Powder: -20°C for 3 years | In solvent: -80°C for 1 year
EG01377 2HCl is a potent, bioavailable and selective inhibitor of neuropilin-1 (NRP1) with a Kd value of 1.32 μM and an IC50 value of 609 nM for both EG01377 2HCl against NRP1-a1 and NRP1-b1.EG01377 exhibits anti-angiogenic, antimigratory and antitumor activities.
説明 | EG01377 2HCl is a potent, bioavailable and selective inhibitor of neuropilin-1 (NRP1) with a Kd value of 1.32 μM and an IC50 value of 609 nM for both EG01377 2HCl against NRP1-a1 and NRP1-b1.EG01377 exhibits anti-angiogenic, antimigratory and antitumor activities. |
ターゲット&IC50 | NRP1-a1 and NRP1-b:609 nM |
In vitro |
EG0 1377 2HCl (30 μM) effectively diminishes HUVEC cell migration induced by VEGFA. Additionally, EG01377 2HCl leads to reductions in network area, length, and branching points.[1] EG0 1377 2HCl (3-30 μM; 30 minutes) inhibits vascular endothelial growth factor A (VEGF-A) stimulated tyrosine phosphorylation of VEGF-R2/KDR with an IC50 of 30 μM.[1] EG0 1377 2HCl (30 μM; 5 days) can delay the VEGF-induced wound closure.[1] EG0 1377 2HCl diminishes VEGF-triggered angiogenesis. Moreover, when combined with VEGFA, EG01377 2HCl curtails spheroid outgrowth of A375P (malignant melanoma) cells.[1] EG0 1377 2HCl (500 nM; 2 h) 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] |
In vivo | EG0 1377 2HCl (2 mg/kg; i.v.; BABL/c female mice) possesses a half-life of 4.29 hours, allowing for once-a-day dosing to be maintained in mice.[1] |
別名 | EG01377 2HCl(2227996-00-9 Free base) |
分子量 | 659.6 |
分子式 | C26H32Cl2N6O6S2 |
CAS No. | 2749438-61-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 180.0 mg/mL (272.9 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. 詳細
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EG01377 2HCl 2749438-61-5 Immunology/Inflammation Complement System EG01377 2HCl(2227996-00-9 Free base) EG-01377 EG01377 EG 01377 Inhibitor inhibitor inhibit