TIC10 Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
TIC10 induces the expression of TNF-related apoptosis-inducing ligand (TRAIL) at 1-5 μM in a p53-independent manner. It is orally active, stable, and crosses the blood-brain barrier. The induction of TRAIL results from dual inhibition of Akt and ERK1/2 combined with nuclear translocation of the transcription factor FOXO3a. TIC10 suppresses the growth of orthotopic human glioblastoma multiforme tumors in mice.
Biologische Aktivit?t
TIC10 (also named ONC21), a first-in-class small molecule inducer of TRAIL, has been developed. Preclinical studies have shown that it potently induces TRAIL expression. TIC10 treatment in cancer cells blocks Akt and Erk signalling to activate Foxo3a, which transcriptionally up-regulates the TRAIL gene. TIC10 has displayed ideal properties as a potential anti-cancer drug, including a broad spectrum of activity, wide safety margin, robust stability, aqueous solubility, favourable pharmacokinetics, and oral activity[5].
TIC10 Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
