E7820

SKU: orb1223163

Description

E7820 is a small molecule and aromatic sulfonamide derivative with potential antiangiogenic and antitumor activities. E7820 inhibits angiogenesis by suppressing integrin alpha 2, a cell adhesion molecule expressed on endothelial cells. Inhibition of integrin alpha 2 leads to an inhibition of cell-cell interactions, endothelial cell-matrix interactions, vascular endothelial cell proliferation and angiogenesis. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).(In Vitro):E7820 (ER68203-00) inhibits both bFGF- and VEGF-driven ube formation of human umbilical vascular endothelial cell (HUVEC) in a dose-dependent manner with IC50 of 0.20 and 0.24 μg/ml, respectively.E7820 inhibits proliferation of HUVEC induced by either bFGF or VEGF in serum-free medium (SFM). The IC50 values are 0.10 and 0.081 μg/ml, respectively. Antiproliferative activity of E7820 against both WiDr and LoVo cells is very weak compared with that against HUVEC. The values of IC50 were 29 and 15 μg/ml, respectively.(In Vivo):E7820 (ER68203-00) (50-200 mg/kg; p.o. ; twice daily for 14 days) delays the growth of WiDr cells inoculated s.c..E7820 (200-400 mg/kg; p.o.;once daily for 4 days) potently inhibits WiDr-induced angiogenesis.

Key Properties

• CAS Number: 289483-69-8
• MW: 336.37
• Purity: >98% (HPLC)
• Formula: C₁₇H₁₂N₄O₂S
• SMILES: Cc1ccc(NS(=O)(=O)c2cccc(c2)C#N)c2[nH]cc(C#N)c12
• Target: AChR
• Solubility: DMSO : ≥ 33 mg/mL; 98.11 mM

Bioactivity

• In Vivo:
  E7820 (ER68203-00) (50-200 mg/kg; p.o. ; twice daily for 14 days) delays the growth of WiDr cells inoculated s. c.. E7820 (200-400 mg/kg; p.o. ; once daily for 4 days) potently inhibits WiDr-induced angiogenesis. Animal model: Six-week-old female nude mice (KSN mice, WiDr-induced angiogenesis model). Dosage: 50, 100, 200 mg/kg. Administration: p.o. ; twice daily for 14 days from 2 days after inoculation of the tumor cells. Result: The antitumor effect was dose-dependent at 50, 100, and 200 mg/kg, and the tumor growth rates were 52%, 46%, and 27%, respectively.
• In Vitro:
  E7820 (ER68203-00) inhibits both bFGF- and VEGF-driven ube formation of human umbilical vascular endothelial cell (HUVEC) in a dose-dependent manner with IC50 of 0.20 and 0.24 μg/ml, respectively. E7820 inhibits proliferation of HUVEC induced by either bFGF or VEGF in serum-free medium (SFM). The IC50 values are 0.10 and 0.081 μg/ml, respectively. Antiproliferative activity of E7820 against both WiDr and LoVo cells is very weak compared with that against HUVEC. The values of IC50 were 29 and 15 μg/ml, respectively.

Storage & Handling

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

Alternative Names

E7820 | E-7820 | E 7820

Quick Database Links

Gene Symbol

AChR