Drug intelligence / Profile preview

ER520

Development stage
Preclinical
Modality
Small Molecules
01

Overview

ER520 is a patented derivative of indenoisoquinoline investigated as a selective modulator of estrogen receptor subtypes. It inhibits the expression of ERα and increases ERβ protein levels in breast cancer (MCF-7) and endometrial carcinoma (Ishikawa) cells. ER520 suppresses proliferation, adhesion, migration, and invasion of these cancer cell lines, reduces VEGF secretion, inhibits tube formation and angiogenesis in vitro and in vivo, and limits tumor growth in nude mice. It has been proposed as an antineoplastic and antiangiogenic agent with potential applications in cancer therapy, particularly breast cancer and angiogenesis inhibition[1].

02

Targets

VEGFR-1 (Vascular endothelial growth factor receptor 1)ESR1 (ERα)ESR2 (ERβ)

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