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  3. EG01377 dihydrochloride

EG01377 dihydrochloride is a potent, bioavailable and selective inhibitor of neuropilin-1 (NRP1), with a Kd of 1.32 μM, and IC50s of 609 nM for both NRP1-a1 and NRP1-b1. EG01377 dihydrochloride has antiangiogenic, antimigratory, and antitumor effects.

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

EG01377 dihydrochloride Chemical Structure

EG01377 dihydrochloride Chemical Structure

CAS No. : 2749438-61-5

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 653 In-stock
Solution
10 mM * 1 mL in DMSO USD 653 In-stock
Solid
5 mg USD 450 In-stock
10 mg USD 750 In-stock
50 mg USD 2100 In-stock
100 mg USD 3350 In-stock
200 mg   Get quote  
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Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of EG01377 dihydrochloride:

Top Publications Citing Use of Products
WB
Proliferation Assay

    EG01377 dihydrochloride purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2023 Feb 25;14(2):159.  [Abstract]

    EG01377 (20, 40, 80 µM; 14 days) significantly attenuates clone formation ability of PC-3 and DU-145 cells in a concentration-dependent manner.

    EG01377 dihydrochloride purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2023 Feb 25;14(2):159.  [Abstract]

    EG01377 (20, 40, 80 µM) attenuates the phosphorylation of EGFR, AKT, GSK3β, and mTOR in PC-3 and DU-145 cells.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    EG01377 dihydrochloride is a potent, bioavailable and selective inhibitor of neuropilin-1 (NRP1), with a Kd of 1.32 μM, and IC50s of 609 nM for both NRP1-a1 and NRP1-b1. EG01377 dihydrochloride has antiangiogenic, antimigratory, and antitumor effects[1].

    IC50 & Target

    IC50: 609 nM (NRP1-a1 and NRP1-b)[1]

    In Vitro

    EG01377 (3-30 μM; 30 minutes) inhibits vascular endothelial growth factor A (VEGF-A) stimulated tyrosine phosphorylation of VEGF-R2/KDR[1].
    EG01377 (30 μM) is able to significantly reduce HUVEC cell migration in response to VEGFA[1].
    EG01377 (30 μM; 5 days) can delay the VEGF-induced wound closure[1].
    EG01377 (30 μM) reduces network area, length, and branching points[1].
    EG01377 (30 μM; 7 days) reduces VEGF-induced angiogenesis[1].
    EG01377 (30 μM; 7 days) in combination with VEGFA reduces A375P (malignant melanoma) spheroid outgrowth[1].
    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[1].

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

    Western Blot Analysis[1]

    Cell Line: Human umbilical vein endothelial cells (HUVECs)
    Concentration: 3, 10, 30 μM
    Incubation Time: 30 minutes
    Result: Inhibited VEGF-A stimulated tyrosine phosphorylation of VEGF-R2/KDR with an IC50 of 30 μM.
    In Vivo

    EG01377 (2 mg/kg; i.v.) exhibits an encouraging half-life of 4.29 h, sufficient to sustain once per day dosing in mice[1].

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

    Animal Model: 6-8 week-old BABL/c female mice[1]
    Dosage: 2 mg/kg (Pharmacokinetic Analysis)
    Administration: I.v. administration
    Result: The half time (T1/2) of 4.29 h.
    Molecular Weight

    659.60

    Formula

    C26H32Cl2N6O6S2

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    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.Cl.Cl

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    -20°C, stored under nitrogen, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : 200 mg/mL (303.21 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.5161 mL 7.5804 mL 15.1607 mL
    5 mM 0.3032 mL 1.5161 mL 3.0321 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 5 mg/mL (7.58 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 5 mg/mL (7.58 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.5161 mL 7.5804 mL 15.1607 mL 37.9018 mL
    5 mM 0.3032 mL 1.5161 mL 3.0321 mL 7.5804 mL
    10 mM 0.1516 mL 0.7580 mL 1.5161 mL 3.7902 mL
    15 mM 0.1011 mL 0.5054 mL 1.0107 mL 2.5268 mL
    20 mM 0.0758 mL 0.3790 mL 0.7580 mL 1.8951 mL
    25 mM 0.0606 mL 0.3032 mL 0.6064 mL 1.5161 mL
    30 mM 0.0505 mL 0.2527 mL 0.5054 mL 1.2634 mL
    40 mM 0.0379 mL 0.1895 mL 0.3790 mL 0.9475 mL
    50 mM 0.0303 mL 0.1516 mL 0.3032 mL 0.7580 mL
    60 mM 0.0253 mL 0.1263 mL 0.2527 mL 0.6317 mL
    80 mM 0.0190 mL 0.0948 mL 0.1895 mL 0.4738 mL
    100 mM 0.0152 mL 0.0758 mL 0.1516 mL 0.3790 mL
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    EG01377 dihydrochloride Related Classifications

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Product Name:
    EG01377 dihydrochloride
    Cat. No.:
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