EG01377 是有效的、可生物利用的和选择性的neuropilin-1 (NRP1)抑制剂，Kd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。
| 生物活性 | EG01377 is a potent, bioavailable and selective inhibitor ofneuropilin-1 (NRP1), with aKdof 1.32 μM, andIC50s of both 609 nM forNRP1-a1andNRP1-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] |
体外研究
(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].
Western Blot Analysis[1] | Cell Line: | Human umbilical vein endothelial cells (HUVECs) | | Concentration: | 3, 10, 30 μM | | Incubation Time: | 30 minutes | | Result: | Inhibited VEGF-A stimulated tyrosine phosphorylation of VEGF-R2/KDR with an IC50of 30 μM. |
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体内研究
(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].
| Animal Model: | 6–8 week-old BABL/c female mice[1] | | Dosage: | 2 mg/kg (Pharmacokinetic Analysis) | | Administration: | I.v. administration | | Result: | The half time (T1/2) of 4.29 h. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
