产品
编 号:F741757
分子式:C26H32Cl2N6O6S2
分子量:659.6
产品类型
结构图
CAS No: 2749438-61-5
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产品详情
生物活性:
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.
体内研究:
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.
体外研究:
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.