E7820 (ER68203-00), an orally active aromatic sulfonamide derivative, is a unique angiogenesis inhibitor suppressing an expression of integrin alpha2 subunit on endothelium. E7820 inhibits rat aorta angiogenesis with an IC50 of 0.11 μg/ml. E7820 modulates α-1, α-2, α-3, and α-5 integrin mRNA expression.

E7820 (ER68203-00), an orally active aromatic sulfonamide derivative, is a unique angiogenesis inhibitor suppressing an expression of integrin alpha2 subunit on endothelium. E7820 inhibits rat aorta angiogenesis with an IC50 of 0.11 μg/ml. E7820 modulates α-1, α-2, α-3, and α-5 integrin mRNA expression. Antiangiogenic and antitumor activity.

2005年6月1日 · E7820 is a potent inhibitor of endothelial cell proliferation and vascular tube formation in vitro, and it effectively inhibits the growth of human breast and pancreatic cancer xenografts.

2011年1月1日 · The recommended phase II dose of E7820 is 100 mg/d, based on a fasting schedule. E7820 downregulates integrin α-2 expression in surrogate tissues (platelets) and is associated with stable disease in a wide variety of heavily pretreated malignancies.

E7820 is a novel angiogenesis inhibitor, which modulates integrinα2 expression on endothelial cells and shows anti-tumor activity in a variety of xenograft models in nude mice.

E 7820 is a α 2 integrin inhibitor. Inhibits angiogenesis in vitro (IC 50 = 0.11 - 0.25 μM). Also inhibits growth of human colorectal cancer cell lines. Enhances efficacy of erlotinib in a non-small-cell lung cancer xenograft model. Also acts as a molecular glue to induce proteosomal degradation of mRNA splicing factor RBM39.

2021年5月18日 · Currently the application of E7820 in the treatment of various malignancies including pancreas carcinoma and breast cancer is being investigated in pre-clinical and clinical trials. It has been shown, that integrin α2 deficiency has beneficial effects on bone homeostasis in …

Synthetic sulfonamide anticancer drugs, including E7820, indisulam, tasisulam, and chloroquinoxaline sulfonamide, exhibit diverse mechanisms of action and therapeutic potential, functioning as molecular glue degraders. E7820 targets RBM39, affecting RNA splicing and angiogenesis by suppressing integrin α2.

E7820 [N - (3-cyano-4-methyl-1 H -indol-7-yl)-3-cyanobenzene-sulfonamide] is a first-in-class, orally available aromatic sulfonamide derivative that inhibits the proliferation and tube formation of human umbilical vein cells induced by either basic fibroblast growth factor or VEGF (12).

Here we report that a novel angiogenesis inhibitor, E7820 (an aromatic sulfonamide derivative), inhibited in vitro proliferation and tube formation of human umbilical vascular endothelial cell (HUVEC).