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

NVP-BHG712 (Synonyms: BHG712)

Cat. No.: HY-13258A Purity: 99.93%
Handling Instructions

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

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 100 In-stock
Estimated Time of Arrival: December 31
5 mg USD 90 In-stock
Estimated Time of Arrival: December 31
10 mg USD 160 In-stock
Estimated Time of Arrival: December 31
50 mg USD 660 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of NVP-BHG712:

Top Publications Citing Use of Products

    NVP-BHG712 purchased from MCE. Usage Cited in: Pharmacol Res. 2020 May 11:104868.

    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 MCE. Usage Cited in: Cell Death Dis. 2020 Aug 14;11(8):632.

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

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    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].

    In Vivo

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

    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.

    940310-85-0

    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 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 31.25 mg/mL (62.07 mM; Need ultrasonic)

    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
    10 mM 0.1986 mL 0.9931 mL 1.9862 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

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

    *All of the co-solvents are provided by MCE.
    References
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    Keywords:

    NVP-BHG712BHG712BHG 712BHG-712Ephrin ReceptorInhibitorinhibitorinhibit

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    Product Name:
    NVP-BHG712
    Cat. No.:
    HY-13258A
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