EG01377 2HCl

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

EG01377 dihydrochloride 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 dihydrochloride 具有抗血管生成，抗迁移及抗肿瘤等活性。

EG01377 dihydrochloride is a potent, bioavailable and selective inhibitor of neuropilin-1 (NRP1), with a Kd of 1.32 μM, and IC50s of 609 nM for both NRP1-a1 and NRP1-b1. EG01377 dihydrochloride has antiangiogenic, antimigratory, and antitumor effects.

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 IC50 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 (T1/2) of 4.29 h.

——

Immunology/Inflammation

Complement System

Complement System

——

——

2749438-61-5

659.6

C26H32Cl2N6O6S2

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 200 mg/mL (303.21 mM; 超声助溶 )

N=C(N)NCCC[C@@H](C(O)=O)NC(C(SC=C1)=C1NS(=O)(C2=C3C(CCO3)=CC(C4=CC=C(C=C4)CN)=C2)=O)=O.Cl.Cl

——

(-20℃)

With Ice Pack

≥ 2 years