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Chemical Structure| 1638178-87-6 Chemical Structure| 1638178-87-6

Structure of ONC206
CAS No.: 1638178-87-6

Chemical Structure| 1638178-87-6

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ONC206 is an analogue of ONC201. ONC206 is a selective antagonist of dopamine D2-like receptors (DRD2/3/4) with nanomolar potency. ONC206 exhibits broad-spectrum antitumor activity.

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Product Details of ONC206

CAS No. :1638178-87-6
Formula : C23H22F2N4O
M.W : 408.44
SMILES Code : O=C1N(CC2=CC=C(F)C=C2F)C3=NCCN3C4=C1CN(CC5=CC=CC=C5)CC4
MDL No. :MFCD32671364

Safety of ONC206

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Related Pathways of ONC206

GPCR

Isoform Comparison

Biological Activity

Description
ONC206 is a derivative of the TRAIL inducer ONC201[1].
Target
  • D2 receptor

In Vitro:

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.

In Vivo:

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. Neoplasia. 2024 Sep;55:101015.

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT04541082 Central Nervous System Neoplas... More >>ms|Glioblastoma|Gliosarcoma, Adult|Anaplastic Oligodendroglioma|Anaplastic Astrocytoma|Pilocytic Astrocytoma|Oligodendroglioma|Gliomatosis Cerebri|Pleomorphic Xanthoastrocytoma|Anaplastic Pleomorphic Xanthoastrocytoma|Diffuse Midline Glioma, H3 K27M-Mutant|Ependymoma|Ependymoma, Anaplastic|Medulloblastoma|Teratoid Rhabdoid Tumor|Neuroectodermal Tumors, Primitive|Neuroectodermal Tumors|Anaplastic Meningioma|Atypical Meningioma|Choroid Plexus Neoplasms|Pineal Tumor|Diffuse Astrocytoma|Glial Tumor Less << PHASE1 RECRUITING 2025-12-26 National Institutes of Health,... More >> Bethesda, Maryland, 20892, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.45mL

0.49mL

0.24mL

12.24mL

2.45mL

1.22mL

24.48mL

4.90mL

2.45mL

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