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EG01377 

Cat. No.: HY-112151
Handling Instructions

EG01377 is a neuropilin-1 (NRP1) antagonist, with a Kd of 1.32 μM for NRP1-b1, and IC50s of both 609 nM for NRP1-a1 and NRP1-b1, but shows no effect on NRP2; EG01377 has antiangiogenic, antimigratory, and antitumor effects.

For research use only. We do not sell to patients.

EG01377 Chemical Structure

EG01377 Chemical Structure

CAS No. : 2227996-00-9

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

EG01377 is a neuropilin-1 (NRP1) antagonist, with a Kd of 1.32 μM for NRP1-b1, and IC50s of both 609 nM for NRP1-a1 and NRP1-b1, but shows no effect on NRP2; EG01377 has antiangiogenic, antimigratory, and antitumor effects.

IC50 & Target

IC50: 609 nM (NRP1-a1), 609 nM (NRP1-b1)[1]
Kd: 1.32 μM (NRP1-b1)[1]

In Vitro

EG01377 is a neuropilin-1 (NRP1) antagonist, with a Kd of 1.32 μM for NRP1-b1, and IC50s of both 609 nM for NRP1-a1 and NRP1-b1, but shows no effect on NRP2. EG01377 inhibits NRP1 in DU145/cells.Ad.NRP1 cells (IC50, 1.6 μM). EG01377 (3, 10, and 30 μM) inhibits VEGF-A stimulated tyrosine phosphorylation of VEGF-R2/KDR. EG01377 (30 μM) also significantly reduces HUVEC cell migration in response to VEGFA, and reduces VEGF-induced angiogenesis. Moreover, EG01377 (30 μM) in combination with VEGFA causes reduction in A375P spheroid outgrowth. EG01377 blocks the production of TGFβ by Nrp1+ Tregs in the presence of tumor cell-derived factors[1].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7045 mL 8.5225 mL 17.0451 mL
5 mM 0.3409 mL 1.7045 mL 3.4090 mL
10 mM 0.1705 mL 0.8523 mL 1.7045 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

The 96-well plates are precoated with NP1 protein at 3 μg/mL overnight at 4°C. On the following day, the plates are treated with blocking buffer (PBS containing 1% BSA) and washed three times with wash buffer (PBS containing 0.1% Tween-20). The various concentrations of compounds (EG01377, etc.) diluted in PBS containing 1% DMSO are added, followed by addition of 0.25 nM of bt-VEGF-A165. After 2 h of incubation at room temperature, the plates are washed three times with wash buffer. The bound bt-VEGF-A165 to NP-1 is detected by streptavidin-horseradish peroxidase conjugates and the enzyme substrate, and measured using a plate reader at A450 nm with a reference wavelength at A595 nm. Nonspecific binding is determined in the absence of NP-1 coated wells of the plates[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

586.68

Formula

C₂₆H₃₀N₆O₆S₂

CAS No.

2227996-00-9

SMILES

O=S(C1=CC(C2=CC=C(CN)C=C2)=CC3=C1OCC3)(NC4=C(C(N[[email protected]@H](CCC/N=C(N)/N)C(O)=O)=O)SC=C4)=O

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
EG01377
Cat. No.:
HY-112151
Quantity:

EG01377

Cat. No.: HY-112151