2. Protein Tyrosine Kinase/RTK Apoptosis
  3. FAK Apoptosis
  4. PND-1186 hydrochloride

PND-1186 hydrochloride  (Synonyms: VS-4718 hydrochloride; SR-2516 hydrochloride)

Cat. No.: HY-13917A Purity: 99.38%
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PND-1186 hydrochloride (VS-4718 hydrochloride) is a potent, highly-specific and reversible inhibitor of FAK with an IC50 of 1.5 nM. PND-1186 hydrochloride selectively promotes tumor cell apoptosis.

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

PND-1186 hydrochloride Chemical Structure

PND-1186 hydrochloride Chemical Structure

CAS No. : 1356154-94-3

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10 mM * 1 mL in DMSO
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Customer Review

Based on 10 publication(s) in Google Scholar

Other Forms of PND-1186 hydrochloride:

PND-1186 hydrochloride Related Antibodies

Top Publications Citing Use of Products

    PND-1186 hydrochloride purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2019 Mar 18;35(3):457-472.e5.  [Abstract]

    Immunoblot showing YAP nuclear and cytoplasmic localization after 2 h VS-4718 (1 mM) treatment in OMM1.3 cells, using lamin A/C and a-tubulin as nuclear and cytoplasmic markers, respectively.

    PND-1186 hydrochloride purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2019 Mar 18;35(3):457-472.e5.  [Abstract]

    Immunoblot showing the association of MOB1 with LATS1 after HA or pY immunoprecipitation of OMM1.3 cells transfected with HA-MOB1 with or without 1 h VS-4718 treatment.

    • Biological Activity

    • Purity & Documentation

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    Description

    PND-1186 hydrochloride (VS-4718 hydrochloride) is a potent, highly-specific and reversible inhibitor of FAK with an IC50 of 1.5 nM. PND-1186 hydrochloride selectively promotes tumor cell apoptosis[1].

    In Vitro

    PND-1186 has an IC50 of ~100 nM in breast carcinoma cells as determined by anti-phospho-specific immunoblotting to FAK Tyr-397[1].
    In murine 4T1 breast carcinoma cells, FAK is important in promoting an invasive and metastatic cell phenotype. Increasing concentrations of PND-1186 (0.1 to 1.0 µM) added to 4T1 cells inhibits FAK Tyr-397 phosphorylation (pY397) and results in elevated levels of total FAK protein within 1 h[1].

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

    PND-1186 hydrochloride Related Antibodies

    Western Blot Analysis[1]

    Cell Line: 4T1 breast carcinoma cells
    Concentration: 0.1, 0.2, 0.4, 0.6 and 1.0 µM
    Incubation Time: 1 hour
    Result: Inhibited FAK Tyr-397 phosphorylation (pY397) and resulted in elevated levels of total FAK protein.
    In Vivo

    PND-1186 (30 mg/kg or 100 mg/kg; subcutaneously; injected subcutaneously in the neck region) inhibits 4T1 subcutaneous tumor growth by induction of apoptosis[1].

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

    Animal Model: BALB/c mice[1]
    Dosage: 30 mg/kg or 100 mg/kg
    Administration: Injected (100 µL) subcutaneously in the neck region; every 12 h (twice-daily, b.i.d.) for 5 days.
    Result: 100 mg/kg treatment significantly reduced final 4T1 tumor weight 2-fold whereas 30 mg/kg treatment slightly reduced final tumor weight but was not significantly different compared to control.
    Clinical Trial
    Molecular Weight

    537.96

    Formula

    C25H27ClF3N5O3
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    [H]Cl.O=C(NC)C1=CC=CC=C1NC2=CC(NC3=CC=C(N4CCOCC4)C=C3OC)=NC=C2C(F)(F)F
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

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

    Solvent & Solubility
    In Vitro: 

    DMSO : 200 mg/mL (371.77 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 20 mg/mL (37.18 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8589 mL 9.2944 mL 18.5887 mL
    5 mM 0.3718 mL 1.8589 mL 3.7177 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 (sealed storage, 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.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • 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)

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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 (9.29 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 (9.29 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.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    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).
    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 (sealed storage, 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
    H2O / DMSO 1 mM 1.8589 mL 9.2944 mL 18.5887 mL 46.4719 mL
    5 mM 0.3718 mL 1.8589 mL 3.7177 mL 9.2944 mL
    10 mM 0.1859 mL 0.9294 mL 1.8589 mL 4.6472 mL
    15 mM 0.1239 mL 0.6196 mL 1.2392 mL 3.0981 mL
    20 mM 0.0929 mL 0.4647 mL 0.9294 mL 2.3236 mL
    25 mM 0.0744 mL 0.3718 mL 0.7435 mL 1.8589 mL
    30 mM 0.0620 mL 0.3098 mL 0.6196 mL 1.5491 mL
    DMSO 40 mM 0.0465 mL 0.2324 mL 0.4647 mL 1.1618 mL
    50 mM 0.0372 mL 0.1859 mL 0.3718 mL 0.9294 mL
    60 mM 0.0310 mL 0.1549 mL 0.3098 mL 0.7745 mL
    80 mM 0.0232 mL 0.1162 mL 0.2324 mL 0.5809 mL
    100 mM 0.0186 mL 0.0929 mL 0.1859 mL 0.4647 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    PND-1186 hydrochloride 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:

    PND-11861356154-94-3VS-4718SR-2516PND1186PND 1186VS4718VS 4718SR2516SR 2516FAKApoptosisPTK2 protein tyrosine kinase 2PTK2Focal adhesion kinasecellsurvivalintegrintumorgrowthInhibitorinhibitorinhibit

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