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> AF38469 [1531634-31-7]

AF38469 [1531634-31-7]

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AF38469 is a selective, orally bioavailable Sortilin inhibitor with an IC50 value of 330 nM.

Para uso exclusivo en investigación. No vendemos a pacientes.

AF38469 Estructura química

AF38469 Estructura química

No. CAS : 1531634-31-7

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

Based on 9 publication(s) in Google Scholar

    AF38469 purchased from MedChemExpress. Usage Cited in: Am J Pathol. 2020 Sep;190(9):1931-1942.  [Abstract]

    Western blot detection of phosphorylation of FAK (Tyr925), FAK (Tyr397) and FAK (Tyr576/577) in the treatment with AF38469. The phosphorylation of residue Tyr925 of FAK is decreased in sortilin-inhibited compared to NT control.

    AF38469 purchased from MedChemExpress. Usage Cited in: Breast Cancer Res. 2018 Nov 20;20(1):137.   [Abstract]

    Immunohistochemical analyses of the GRN A- and AF38469-treated groups of MDA-MB 231 luc xenografts with skin is performed using Ki67 and haematoxylin staining.
    Descripciòn

    AF38469 is a selective, orally bioavailable Sortilin inhibitor with an IC50 value of 330 nM.

    IC50 & Target

    IC50:330 nM (Sortilin)[1]
    In Vivo

    AF38469 (1 mg/kg; i.v.) has a low volume of distribution (blood volume of 0.7 L/kg) and low clearance (4.8 L/h/kg), and a half-life (t1/2) of 1.2 h in rat[1].

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

    324.25

    Fòrmula

    C15H11F3N2O3
    No. CAS

    1531634-31-7
    Appearance

    Solid

    Color

    Off-white to light yellow

    SMILES

    O=C(NC1=CC=CC(C)=N1)C2=CC=C(C(F)(F)F)C=C2C(O)=O
    Envío

    Room temperature in continental US; may vary elsewhere.
    Almacenamiento
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvente y solubilidad
    In Vitro: 

    DMSO : ≥ 43 mg/mL (132.61 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.0840 mL 15.4202 mL 30.8404 mL
    5 mM 0.6168 mL 3.0840 mL 6.1681 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.

    • Calculadora de molaridad

    • Calculadora de dilución

    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:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: 2.5 mg/mL (7.71 mM); Suspended solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.08 mg/mL (6.41 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)

    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.
    Pureza y Documentación

    Purity: 99.28%

    COA (252 KB) HNMR (164 KB) LCMS (404 KB)

    Instrucciones de manejo (2659 KB)
    Referencias

    • [1]. Schroder TJ, et al. The identification of AF38469: an orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin. Bioorg Med Chem Lett. 2014 Jan 1;24(1):177-80.  [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 3.0840 mL 15.4202 mL 30.8404 mL 77.1010 mL
    5 mM 0.6168 mL 3.0840 mL 6.1681 mL 15.4202 mL
    10 mM 0.3084 mL 1.5420 mL 3.0840 mL 7.7101 mL
    15 mM 0.2056 mL 1.0280 mL 2.0560 mL 5.1401 mL
    20 mM 0.1542 mL 0.7710 mL 1.5420 mL 3.8551 mL
    25 mM 0.1234 mL 0.6168 mL 1.2336 mL 3.0840 mL
    30 mM 0.1028 mL 0.5140 mL 1.0280 mL 2.5700 mL
    40 mM 0.0771 mL 0.3855 mL 0.7710 mL 1.9275 mL
    50 mM 0.0617 mL 0.3084 mL 0.6168 mL 1.5420 mL
    60 mM 0.0514 mL 0.2570 mL 0.5140 mL 1.2850 mL
    80 mM 0.0386 mL 0.1928 mL 0.3855 mL 0.9638 mL
    100 mM 0.0308 mL 0.1542 mL 0.3084 mL 0.7710 mL
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    AF38469 Related Classifications

    Help & FAQs

    Keywords:

    AF384691531634-31-7AF 38469AF-38469Neurotensin ReceptorInhibitorinhibitorinhibit

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