ONC206 is a derivative of the TRAIL inducer ONC201[1]. ONC206 selectively antagonizes D2-like dopamine receptors (DRD2/3/4) at nanomolar concentrations. ONC206 exhibits wide-ranging antitumor efficacy[2].
体内研究
ONC206 (100 mg/kg;pO.; every 10 days) results in notable inhibition of tumor growth[2].
体外研究
ONC206 exhibits selective antagonism towards the D2-like (DRD2/3/4), rather than the D1-like (DRD1/5), subfamily of dopamine receptors[2].
ONC206 markedly suppresses tumor cell migration and invasion in vitro[1].
ONC206 (0.05 μM; for 48 hours) impedes the migration of ONC201- and TRAIL-resistant HCT116 Bax cells without eliciting cell death or hindering cell proliferation[1].
ONC206 activates the ISR and TRAIL pathway, resulting in tumor growth arrest and cell death[1].
ONC206 does not cause cell cycle arrest in a colorectal cell line that has developed resistance to ONC201[1].
ONC206 细胞实验
Cell Line
Concentration
Treated Time
Description
References
SF188
200 nM
24 hours
Evaluate the effect of ONC206 on glycolytic activity in SF188 cells, results showed ONC206 significantly suppressed baseline extracellular acidification rate (ECAR).
Clin Cancer Res. 2018 Nov 1;24(21):5392-5406.
GBM14
10 µM
24 hours
Evaluate the effect of ONC206 on GBM14 cell viability, results showed modest reduction in cell viability with ONC206 alone
Clin Cancer Res. 2022 May 2;28(9):1881-1895.
Hep3B
0.5 µM
24 hours
ONC206 inhibited Hep3B cell proliferation and induced apoptosis, accompanied by mitochondrial swelling and dysfunction.
Neoplasia. 2024 Sep;55:101015.
Huh7
1 µM
48 hours
ONC206 inhibited Huh7 cell proliferation and induced apoptosis, accompanied by mitochondrial swelling and dysfunction.
Neoplasia. 2024 Sep;55:101015.
U87
200 nM
72 hours
Evaluate the effect of ONC206 on the expression of anti-apoptotic proteins in U87 cells, results showed ONC206 significantly inhibited the expression of Bcl-2, Bcl-xL, and Mcl-1.
Clin Cancer Res. 2018 Nov 1;24(21):5392-5406.
NCH421k
200 nM
72 hours
Evaluate the apoptotic induction effect of ONC206 on NCH421k cells, results showed ONC206 significantly increased the proportion of apoptotic cells.
Clin Cancer Res. 2018 Nov 1;24(21):5392-5406.
NCH644
10 µM
72 hours
Evaluate the effect of ONC206 on NCH644 cell viability, results showed modest reduction in cell viability with ONC206 alone
Clin Cancer Res. 2022 May 2;28(9):1881-1895.
U251
10 µM
72 hours
Evaluate the effect of ONC206 on U251 cell viability, results showed modest reduction in cell viability with ONC206 alone
Clin Cancer Res. 2022 May 2;28(9):1881-1895.
HEC50 cells
0-10 µM
72 hours
ONC206 significantly inhibited HEC50 cell viability and induced apoptosis
Cancers (Basel). 2020 Aug 27;12(9):2436.
ARK2 cells
0-10 µM
72 hours
ONC206 significantly inhibited ARK2 cell viability and induced apoptosis
Cancers (Basel). 2020 Aug 27;12(9):2436.
ARK1 cells
0-10 µM
72 hours
ONC206 significantly inhibited ARK1 cell viability and induced apoptosis
Cancers (Basel). 2020 Aug 27;12(9):2436.
HEC-1A
0.31 µM
72 hours
ONC206 significantly inhibited HEC-1A cell proliferation with an IC50 of 0.31 µM.
Cancer Biol Ther. 2023 Dec 31;24(1):2202104.
ECC-1
0.19 µM
72 hours
ONC206 significantly inhibited ECC-1 cell proliferation with an IC50 of 0.19 µM.
Cancer Biol Ther. 2023 Dec 31;24(1):2202104.
OVCAR5
0.01 to 100 µM
72 hours
ONC206 inhibited cell proliferation with an IC50 of 0.18 μM, more potent than ONC201.
Am J Cancer Res. 2022 Feb 15;12(2):521-536.
SKOV3
0.01 to 100 µM
72 hours
ONC206 inhibited cell proliferation with an IC50 of 0.37 μM, more potent than ONC201.
Am J Cancer Res. 2022 Feb 15;12(2):521-536.
SPEC-2 cells
0.24 µM (IC50)
72 hours
ONC206 inhibits cell proliferation through DRD2/5 and TRAIL/DR5 pathways and shows more cytostatic function compared with ONC201 in SEC cells.
Front Oncol. 2020 Oct 20;10:577141.
ARK1 cells
0.33 µM (IC50)
72 hours
ONC206 inhibits cell proliferation through DRD2/5 and TRAIL/DR5 pathways and shows more cytostatic function compared with ONC201 in SEC cells.
Front Oncol. 2020 Oct 20;10:577141.
ONC206 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Nude mice
ARK1 cell xenograft model
Intraperitoneal injection
100 mg/kg
Twice per week for 6 weeks
ONC206 significantly reduced tumor burden and increased tumor cell apoptosis
Cancers (Basel). 2020 Aug 27;12(9):2436.
Mice
Lkb1fl/flp53fl/fl genetically engineered Mice model
Oral
100 mg/kg
Weekly for 4 weeks
ONC206 significantly reduced tumor weight in both obese and lean mice, with 84% reduction in obese and 77% in lean mice.
Cancer Biol Ther. 2023 Dec 31;24(1):2202104.
Mice
KpB Mice model
Oral gavage
125 mg/kg
Weekly for 4 weeks
ONC206 significantly inhibited ovarian tumor growth in both obese and non-obese mice, reducing tumor weight and volume.
Am J Cancer Res. 2022 Feb 15;12(2):521-536.
Nu/nu Mice
U87-EGFRvIII xenograft model
Intraperitoneal injection
50 mg/kg
Three times a week until the end of the experiment
Evaluate the anti-tumor effect of ONC206 in the U87-EGFRvIII model, results showed ONC206 significantly reduced tumor volume.
Clin Cancer Res. 2018 Nov 1;24(21):5392-5406.
SCID/SHO mice
GBM12 and GBM43 subcutaneous xenograft models
Intraperitoneal injection
50 mg/kg
Three times per week until the end of the experiment
Evaluate the effect of ONC206 on the growth of GBM12 and GBM43 subcutaneous tumors, results showed ONC206 alone had little impact on tumor growth
Clin Cancer Res. 2022 May 2;28(9):1881-1895.
Nude mice
Huh7 subcutaneous xenograft model
Intraperitoneal injection
80 mg/kg
Once daily for 20 days
ONC206 significantly inhibited the growth of Huh7 xenografts, reduced tumor volume and weight, and induced tumor cell apoptosis.
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