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ONC212
- Soluble in 0.1N HCl(aq), DMSO and EtOH
- MF: C24H23F3N4O
- MW: 440.46
Description
ONC212 caused similar TRAIL/DR5 upregulation and activation of the integrated stress response as ONC201 (Axon 2300), with ONC212 having relatively rapid kinetics. ONC212 is also a mitocan acting on the ClpXP complex and causing collapse of mitochondrial bioenergetics. Moreover, ONC212 activates the orphan G protein-coupled receptor GPR132 and integrated stress response in acute myeloid leukemia.
More Information
| Parent CAS No. | 1807861-48-8 |
|---|---|
| Chemical Name | 7-Benzyl-4-(4-(trifluoromethyl)benzyl)-1,2,6,7,8,9-hexahydroimidazo[1,2-a]pyrido[3,4-e]pyrimidin-5(4H)-one |
| SMILES | C1C=C(C(F)(F)F)C=CC=1CN1C(=O)C2CN(CC3C=CC=CC=3)CCC=2N2CCN=C12 |
| MFCD | N.A. |
| InChi | InChI=1S/C24H23F3N4O/c25-24(26,27)19-8-6-18(7-9-19)15-31-22(32)20-16-29(14-17-4-2-1-3-5-17)12-10-21(20)30-13-11-28-23(30)31/h1-9H,10-16H2 |
| InChiKey | DFULPGUTXZTYKA-UHFFFAOYSA-N |
| CID | 124085867 |
| Short Description | TRAIL activator |
References
- J Wagner et al. Preclinical evaluation of the imipridone family, analogs of clinical stage anti-cancer small molecule ONC201, reveals potent anti-cancer effects of ONC212. Cell Cycle. 2017 Oct 2;16(19):1790-1799.
- I Ferrarini et al. ONC212 is a Novel Mitocan Acting Synergistically with Glycolysis Inhibition in Pancreatic Cancer. Mol Cancer Ther. 2021 Sep;20(9):1572-1583.
- T Nii et al. Imipridone ONC212 activates orphan G protein-coupled receptor GPR132 and integrated stress response in acute myeloid leukemia. Leukemia. 2019 Dec;33(12):2805-2816.
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