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GPCR/G Protein GHSR ONC212

ONC212

Catalog No. T7398   CAS 1807861-48-8

ONC212, a fluorinated-ONC201 analogue, is a selective agonist of GPR132.

ONC212, CAS 1807861-48-8
Pack Size Availability Price/USD Quantity
2 mg In stock 77.00
5 mg In stock 110.00
10 mg In stock 182.00
25 mg In stock 376.00
50 mg In stock 658.00
1 mL * 10 mM (in DMSO) In stock 120.00
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Purity 98.00%
Biological Description
Chemical Properties
Storage & Solubility Information
Description ONC212, a fluorinated-ONC201 analogue, is a selective agonist of GPR132.
Targets&IC50 GPR132,  
In vitro 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[1].
In vivo ONC212 is active in pancreatic cancer as single agent or in combination with 5-fluorouracil, irinotecan, oxaliplatin or RTK inhibitor crizotinib. Based on upregulation of pro-survival IGF1-R in some tumors, Founded an active combination of ONC212 with inhibitor AG1024, including in vivo[2].
Molecular Weight 440.46
Formula C24H23F3N4O
CAS No. 1807861-48-8

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 50 mg/mL (113.52 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. Nii T, Prabhu VV, Ruvolo V,et al.Imipridone ONC212 activates orphan G protein-coupled receptor GPR132 and integrated stress response in acute myeloid leukemia[J].Leukemia. 2019 Dec;33(12):2805-2816. 2. Lev A , Lulla A R , Wagner J , et al. Anti-pancreatic cancer activity of ONC212 involves the unfolded protein response (UPR) and is reduced by IGF1-R and GRP78/BIP.[J]. Oncotarget, 2017, 8(47):81776-81793.

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