EG 01377)
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- CAS号:
- 2227996-00-9
- 英文名:
- EG 01377)
- 英文别名:
- EG 01377);EG01377 free base;EG01377
(EG-01377;L-Arginine, N2-[[3-[[[5-[4-(aminomethyl)phenyl]-2,3-dihydro-7-benzofuranyl]sulfonyl]amino]-2-thienyl]carbonyl]-
- 中文名:
- EG 01377)
- 中文别名:
- 化合物 T11154
- CBNumber:
- CB74844748
- 分子式:
- C26H30N6O6S2
- 分子量:
- 586.68
- MOL File:
- 2227996-00-9.mol
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EG 01377)化学性质
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密度:
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1.56±0.1 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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Soluble in DMSO
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酸度系数(pKa):
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3.40±0.21(Predicted)
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EG 01377)性质、用途与生产工艺
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。
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
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regulatory T-cell SMAD3/AKT (Tregs) in the presence of tumor cell-derived factors.
Western Blot Analysis
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Cell Line:
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Human umbilical vein endothelial cells (HUVECs)
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Concentration:
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3, 10, 30 μM
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Incubation Time:
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30 minutes
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Result:
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Inhibited VEGF-A stimulated tyrosine phosphorylation of VEGF-R2/KDR with an IC
50
of 30 μM.
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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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Animal Model:
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6–8 week-old BABL/c female mice
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Dosage:
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2 mg/kg (Pharmacokinetic Analysis)
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Administration:
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I.v. administration
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Result:
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The half time (T
1/2
) of 4.29 h.
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EG 01377)
上下游产品信息
上游原料
下游产品
2227996-00-9, EG 01377) 相关搜索:
- 化合物 T11154
- 2227996-00-9
- L-Arginine, N2-[[3-[[[5-[4-(aminomethyl)phenyl]-2,3-dihydro-7-benzofuranyl]sulfonyl]amino]-2-thienyl]carbonyl]-
- EG01377 free base
- EG01377
(EG-01377
- EG 01377)