EG01377

EG01377 is a potent, bioavailable and selective inhibitor of neuropilin-1 (NRP1), with a K_d of 1.32 μM, and IC₅₀s of both 609 nM for NRP1-a1 and NRP1-b1. EG01377 has antiangiogenic, antimigratory, and antitumor effects^[1]. IC50 & Target: IC50: 609 nM (NRP1-a1 and NRP1-b)^[1] Kd: 1.32 μM (NRP1-b1)^[1] In Vitro: EG01377 (3-30 μM; 30 minutes) inhibits vascular endothelial growth factor A (VEGF-A) stimulated tyrosine phosphorylation of VEGF-R2/KDR^[1].
EG01377 (30 μM) is able to significantly reduce HUVEC cell migration in response to VEGFA^[1].
EG01377 (30 μM; 5 days) can delay the VEGF-induced wound closure^[1].
EG01377 (30 μM) reduces network area, length, and branching points^[1].
EG01377 (30 μM; 7 days) reduces VEGF-induced angiogenesis^[1].
EG01377 (30 μM; 7 days) in combination with VEGFA reduces A375P (malignant melanoma) spheroid outgrowth^[1].
EG01377 (500 nM; 2 hours) blocks the production of transforming growth factor beta (TGFβ) by Nrp1⁺ regulatory T-cell SMAD3/AKT (Tregs) in the presence of tumor cell-derived factors^[1].
In Vivo: EG01377 (2 mg/kg; i.v.) exhibits an encouraging half-life of 4.29 h, sufficient to sustain once per day dosing in mice^[1].