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374101-64-1

374101-64-1 Structure

374101-64-1 Structure
IdentificationBack 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 PropertiesBack 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 InformationBack 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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