EG01377 dihydrochloride 是有效的、可生物利用的和选择性的 neuropilin-1 (NRP1) 抑制剂，K_d 值为 1.32 μM，对 NRP1-a1 和 NRP1-b1 的 IC₅₀ 值均为 609 nM。EG01377 dihydrochloride 具有抗血管生成，抗迁移及抗肿瘤等活性。

EG01377 dihydrochloride is a potent, bioavailable and selective inhibitor of neuropilin-1 (NRP1), with a K d of 1.32 μM, and IC 50 s of 609 nM for both NRP1-a1 and NRP1-b1. EG01377 dihydrochloride has antiangiogenic, antimigratory, and antitumor effects.

Solid

IC50: 609 nM (NRP1-a1 and NRP1-b)

EG01377 (3-30 μM; 30 minutes) inhibits vascular endothelial growth factor A (VEGF-A) stimulated tyrosine phosphorylation of VEGF-R2/KDR.
EG01377 (30 μM) is able to significantly reduce HUVEC cell migration in response to VEGFA.
EG01377 (30 μM; 5 days) can delay the VEGF-induced wound closure.
EG01377 (30 μM) reduces network area, length, and branching points.
EG01377 (30 μM; 7 days) reduces VEGF-induced angiogenesis.
EG01377 (30 μM; 7 days) in combination with VEGFA reduces A375P (malignant melanoma) spheroid outgrowth.
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.
has not independently confirmed the accuracy of these methods. They are for reference only.<

EG01377 (2 mg/kg; i.v.) exhibits an encouraging half-life of 4.29 h, sufficient to sustain once per day dosing in mice. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 6-8 week-old BA

Room temperature in continental US; may vary elsewhere.

-20°C, stored under nitrogen, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

[1]. Powell J, et al. Small Molecule Neuropilin-1 Antagonists Combine Antiangiogenic and Antitumor Activity with Immune Modulation through Reduction of Transforming Growth Factor Beta (TGFβ) Production in Regulatory T-Cells. J Med Chem. 2018 May 10;61(9):4135-

In Vitro: DMSO : 200 mg/mL (303.21 mM; Need ultrasonic)配制储备液