EG01377 2HCl

SKU: orb1819294

Description

EG01377 2HCl is a potent and selective neuropilin-1 (NRP1) inhibitor with a Kd of 1.32 µM and an IC50 of 609 nM. This small molecule exhibits anti-angiogenic and antimigratory properties, demonstrating antitumor efficacy in both cellular assays and in vivo models of cancer research.

Research Area

Immunology & Inflammation

Key Properties

• CAS Number: 2749438-61-5
• MW: 659.6
• Purity: 99.56% (May vary between batches)
• Formula: C₂₆H₃₂Cl₂N₆O₆S₂
• SMILES: N=C(N)NCCC[C@@H](C(O)=O)NC(C(SC=C1)=C1NS(=O)(C2=C3C(CCO3)=CC(C4=CC=C(C=C4)CN)=C2)=O)=O.Cl.Cl
• Target: Complement System
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (7.58 mM);DMSO:180 mg/mL (272.89 mM)

Bioactivity

• Target IC50:
  NRP1-a1 and NRP1-b:609 nM
• In Vivo:
  EG0 1377 2HCl (2 mg/kg; i.v.; BABL/c female mice) possesses a half-life of 4.29 hours, allowing for once-a-day dosing to be maintained in mice.
• In Vitro:
  EG0 1377 2HCl (30 μM) effectively diminishes HUVEC cell migration induced by VEGFA. Additionally, EG01377 2HCl leads to reductions in network area, length, and branching points. EG0 1377 2HCl (3-30 μM; 30 minutes) inhibits vascular endothelial growth factor A (VEGF-A) stimulated tyrosine phosphorylation of VEGF-R2/KDR with an IC50 of 30 μM. EG0 1377 2HCl (30 μM; 5 days) can delay the VEGF-induced wound closure. EG0 1377 2HCl diminishes VEGF-triggered angiogenesis. Moreover, when combined with VEGFA, EG01377 2HCl curtails spheroid outgrowth of A375P (malignant melanoma) cells. EG0 1377 2HCl (500 nM; 2 h) 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

neuropilin-1(NRP1), EG 01377, EG01377, EG-01377, EG01377 2HCl, EG01377 2HCl(2227996-00-9 Free base), Complement System, ComplementSystem

Compound Identifiers

PubChem CID

146681179