E 7820

E7820 is a α2 integrin inhibitor 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.

Product information

CAS Number: 289483-69-8

Molecular Weight: 336.37

Formula: C17H12N4O2S

Chemical Name: N-(3-cyano-4-methyl-1H-indol-7-yl)-3-cyanobenzene-sulfonamide

Smiles: CC1C=CC(NS(=O)(=O)C2=CC(=CC=C2)C#N)=C2NC=C(C#N)C2=1

InChiKey: LWGUASZLXHYWIV-UHFFFAOYSA-N

InChi: InChI=1S/C17H12N4O2S/c1-11-5-6-15(17-16(11)13(9-19)10-20-17)21-24(22,23)14-4-2-3-12(7-14)8-18/h2-7,10,20-21H,1H3

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO: 67 mg/mL(199.18 mM). Water: Insoluble.

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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.

References:

1. Funahashi Y, et al. Sulfonamide derivative, E7820, is a unique angiogenesis inhibitor suppressing an expression of integrin alpha2 subunit on endothelium. Cancer Res. 2002;62(21):6116-6123.
2. Ito K, et al. Enhanced anti-angiogenic effect of E7820 in combination with erlotinib in epidermal growth factor receptor-tyrosine kinase inhibitor-resistant non-small-cell lung cancer xenograft models. Cancer Sci. 2014;105(8):1023-1031.

Products are for research use only. Not for human use.