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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 COA & MSDSRelated productsDatasheet
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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