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TIC10

Cat. No. M3068
TIC10 Structure
Synonym:

ONC-201; Dordaviprone

Size Price Availability Quantity
5mg USD 50  USD50 In stock
10mg USD 65  USD65 In stock
25mg USD 110  USD110 In stock
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Quality Control & Documentation
Biological Activity

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.

Product Citations
Customer Product Validations & Biological Datas
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
Protocol (for reference only)
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
Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Allen JE, et al. Sci Transl Med. Dual inactivation of Akt and ERK by TIC10 signals Foxo3a nuclear translocation, TRAIL gene induction, and potent antitumor effects.

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Keywords: TIC10, ONC-201; Dordaviprone supplier, Akt, inhibitors, activators


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