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ONC201

Chemical Structure : ONC201

CAS No.: 1616632-77-9

ONC201 (Dordaviprone, TIC10, ONC-201)

Catalog No.: PC-61649Not For Human Use, Lab Use Only.

ONC201 (Dordaviprone, TIC10, ONC-201) is a potent, orally active, and brain-permeable small molecule that transcriptionally induces TRAIL in a p53-independent manner, a selective dopamine receptor D2 (DRD2) antagonist.

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Biological Activity

ONC201 (Dordaviprone, TIC10, ONC-201) is a potent, orally active, and brain-permeable small molecule that transcriptionally induces TRAIL in a p53-independent manner, a selective dopamine receptor D2 (DRD2) antagonist.
ONC201 induces a sustained up-regulation of TRAIL in tumors and normal cells, inactivates kinases Akt and ERK, leading to the translocation of Foxo3a into the nucleus.
ONC201 is an efficacious antitumor therapeutic agent that acts on tumor cells and their microenvironment to enhance the concentrations of the endogenous tumor suppressor TRAIL.

Physicochemical Properties

M.Wt 386.50
Formula C24H26N4O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2,4,6,7,8,9-hexahydro-4-[(2-methylphenyl)methyl]-7-(phenylmethyl)-imidazo[1,2-a]pyrido[3,4-e]pyrimidin-5(1H)-one

References

1. Allen JE, et al. Sci Transl Med. 2013 Feb 6;5(171):171ra17.

2. Prabhu VV, et al. Cancer Res. 2015 Apr 1;75(7):1423-32.

3. Allen JE, et al. Cancer Res. 2015 Apr 15;75(8):1668-74.

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