AGX51

SKU: orb1940831

Description

AGX51 is an antagonist of inhibitor of DNA binding (ID) proteins. AGX51 treatment lead to pan-Id degradation, cell cycle arrest, and cell death.(In Vitro):AGX51 inhibits the Id1-E47 interaction. AGX51 is well-tolerated in mice and phenocopies the genetic loss of Id expression in AMD and ROP models by inhibiting retinal neovascularization. AGX51 may have utility in the management of multiple diseases.

Key Properties

• CAS Number: 330834-54-3
• MW: 431.532
• Purity: >98% (HPLC)
• Formula: C₂₇H₂₉NO₄
• SMILES: CCC(=O)N(CCC(c1ccc2OCOc2c1)c1ccccc1OC)Cc1ccccc1
• Target: Parasite| Sodium Channel
• Solubility: In Vitro: DMSO : 100 mg/mL (231.74 mM)

Bioactivity

• In Vivo:
  Animal model: Balb/c mice with luciferase-labeled 4T1 cells. 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. 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.
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• In Vitro:
  Western blot analysis. Cell line: 4T1 cells. Concentration: 0, 5, 10, 20, 40 and 80 μM. Incubation time: 24 hours. Result: Decreased ID1 protein levels starting at a concentration of 40 μM in 4T1 cells. Western blot analysis. Cell line: 4T1 cells. Concentration: 40 μM. Incubation time: 0, 2, 4, 8, 12, 24, 48 and 72 hours. Result: Decreased ID1 protein levels starting at 4 h, while until 24 h ID1 protein completely loss. Cell Viability Assay Cell line: 4T1 cells, HMLE RAS Twist, MDA-MB-157, MDA-MB-436, MDA-MB-231, MDA-MB-453, BT-474, MDA-MB-361, SK-BR-3, MCF-7, T47-D, PDX-BR7, PDX-IBT and PDX-BR11. Concentration: 40 μM. Incubation time: 24 hours. Result: Inhibited 4T1, HMLE RAS Twist, MDA-MB-157, MDA-MB-436, SK-BR-3, MCF-7, PDX-BR7, PDX-IBT and PDX-BR11 cell lines with IC50s of 26.66, 8.7, 22.28, 30.91, 36.55, 60, 10.89, 11.97 and 18.56 μM, respectively. Cell Cycle Analysis Cell line: 4T1 cells. Concentration: 40 μM. Incubation time: 24 and 48 hours. Result: Affected cell cycle of 4T1 cells with a G0/G1 phase accumulation. Cell Viability Assay Cell line: 4T1 cells. Concentration: 40 μM. Incubation time: 4 and 24 hours. Result: Reduced phospho-histone H3 levels in 4T1 cells. Cell Viability Assay Cell line: 4T1 cells. Concentration: 40 μM. Incubation time: 24 hours. Result: Increased ROS level of 4T1 cells and indicated ROS production is a main mechanism of cell killing.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

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Gene Symbol

Parasite| Sodium Channel