| Bioactivity | TIC10 (ONC-201) is a potent, orally active, and stable tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) inducer which acts by inhibiting Akt and ERK, consequently activating Foxo3a and significantly inducing cell surface TRAIL. TIC10 can cross the blood-brain barrier[1]. | ||||||||||||
| Invitro | TIC10 transcriptionally induces TRAIL in a p53-independent manner and crosses the blood-brain barrier[1]. TIC10 induces a sustained up-regulation of TRAIL in tumors and normal cells that may contribute to the demonstrable antitumor activity of TIC10[1]. TIC10 inactivates kinases Akt and extracellular signal-regulated kinase (ERK), leading to the translocation of Foxo3a into the nucleus, where it binds to the TRAIL promoter to up-regulate gene transcription[1]. TIC10 is an efficacious antitumor therapeutic agent that acts on tumor cells and their micro-environment to enhance the concentrations of the endogenous tumor suppressor TRAIL[1]. TIC10 also causes a down-regulation of the total expression of ERK[1]. | ||||||||||||
| Name | Dordaviprone | ||||||||||||
| CAS | 1616632-77-9 | ||||||||||||
| Formula | C24H26N4O | ||||||||||||
| Molar Mass | 386.49 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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Dordaviprone
CAS: 1616632-77-9 F: C24H26N4O W: 386.49
TIC10 (ONC-201) is a potent, orally active, and stable tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) i
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