| Bioactivity | 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 | ||||||||||||
| Invitro | 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: | ||||||||||||
| In Vivo | ONC206 (100 mg/kg;p.o.; every 10 days) causes significant tumor growth inhibition[2]. | ||||||||||||
| Name | ONC206 | ||||||||||||
| CAS | 1638178-87-6 | ||||||||||||
| Formula | C23H22F2N4O | ||||||||||||
| Molar Mass | 408.44 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |