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 |
| Method | western blotting | |
| 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 Experiment | |
|---|---|
| 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). |
| Concentrations | 5 μM |
| Incubation time | - |
| Animal Experiment | |
|---|---|
| Animal models | Female athymic nu/nu mice |
| Formulation | DMSO |
| Dosages | 25, 50, 100 mg/kg |
| Administration | Intraperitoneal/oral |
| Molecular Weight | 386.49 |
| Formula | C24H26N4O |
| CAS Number | 1616632-77-9 |
| Solubility (25°C) | DMSO: ≥ 12 mg/mL (Need warming) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| 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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