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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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $148 | In Stock | |
5 mg | $372 | In Stock | |
10 mg | $568 | In Stock | |
25 mg | $915 | In Stock | |
50 mg | $1,250 | In Stock | |
100 mg | $1,680 | In Stock | |
500 mg | $3,370 | In Stock | |
1 mL x 10 mM (in DMSO) | $539 | In Stock |
Description | 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. |
Targets&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] |
Alias | EG01377 2HCl(2227996-00-9 Free base) |
Molecular Weight | 659.6 |
Formula | C26H32Cl2N6O6S2 |
Cas No. | 2749438-61-5 |
Smiles | 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 |
Relative Density. | no data available |
Storage | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 180.0 mg/mL (272.9 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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