK fusion lines and relevant activity in TRKB lines. The recommended dose of 300 nM will be above the level that shows effects in ALK lines (as low as 2nM) and TRKB lines (90 nM), which may be confounding.
The compound is suitable for in vivo doing. Although 10 mg/kg in rats was shown to produce intracranial exposure of the compound after 1h, but no efficacy or tolerability data are available. 2 mg/kg was shown to suppress tumor growth and increase survival of animals on study. Thus, 2 mg/kg in rat may be more suitable for a recommended dose. Mouse is likely suitable as another model organism. Recommended doses range from 0.2 mg/kg to 15 mg/kg; depending on the model selected, each of these doses were shown to produce suppression of tumor growth with no adverse effects noted over a multi-week dosing period.
(last updated:
14 Dec 2025 )
