产品
编 号：F619104
分子式：C26H30N6O6S2
分子量：586.68
分子式：C26H30N6O6S2
分子量：586.68
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CAS No: 2227996-00-9
产品详情
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.
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.
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.
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.
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