| Identification | Back Directory | [Name]
1-(ethylthio)-4-phenethyl-4H-spiro[benzo[h][1,2,4]triazolo[4,3-a]quinazoline-6,1'-cyclohexan]-5(7H)-one | [CAS]
374101-64-1 | [Synonyms]
NR2F1 agonist 1
1-(ethylthio)-4-phenethyl-4H-spiro[benzo[h][1,2,4]triazolo[4,3-a]quinazoline-6,1'-cyclohexan]-5(7H)-one
Spiro[benzo[h][1,2,4]triazolo[4,3-a]quinazoline-6(4H),1'-cyclohexan]-5(7H)-one, 1-(ethylthio)-4-(2-phenylethyl)- | [Molecular Formula]
C28H30N4OS | [MOL File]
374101-64-1.mol | [Molecular Weight]
470.63 |
| Chemical Properties | Back Directory | [Boiling point ]
719.9±70.0 °C(Predicted) | [density ]
1.31±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
1.47±0.20(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
NR2F1 agonist 1, a nuclear receptor NR2F1 agonist, specifically activates dormancy programs in malignant cells. NR2F1 agonist 1 up-regulates NR2F1 and downstream target genes that regulate dormancy. NR2F1 agonist 1 induces neural crest-like and growth suppression in head and neck squamous cell carcinoma (HNSCC) via NR2F1 activation. NR2F1 agonist 1 inhibits tumor growth in a mouse primary tumor model[1]. | [in vivo]
NR2F1 agonist 1 (0.5 mg/kg/day; i.p.; 3 weeks) inhibits inhibits primary tumor growth and metastatic growth in lungs in mouse models[1].
| Animal Model: | BALB/c nu/nu mice bearing GFP-tagged T-HEp3 PDX cells[1] | | Dosage: | 0.5 mg/kg/day | | Administration: | Intraperitoneal injection; injected for 3 weeks or for 1 week followed by DMSO for 2 weeks | | Result: | Did not induce apoptosis of proliferating primary tumor cells, but exhibited metastasis inhibitory effect against T-HEp3 cells. |
| [References]
[1] Khalil BD, et al. An NR2F1-specific agonist suppresses metastasis by inducing cancer cell dormancy. J Exp Med. 2022 Jan 3;219(1):e20210836. DOI:10.1084/jem.20210836 |
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