Product Name:CAS No.: Cat. No.:MWt:Formula:Purity :
TIC10 isomer41276-02-2HY-15615386.49C24H26N4O>98%
Solubility:DMSO
Mechanisms:
Pathways:PI3K/Akt/mTOR; Target:Akt
Pathways:MAPK/ERK Pathway; Target:ERK
Biological Activity:
TIC10 isomer(ONC201 isomer) is an isomer of TIC10; TIC10 is a potent, orally active, and stable smallmolecule that transcriptionally induces TRAIL in a p53-independent manner and crosses the blood-brainbarrier.
IC50 Value:
Target: Akt; ERK
TIC10 induces a sustained up-regulation of TRAIL in tumors and normal cells that may contribute to thedemonstrable antitumor activity of TIC10. TIC10 inactivates kinases Akt and extracellular signal-regulatedkinase (ERK), leading to the translocation of Foxo3a into the nucleus, where it binds to the TRAIL promoterto up-regulate gene transcription. TIC10 is an efficacious antitumor therapeutic agent that acts on tumorcells and their microenvironment to enhance the concentrations of the endogenous tumor suppressor TRAIL[1]....
References:
[1]. Allen, Joshua E.; Krigsfeld, Gabriel; Mayes, Patrick A. et al. Dual inactivation of Akt and ERK by TIC10signals Foxo3a nuclear translocation, TRAIL gene induction, and potent antitumor effects. ScienceTranslational Medicine (2013), 5(171), 171ra17, 14 pp..
[2]. Nicholas T. Jacob, et al. Pharmacophore Reassignment for Induction of the ImmunosurveillanceCytokine TRAIL. Angewandte Chemie . DOI: 10.1002/anie.201402133
Caution: Not fully tested. For research purposes only
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