2. Protein Tyrosine Kinase/RTK
  3. Ephrin Receptor
  4. NVP-BHG712

NVP-BHG712 is an oral active EphB4 kinase autophosphorylation inhibitor, with IC50 values of 3.3 nM and 3.0 nM for EphA2 and EphB4, respectively.

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

NVP-BHG712 Chemical Structure

NVP-BHG712 Chemical Structure

CAS No. : 940310-85-0

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 100 In-stock
Solid
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10 mg USD 140 In-stock
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50 mg USD 500 In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of NVP-BHG712:

NVP-BHG712 Related Antibodies

Top Publications Citing Use of Products

    NVP-BHG712 purchased from MedChemExpress. Usage Cited in: Pharmacol Res. 2020 Aug;158:104868.  [Abstract]

    Protein expression of EphB4, JAK2, p-JAK2, STAT3, and p-STAT3 in HepG2 cells treated with either CTD (2.5 μM), NVP-BHG-712 (1 μM), or the combination of both.

    NVP-BHG712 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2020 Aug 14;11(8):632.  [Abstract]

    Western blot analysis of HepG2 cells EphB4 expression after NVP-BHG712 treatment. NVP-BHG712treatment decreases in the expression level of EphB4 in HepG2 cells.

    View All Ephrin Receptor Isoform Specific Products:

    View All Isoforms
    EphA2 EphA3 EphA4

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    NVP-BHG712 is an oral active EphB4 kinase autophosphorylation inhibitor, with IC50 values of 3.3 nM and 3.0 nM for EphA2 and EphB4, respectively[1][2].

    IC50 & Target

    IC50: 3.3 nM (EphA2), 3 nM (EphB4)[2].
    In Vitro

    NVP-BHG712 inhibits VEGF driven vessel formation, while it has only little effects on VEGF receptor (VEGFR) activity. The data suggests a close cross talk between the VEGFR and EphR signaling during vessel formation[2].

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

    NVP-BHG712 Related Antibodies
    In Vivo

    NVP-BHG712 (3, 10 and 30 mg/kg, p.o., daily) inhibits VEGF driven tissue growth and angiogenesis[2].

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

    Animal Model: Mice arrying chambers[1].
    Dosage: 3, 10 and 30 mg/kg.
    Administration: P.O. daily for 4 days.
    Result: Significantly inhibited VEGF stimulated tissue formation and vascularization at doses of daily 3 mg/kg. Administration of 10 mg/kg/kg p.o. was sufficient to reverse VEGF enhanced tissue formation and vessel growth.
    Molecular Weight

    503.48

    Formula

    C26H20F3N7O
    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    CC1=CC=C(C=C1NC2=NC(C3=CC=CN=C3)=NC4=C2C=NN4C)C(NC5=CC=CC(C(F)(F)F)=C5)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 31.25 mg/mL (62.07 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 1.9862 mL 9.9309 mL 19.8618 mL
    5 mM 0.3972 mL 1.9862 mL 3.9724 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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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: ≥ 2.08 mg/mL (4.13 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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% Corn Oil

      Solubility: ≥ 2.08 mg/mL (4.13 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

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    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).
    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

    Purity: 99.70%

    SDS (479 KB)

    COA (251 KB) HNMR (289 KB) LCMS (266 KB)

    Handling Instructions (2659 KB)
    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.9862 mL 9.9309 mL 19.8618 mL 49.6544 mL
    5 mM 0.3972 mL 1.9862 mL 3.9724 mL 9.9309 mL
    10 mM 0.1986 mL 0.9931 mL 1.9862 mL 4.9654 mL
    15 mM 0.1324 mL 0.6621 mL 1.3241 mL 3.3103 mL
    20 mM 0.0993 mL 0.4965 mL 0.9931 mL 2.4827 mL
    25 mM 0.0794 mL 0.3972 mL 0.7945 mL 1.9862 mL
    30 mM 0.0662 mL 0.3310 mL 0.6621 mL 1.6551 mL
    40 mM 0.0497 mL 0.2483 mL 0.4965 mL 1.2414 mL
    50 mM 0.0397 mL 0.1986 mL 0.3972 mL 0.9931 mL
    60 mM 0.0331 mL 0.1655 mL 0.3310 mL 0.8276 mL
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    NVP-BHG712 Related Classifications

    Help & FAQs
    • 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.

    Keywords:

    NVP-BHG712940310-85-0BHG712BHG 712BHG-712Ephrin ReceptorInhibitorinhibitorinhibit

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