TIC10 Chemical Properties

Boiling point:

559.7±60.0 °C(Predicted)

Density 

1.24±0.1 g/cm3(Predicted)

storage temp. 

Sealed in dry,Store in freezer, under -20°C

solubility 

Soluble in DMSO (up to 25 mg/ml with warming).

pka

6.38±0.20(Predicted)

form 

solid

color 

Pale yellow

Stability:

Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 2 months.

TIC10 Usage And Synthesis

Description

TIC10 induces the expression of TNF-related apoptosis-inducing ligand (TRAIL) at 1-5 μM in a p53-independent manner. It is orally active, stable, and crosses the blood-brain barrier. The induction of TRAIL results from dual inhibition of Akt and ERK1/2 combined with nuclear translocation of the transcription factor FOXO3a. TIC10 suppresses the growth of orthotopic human glioblastoma multiforme tumors in mice.

Uses

7-Benzyl-4-(2-methylbenzyl)-1,2,6,7,8,9-hexahydroimidazo[1,2-a]pyrido[3,4-e]pyrimidin-5(4H)-one is used in biological studies for structure confirmation and pharmacophore reassignment for induction of immunosurveillance cytokine TRAIL in macrophages. The structure of this compound was misassigned for many years as H291055. The resolution of this issue was recently highlighted in Chemical and Engeneering News 92(23) 32 (2014).

References

1) Allen?et al.?(2013)?Dual Inactivation of Akt and ERK by TIC10 Signals Foxo3a Nuclear Translocation, TRAIL Gene Induction, and Potent Antitumor Effects, Sci. Transl. Med.?5?171ra17 2) Allen?et al.?(2015)?Identification of TRAIL-inducing compounds highlights small molecule ONC201/TIC10 as a unique anti-cancer agent that activates the TRAIL pathway,?Mol. Cancer.?14?99 3) Allen?et al.?(2016)?Discovery and Clinical Introduction of First-In-Class Imipridone ONC201, Oncotarget?7?74380 4) Ishizawa?et al.?(2019)?Mitochondrial ClpP-Mediated Proteolysis Induces Selective Cancer Cell Lethality, Cancer Cell?35?721

TIC10(1616632-77-9)Related Product Information

• Volasertib (BI 6727)
• NORFLUOXETINE HYDROCHLORIDE
• RESINIFERATOXIN
• Imiquimod
• Felodipine
• NYLON 6