hVEGF-IN-1

SKU: orb1223254

Description

hVEGF-IN-1 inhibits human VEGF-A translation and has antitumor activity.

Key Properties

• CAS Number: 1637443-98-1
• MW: 581.75
• Purity: >98% (HPLC)
• Formula: C₃₄H₄₃N₇O₂
• SMILES: CCN(CC)CCOc1ccc(cc1)Nc1nc(c2c(NC(=O)CCN3CCN(C)CC3)cccc2)nc2ccccc12
• Target: VEGF-A
• Solubility: DMSO : 25 mg/mL42.97 mM;H2O : < 0.1 mg/mL

Bioactivity

• In Vivo:
  hVEGF-IN-1 (compound 1) (7.5 mg/kg; i.p. once daily for 20 d) inhibits tumor growth in a human breast tumor xenograft. Animal model: BALB/c female nude mice were implanted MCF-7 cells. Dosage: 7.5 mg/kg. Administration: i.p. once daily for 20 days. Result: Reduced the tumor volume to <300 mm3.Reduced the tumor weight around 60.1% to a final weight of 0.18 g. Decreased the VEGF-A level in tumor tissue.
• In Vitro:
  hVEGF-IN-1 (compound 1) (1 nM-100 μM; 5 min) binds to IRES-A (WT) and IRES-A mutant RNA oligomer (IRES-MU1) with Kds of 1.29 and 13.4 μM by microscale thermophoresis (MST) measurements, respectively. hVEGF-IN-1 (0.375-3 μM; 0-24 h) reduces MDA-MB-231 cell migration approximately 25% at the concentration of 3 μM. hVEGF-IN-1 (0.1875-3 μM; 48 h) reduces the level of VEGF-A protein in MCF-7 cells. hVEGF-IN-1 (0.375-3 μM; 48 h) decreases the relative wound closure of migrated MCF-7 cells by ~35% at the concentration of 3 μM. hVEGF-IN-1 (1.25-10 μM) reduces the stability of the IRES-A G-Quadruplex in a dose-dependent manner. Western blot analysis. Cell line: MCF-7 cells. Concentration: 0.1875, 0.375, 0.75, 1.5, 3 μM Incubation time: 48 hours. Result: Down-regulated hVEGF-A expression.

Storage & Handling

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

Quick Database Links

Gene Symbol

VEGF-A