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EG01377

Catalog No.GC33272

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.

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EG01377 Chemical Structure

Cas No.: 2227996-00-9

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Kinase experiment:

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].

References:

[1]. Powell J, et al. Small Molecule Neuropilin-1 Antagonists Combine Antiangiogenic and Antitumor Activity with Immune Modulation through Reduction of Transforming Growth Factor Beta (TGFβ) Production in Regulatory T-Cells. J Med Chem. 2018 May 10;61(9):4135-4154.

Background

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.

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].

[1]. Powell J, et al. Small Molecule Neuropilin-1 Antagonists Combine Antiangiogenic and Antitumor Activity with Immune Modulation through Reduction of Transforming Growth Factor Beta (TGFβ) Production in Regulatory T-Cells. J Med Chem. 2018 May 10;61(9):4135-4154.

Chemical Properties

Cas No. 2227996-00-9 SDF
Canonical SMILES O=S(C1=CC(C2=CC=C(CN)C=C2)=CC3=C1OCC3)(NC4=C(C(N[C@@H](CCC/N=C(N)/N)C(O)=O)=O)SC=C4)=O
Formula C26H30N6O6S2 M.Wt 586.68
Solubility Soluble in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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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 3.409 mL
10 mM 0.1705 mL 0.8523 mL 1.7045 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Average Rating: 5 ★★★★★ (Based on Reviews and 8 reference(s) in Google Scholar.)

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