EG01377

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

EG01377 

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。

EG01377

EG01377 Chemical Structure

CAS No. : 2227996-00-9

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EG01377 的其他形式现货产品:

EG01377 dihydrochloride

生物活性

EG01377 is a potent, bioavailable and selective inhibitor of neuropilin-1 (NRP1), with a Kd of 1.32 μM, and IC50s of both 609 nM for NRP1-a1 and NRP1-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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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 IC50 of 30 μM.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

586.68

Formula

C26H30N6O6S2
CAS 号

2227996-00-9
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.
参考文献

  • [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):4135-4154.

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