EG01377,2227996-00-9

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EG01377

CAS No. : 2227996-00-9

MCE 国际站：EG01377

产品活性：EG01377 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 具有抗血管生成，抗迁移及抗肿瘤等活性。

研究领域：Immunology/Inflammation

作用靶点：Complement System

In Vitro: 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.

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.

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