EG 01377)
| 中文名稱 | EG 01377) |
|---|---|
| 中文同義詞 | 化合物 T11154;化合物 EG01377 |
| 英文名稱 | EG 01377) |
| 英文同義詞 | EG 01377);EG01377 (EG-01377;EG01377 free base;L-Arginine, N2-[[3-[[[5-[4-(aminomethyl)phenyl]-2,3-dihydro-7-benzofuranyl]sulfonyl]amino]-2-thienyl]carbonyl]- |
| CAS號 | 2227996-00-9 |
| 分子式 | C26H30N6O6S2 |
| 分子量 | 586.68 |
| EINECS號 | |
| 相關(guān)類別 | |
| Mol文件 | 2227996-00-9.mol |
| 結(jié)構(gòu)式 |  |
EG 01377) 性質(zhì)
| 密度 | 1.56±0.1 g/cm3(Predicted) |
|---|---|
| 儲存條件 | Store at -20°C |
| 溶解度 | 溶于二甲基亞砜 |
| 酸度系數(shù)(pKa) | 3.40±0.21(Predicted) |
IC50: 609 nM (NRP1-a1 and NRP1-b) Kd: 1.32 μM (NRP1-b1)
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.
Western Blot Analysis
| 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 IC 50 of 30 μM. |
EG01377 (2 mg/kg; i.v.) exhibits an encouraging half-life of 4.29 h, sufficient to sustain once per day dosing in mice.
| Animal Model: | 6–8 week-old BABL/c female mice |
| Dosage: | 2 mg/kg (Pharmacokinetic Analysis) |
| Administration: | I.v. administration |
| Result: | The half time (T 1/2 ) of 4.29 h. |