TIC10 (ONC-201) is a potent, orally active, and stable small molecule that transcriptionally induces TRAIL in a p53-independent manner and crosses the blood-brain barrier. TIC10 inactivates Akt and ERK to induce TRAIL through Foxo3a, possesses superior compound properties: delivery across the blood-brain barrier, superior stability and improved pharmacokinetics.
|Source||Cancer Med (2017). Figure 1. TIC10|
|Cell Lines||MPM cell lines|
|Concentrations||50 or 20, 10, 5, 2, 1, 0.5, 0.2, 0.1, and 0.01 μmol/L|
|Incubation Time||48 h|
|Results||In contrast, the expression and phosphorylation levels of PI3K/p85, which negatively regulates the catalytic activity of p110α, were negligible in the MPM cell lines except for NCI-H28, whereas only total PI3K/p85 was detected in normal mesothelial cell line MeT-5A|
|Animal models||Female athymic nu/nu mice|
|Dosages||25, 50, 100 mg/kg|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Dual inactivation of Akt and ERK by TIC10 signals Foxo3a nuclear translocation, TRAIL gene induction, and potent antitumor effects.
Allen JE, et al. Sci Transl Med. 2013 Feb 6;5(171):171ra17. PMID: 23390247.
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