Identification | Back Directory | [Name]
N-[3-(1,3-benzodioxol-5-yl)-3-(2-methoxyphenyl)propyl]-N-benzylpropanamide | [CAS]
330834-54-3 | [Synonyms]
N-[3-(1,3-benzodioxol-5-yl)-3-(2-methoxyphenyl)propyl]-N-benzylpropanamide | [Molecular Formula]
C27H29NO4 | [MDL Number]
MFCD02241518 | [MOL File]
330834-54-3.mol | [Molecular Weight]
431.523 |
Chemical Properties | Back Directory | [Boiling point ]
609.4±55.0 °C(Predicted) | [density ]
1.169±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 250 mg/mL (579.35 mM); Ethanol: 100 mg/mL (231.74 mM); Water: < 0.1 mg/mL (insoluble) | [form ]
Oil | [pka]
-0.50±0.70(Predicted) | [color ]
Light yellow to yellow |
Hazard Information | Back Directory | [Uses]
AGX51 is the first-in-class pan-Id (inhibitors of DNA-binding/differentiation proteins) antagonist and degrader. AGX51 inhibits Id1-E47 interaction, leading to ubiquitin-mediated degradation of Ids, cell growth arrest, and viability reduction. AGX51 can inhibit TNBC and has an IC50 of about 25 nM. AGX51 can be used in cancer research. | [Biological Activity]
AGX51 is an antagonist th at blocks transcriptional regulators ID1-4 from binding basic helix-loop-helix (bHLH) transcription factor E47causing ubiquitin-mediated degradation of IDs (10-40 μM for 2-48h; HCT116). AGX51 reduces cell viabilityG0/G1 growth arrestand a reduction in cyclin D1 levels in cultures (5-40 μM for 4-24h; HUVEC and HCT116) and suppresses ocular neovascularization in mouse models of age-related macular degeneration (AMD) and retinopathy of prematurity (ROP) in vivo (500 μg/mouse via twice daily i.p. or 1-30 μg/eye via intravitreal injection immediately and 7 days after rupture of Bruch's membrane). | [in vivo]
AGX51 (50 mg/kg; i.p. twice a day for 4 weeks) inhibits lung metastasis[1].
AGX51 (15 mg/kg; i.p. twice a day for 3 weeks) exibits anti-tumor activity with autochronous cancer[1]. Animal Model: | Balb/c mice with luciferase-labeled 4T1 cells[1] | Dosage: | 50 mg/kg | Administration: | Intraperitoneal injection; 60 mg/kg twice a day; for 4 weeks | Result: | Inhibited lung metastasis development. |
Animal Model: | A/J mice with AOM colon tumor model[1] | Dosage: | 15 mg/kg | Administration: | Intraperitoneal injection; 15 mg/kg twice a day; for 3 weeks | Result: | Dreased the colon tumors and exhibited anti-tumor activity in AOM colon tumor mice. |
| [References]
[1] Wojnarowicz PM, et al. Anti-tumor effects of an ID antagonist with no observed acquired resistance. NPJ Breast Cancer. 2021 May 24;7(1):58. DOI:10.1038/s41523-021-00266-0 |
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