Chemical Structure : ONC212
CAS No.: 1807861-48-8
Catalog No.: PC-72443Not For Human Use, Lab Use Only.
ONC212 (ONC-212) is a potent anti-cancer small molecule, activator of an orphan GPCR GPR132 and Gαq signaling, also is a potent activator of ClpP activator with EC50 of 131 nM.
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5 mg | $98 | In stock | |
10 mg | $148 | In stock | |
25 mg | $258 | In stock | |
50 mg | $428 | In stock | |
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ONC212 (ONC-212) is a potent anti-cancer small molecule, activator of an orphan GPCR GPR132 and Gαq signaling, also is a potent activator of ClpP activator with EC50 of 131 nM.
ONC212 possesses highly increased antitumor activity compared to the first-generation compound ONC201.
ONC212 induced apoptogenic effects through the induction of an integrated stress response, and reduced MCL-1 expression.
Oral administration of ONC212 inhibited AML growth in vivo and improved overall survival in xenografted mice.
ONC212 exhibited broad-spectrum efficacy at nanomolar concentrations across solid tumors and hematological malignancies.
ONC212 impairs oxidative phosphorylation (OXPHOS) with decrease in mitochondrial-derived ATP production, mitochondrial protease ClpP was identified as an ONC212-binding target.
M.Wt | 440.47 | |
Formula | C24H23F3N4O | |
Appearance | Solid | |
Storage |
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Solubility |
100 mM in DMSO (44 mg/mL) |
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Chemical Name/SMILES |
2,4,6,7,8,9-Hexahydro-7-(phenylmethyl)-4-[[4-(trifluoromethyl)phenyl]methyl]imidazo[1,2-a]pyrido[3,4-e]pyrimidin-5(1H)-one |
1. Nii T, et al. Leukemia. 2019 Dec;33(12):2805-2816.
2. Wagner J, et al. Cell Cycle. 2017 Oct 2;16(19):1790-1799.
3. Lev A, et al. Oncotarget. 2017 Sep 12;8(47):81776-81793.
4. Ferrarini I, et al. Mol Cancer Ther. 2021 Sep;20(9):1572-1583.
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