E7820 (E-7820) is a unique, oral sulfonamide derivative angiogenesis inhibitor, inhibits integrin α2 (ITGA2) mRNA expression and suppresses tube formation through the suppression of integrin alpha2.
E7820 inhibited in vitro proliferation and tube formation of human umbilical vascular endothelial cell (HUVEC).
E7820 decreased integrin alpha2, 3, 5, and beta1 in confluent culture of HUVEC, and integrin alpha2 was initially suppressed in mRNA level, followed by decrement of integrins alpha3, 5, and beta1.
E7820 reduced integrin alpha2 expression on a megakaryocytic cell line, Dami cells, induced by phorbol 12-myristate 13-acetate treatment.
Oral administration of E7820 significantly inhibited basic fibroblast growth factor-induced angiogenesis in Matrigel implants and human colon WiDr tumor-induced angiogenesis in a dorsal air sac model.
E7820 showed a broad-spectrum antitumor effect in mice through inhibition of angiogenesis.