ONC212

01/01/2021 - "ONC212 is a fluorinated imipridone with preclinical efficacy against pancreatic and other malignancies. "
01/01/2020 - "Our findings highlight ONC212 as a promising drug for targeting mitochondrial respiration in cancer."
12/01/2019 - "Comprehensive GPCR screening identified ONC212 as activator of an orphan GPCR GPR132 and Gαq signaling, which functions as a tumor suppressor. "
10/10/2017 - "We demonstrate ONC212 efficacy in 4 in-vivo models including ONC201-resistant tumors. "
10/02/2017 - "Orally administered ONC212 displayed potent anti-tumor effects in vivo, a broad therapeutic window and a favorable PK profile. "

11/01/2018 - ": Imipridones reduce the proliferation of patient-derived xenograft and stem-like glioblastoma cell cultures in vitro and in multiple xenograft models in vivo ONC212 displayed the highest potency. "
11/01/2018 - "Purpose: The goal of this study is to enhance the efficacy of imipridones, a novel class of AKT/ERK inhibitors that displayed limited therapeutic efficacy against glioblastoma (GBM).Experimental Design: Gene set enrichment, LC/MS, and extracellular flux analyses were used to determine the mechanism of action of novel imipridone compounds, ONC206 and ONC212. "

01/01/2021 - "In addition, novel agents, such as ONC212, have preclinical activity in pancreatic cancer, in part through autophagy inhibition. "
01/01/2021 - "We found ClpP is expressed in pancreatic cancer cells and is required for ONC212 cytotoxicity. "
01/01/2021 - "ONC212 is a Novel Mitocan Acting Synergistically with Glycolysis Inhibition in Pancreatic Cancer."
10/10/2017 - "We investigated efficacy of ONC201 and ONC212 against pancreatic cancer cell lines (N=16 including 9 PDX-cell lines). "
10/10/2017 - "We show a rationale for targeting pancreatic cancer using ONC212 combined with targeting the unfolded-protein response and ER chaperones such as GRP78/BIP. "

12/01/2019 - "In vitro studies using human acute myeloid leukemia (AML) cell lines, primary AML, and normal bone marrow (BM) samples demonstrate that ONC212 exerts prominent apoptogenic effects in AML, but not in normal BM cells, suggesting potential clinical utility. "
12/01/2019 - "Imipridone ONC212 activates orphan G protein-coupled receptor GPR132 and integrated stress response in acute myeloid leukemia."

01/01/2020 - "ONC212 reduced respiration in melanoma cells and HDFs, and inhibited the proliferation of melanoma cells. "
10/10/2017 - "ONC212, a fluorinated-ONC201 analogue, shows preclinical efficacy in melanoma and hepatocellular-cancer models. "
10/02/2017 - "ONC212 was efficacious in vivo in BRAF V600E melanoma models that are less sensitive to ONC201. "
01/01/2020 - "We also tested three clinically approved antibiotics, one anti-parasitic drug (pyrvinium pamoate), and a novel anti-cancer agent (ONC212) for effects on mitochondrial respiration and proliferation of melanoma cells and HDFs. "