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.
Carcinogenesis. 2019 May 29.
Extracellular Vesicles-Derived OncomiRs Mediate Communication between Cancer Cells and Cancer-Associated Hepatic Stellate Cells in Hepatocellular Carcinoma Microenvironment.
TIC10 purchased from AbMole
|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|
|Cell lines||HCT116 cells|
|Preparation method||Ability of TIC10 (5 μM) or TRAIL (25 ng/ml) to reduce cell viability in HCT116 cells after a 1-hour preincubation at the indicated temperatures (72 hours, n = 3).|
|Animal models||Female athymic nu/nu mice|
|Dosages||25, 50, 100 mg/kg|
|Solubility (25°C)||DMSO: ≥ 12 mg/mL (Need warming)|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
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