E7820

SKU: orb1302862

Description

E7820 is a small molecule angiogenesis inhibitor that functions by targeting and suppressing integrin α2, a key adhesion molecule on endothelial cells. It has been utilized in both in vitro and in vivo research to study tumor angiogenesis and metastasis in cancer models.

Research Area

Cardiovascular Research, Cell Biology, Protein Biochemistry

Key Properties

• CAS Number: 289483-69-8
• MW: 336.4
• Purity: >98%
• Formula: C₁₇H₁₂N₄O₂S
• SMILES: Cc1ccc(NS(=O)(=O)c2cccc(c2)C#N)c2[nH]cc(C#N)c12
• Target: Molecular glue
• Solubility: Soluble in DMSO (up to at least 25 mg/ml)

Bioactivity

• In Vivo:
  E7820 (50 mg/kg) with erlotinib has a significantly synergistic antitumor effect in three xenograft models without severe body weight loss. E7820 (50 mg/kg) and erlotinib decrease MVD and enhance apoptosis in tumor-associated endothelial cells, inhibit tumor cell proliferation and enhanced apoptosis, and enhance inhibition of cell proliferation and apoptosis through activation of both intrinsic and extrinsic apoptosis pathways in human NSCLC xenograft models. E7820 shows anti-tumor activity at doses of 50, 100, and 200 mg/kg in the tumor growth and α2-integrin expression experiments. E7820 (50, 100, and 200 mg/kg) inhibits tumor growth in a dose-dependent manner in all s.c. xenograft models. E7820 completely inhibits s.c. tumor growth of LoVo tumor cells and also regresses the tumor mass of KP-1 tumor cells at the dosages of both 100 and 200 mg/kg.
• In Vitro:
  E7820 inhibits proliferation of HUVEC induced by either bFGF (IC50: 0.10 μg/mL) and VEGF (IC50: 0.081 μg/mL) in serum-free medium. E7820 also inhibits both bFGF- (IC50: 0.20 μg/mL) and VEGF-driven (IC50: 0.24 μg/mL) tube formation of HUVEC in this assay.

Storage & Handling

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

Alternative Names

derivative, E7820, E-7820, E 7820, cell, colorectal, LoVo, inhibit, HUVEC, Inhibitor, Integrin, integrin a2, ER68203-00, endothelium, WiDr, sulfonamide, tumor

Compound Identifiers

PubChem CID

196970