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Medchemexpress LLC EG01377 dihydrochloride | 2749438-61-5 | 99.0% | 659.60 | 1 ML
Supplier: Medchemexpress LLC HY112151A10MM/1ML
EG01377 dihydrochloride is a potent, bioavailable, and selective inhibitor of neuropilin-1 (NRP1), with a Kd of 1.32 μM, and IC50s of 609 nM for both NRP1-a1 and NRP1-b1. It exhibits antiangiogenic, antimigratory, and antitumor effects.
- Inhibits vascular endothelial growth factor A (VEGF-A) stimulated tyrosine phosphorylation of VEGF-R2/KDR.
- Reduces HUVEC cell migration in response to VEGFA.
- Can delay VEGF-induced wound closure.
- Reduces network area, length, and branching points.
- Reduces VEGF-induced angiogenesis.
- Reduces A375P (malignant melanoma) spheroid outgrowth in combination with VEGFA.
- 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.
- Exhibits an encouraging half-life sufficient to sustain once per day dosing in mice.
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