Description: TIC10 (ONC-201, NSC-350625), an imipridone compound, is a novel, potent, orally bioavailable, brain/BBB penetrant, and stable tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) inducer with potential anticancer activity. It was initially developed in the 1970s as an anti-seizure agent which acts by inhibiting Akt and ERK, consequently activating Foxo3a and significantly inducing cell surface TRAIL. TIC10 can inactivate Akt and ERK to induce TRAIL through Foxo3a, possesses superior drug properties: delivery across the blood-brain barrier, superior stability and improved pharmacokinetics. TIC10 is a potent, orally active, and stable small molecule that transcriptionally induces TRAIL in a p53-independent manner. TIC10 induces a sustained up-regulation of TRAIL in tumors and normal cells that may contribute to the demonstrable antitumor activity of TIC10.
References:Cancer Res. 2015 Apr 15;75(8):1668-74; Sci Transl Med. 2013 Feb 6;5(171):171ra17.
Related CAS #: 1616632-77-9 (free base); 1638178-82-1 (HCl); 41276-02-2 (TIC10 analog); 1777785-71-3 (HBr)
2007141-57-1 (2HBr) 41276-02-2 (TIC10 isomer)