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Dordaviprone
- ONC201 - TIC10 active isomer - Angular TIC10
- Soluble in DMSO
- MF: C24H26N4O
- MW: 386.49
Description
Dordaviprone (ONC201) is the bioactive angular TIC10 isomer and a stable, orally active small molecule that transcriptionally induces TRAIL in a p53-independent manner. It inactivates Akt and ERK signaling, promotes Foxo3a nuclear translocation and up-regulates TRAIL gene expression.
TRAIL pathway activation and stress-signaling modulation are important mechanisms in anticancer pharmacology. Dordaviprone/ONC201 is useful for studying p53-independent apoptosis, Akt/ERK-Foxo3a signaling and TRAIL-mediated tumor-cell responses.
Key Features
- Bioactive angular TIC10 isomer
- Transcriptionally induces TRAIL
- Acts through Akt/ERK inhibition and Foxo3a translocation
- p53-independent anticancer mechanism
Applications
- TRAIL pathway research
- Cancer apoptosis studies
- Akt/ERK signaling assays
- p53-independent antitumor mechanism studies
Promotion: Dordaviprone is also related to ONC212 (Axon 3581), an available analogue for comparative TRAIL-pathway research.
More Information
| Parent CAS No. | 1616632-77-9 |
|---|---|
| Chemical Name | 7-benzyl-4-(2-methylbenzyl)-1,2,6,7,8,9-hexahydroimidazo[1,2-a]pyrido[3,4-e]pyrimidin-5(4H)-one |
| SMILES | C1C=C(CN2CC3C(=O)N(CC4C(C)=CC=CC=4)C4=NCCN4C=3CC2)C=CC=1 |
| MFCD | N.A. |
| InChi | InChI=1S/C24H26N4O/c1-18-7-5-6-10-20(18)16-28-23(29)21-17-26(15-19-8-3-2-4-9-19)13-11-22(21)27-14-12-25-24(27)28/h2-10H,11-17H2,1H3 |
| InChiKey | VLULRUCCHYVXOH-UHFFFAOYSA-N |
| CID | 73777259 |
| Short Description | TRAIL activator |
References
- N.T. Jacob et al. Pharmacophore Reassignment for Induction of the Immunosurveillance Cytokine TRAIL. Angew. Chem. 2014, 126, 6746 –6749.
- J.E. Allen et al. Dual Inactivation of Akt and ERK by TIC10 Signals Foxo3a Nuclear Translocation, TRAIL Gene Induction, and Potent Antitumor Effects. Sci. Transl. Med. 2013, 5, 171ra17.
- J.E. Allen. Efficacy and mechanistic evaluation of TIC10, a novel antitumor agent. Dissertation Univ. Pennsylvania 2012.
- VV Prabhu et al. Small-Molecule ONC201/TIC10 Targets Chemotherapy-Resistant Colorectal Cancer Stem-like Cells in an Akt/Foxo3a/TRAIL-Dependent Manner. Cancer Res. 2015 Apr 1;75(7):1423-32.
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