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ONC206

  Cat. No.:  DC31427   Featured
Chemical Structure
1638178-87-6
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Field of application
ONC206 is a chemical analogue of ONC201. ONC206 is a benzyl-flurobenzyl imipridone that has highly potent activity in preclinical models of difficult-to-treat neuroendocrine tumors and sarcomas. ONC206 acts as a selective antagonist of DRD2 at nanomolar concentrations and has broad-spectrum anti-tumor activity. ONC206 may address tumor types where the properties of ONC201 do not permit for complete therapeutic engagement in vivo.
Chemicals PropertiesBiological activity Related products COA MSDS Datasheet
Cas No.: 1638178-87-6
Chemical Name: CID 135297777
Synonyms: ONC206;CID 135297777;7-Benzyl-4-(2,4-difluorobenzyl)-1,2,6,7,8,9-hexahydroimidazo[1,2-a]pyrido[3,4-e]pyrimidin-5(4H)-one;OW6LM47PNK
SMILES: O=C1C2CN(CCC=2N2C(=NCC2)N1CC1C(F)=CC(F)=CC=1)CC1C=CC=CC=1
Formula: C23H22F2N4O
M.Wt: 408.443791866302
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: ONC206 is an analogue of TRAIL inducer ONC201[1]. ONC206 is a selective antagonist of the D2-like dopamine receptors (DRD2/3/4) at nanomolar concentrations. ONC206 has broad-spectrum anti-tumor activity[2].
Target: DRD2/3/4[2]
In Vivo: ONC206 (100 mg/kg;p.o.; every 10 days) causes significant tumor growth inhibition[2].
In Vitro: ONC206 selectively antagonizes the D2-like (DRD2/3/4), but not the D1-like (DRD 1/5), subfamily of dopamine receptors[2]. ONC206 significantly inhibits tumor cell migration and invasion in vitro[1]. ONC206 (0.05 μM; Over 48 hours) inhibits migration of ONC201- and TRAIL-resistant HCT116 Bax−/− cells without inducing cell death or inhibiting cell proliferation[1]. ONC206 engages the ISR and TRAIL pathway leading to tumor growth arrest and cell death[1]. ONC206 does not induce cell cycle arrest in a colorectal cell line with acquired ONC201-resistance[1]. Cell Proliferation Assay[1] Cell Line: HCT116 cells Concentration: 0.05 μM Incubation Time: Over 48 hours Result: Inhibited migration of ONC201- and TRAIL-resistant HCT116 Bax−/− cells.
References: [1]. Wagner J, 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. [2]. Varun Vijay Prabhu, et al. Potent anti-cancer activity of the imipridone ONC206: A selective dopamine D2-like receptor antagonist. AACR Annual Meeting 2017, April 1-5, 2017; Washington, DC.
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