DPH [484049-04-9]

Katalog-Nummer HY-12070-50mg

Size : 50mg

Marke : MedChemExpress

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DPH is a potent cell permeable c-Abl activator, which displays potent enzymatic and cellular activity in stimulating c-Abl activation.  

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DPH Chemische Struktur

DPH Chemische Struktur

CAS. Nr. : 484049-04-9

This product is a controlled substance and not for sale in your territory.

Based on 6 publication(s) in Google Scholar

    DPH purchased from MedChemExpress. Usage Cited in: Toxicol Sci. 2018 Sep 1;165(1):232-243.  [Abstract]

    Treatment of SN4741 cells with DPH, a c-Abl activator, results in a significant phosphorylation of GSK3β-Y216

    DPH purchased from MedChemExpress. Usage Cited in: Mol Cell Neurosci. 2017 Dec;85:226-234.  [Abstract]

    In a separate experiment, mice are injected with DPH and euthanized 4 hours later. DPH increases hippocampal p190RhoGAP phosphorylation. Representative blots below.
    Beschreibung

    DPH is a potent cell permeable c-Abl activator, which displays potent enzymatic and cellular activity in stimulating c-Abl activation.  

    In Vitro

    DPH binds to the myristoyl binding site and prevents the formation of the bent conformation of the αI helix through steric hindrance, a mode of action distinct from the previously identified allosteric c-Abl inhibitor, GNF-2, that also binds to the myristoyl binding site. DPH represents the first cell-permeable, small-molecule tool compound for c-Abl activation[1].

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

    Molekulargewicht

    336.32

    Formel

    C18H13FN4O2

    CAS. Nr.

    484049-04-9

    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C1NC(C(N1)C2=CN(N=C2C3=CC=C(C=C3)F)C4=CC=CC=C4)=O

    Versand

    Room temperature in continental US; may vary elsewhere.

    Speicherung
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Lösungsmittel & Löslichkeit
    In Vitro: 

    DMSO : 50 mg/mL (148.67 mM; ultrasonic and warming and heat to 60°C; 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 2.9734 mL 14.8668 mL 29.7336 mL
    5 mM 0.5947 mL 2.9734 mL 5.9467 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.

    • Molaritätsrechner

    • Verdünnungsrechner

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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: ≥ 2.5 mg/mL (7.43 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (7.43 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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).
    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.
    Reinheit & Dokumentation

    Purity: 99.20%

    Verweise
    • [1]. Yang J, et al. Discovery and characterization of a cell-permeable, small-molecule c-Abl kinase activator that binds to the myristoyl binding site. Chem Biol. 2011 Feb 25;18(2):177-86  [Content Brief]

      [2]. Shapiro LP, et al. Corticosteroid-induced dendrite loss and behavioral deficiencies can be blocked by activation of Abl2/Arg kinase. Mol Cell Neurosci. 2017 Oct 26;85:226-234.  [Content Brief]

    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 2.9734 mL 14.8668 mL 29.7336 mL 74.3340 mL
    5 mM 0.5947 mL 2.9734 mL 5.9467 mL 14.8668 mL
    10 mM 0.2973 mL 1.4867 mL 2.9734 mL 7.4334 mL
    15 mM 0.1982 mL 0.9911 mL 1.9822 mL 4.9556 mL
    20 mM 0.1487 mL 0.7433 mL 1.4867 mL 3.7167 mL
    25 mM 0.1189 mL 0.5947 mL 1.1893 mL 2.9734 mL
    30 mM 0.0991 mL 0.4956 mL 0.9911 mL 2.4778 mL
    40 mM 0.0743 mL 0.3717 mL 0.7433 mL 1.8583 mL
    50 mM 0.0595 mL 0.2973 mL 0.5947 mL 1.4867 mL
    60 mM 0.0496 mL 0.2478 mL 0.4956 mL 1.2389 mL
    80 mM 0.0372 mL 0.1858 mL 0.3717 mL 0.9292 mL
    100 mM 0.0297 mL 0.1487 mL 0.2973 mL 0.7433 mL
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    DPH Related Classifications

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    Keywords:

    DPH484049-04-9Bcr-AblInhibitorinhibitorinhibit

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