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

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

Cat. No.: HY-13917A Purity: 98.78%
Handling Instructions

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 USD 146 In-stock
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5 mg USD 132 In-stock
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10 mg USD 180 In-stock
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50 mg USD 420 In-stock
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100 mg USD 660 In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of PND-1186 hydrochloride:

Top Publications Citing Use of Products

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

    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 MCE. Usage Cited in: Cancer Cell. 2019 Mar 18;35(3):457-472.e5.

    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

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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].

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

    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].

    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.
    Molecular Weight

    537.96

    Formula

    C₂₅H₂₇ClF₃N₅O₃

    CAS No.

    1356154-94-3

    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
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 200 mg/mL (371.77 mM; Need ultrasonic)

    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
    10 mM 0.1859 mL 0.9294 mL 1.8589 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: ≥ 5 mg/mL (9.29 mM); Clear solution

    • 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

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

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

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    Product Name:
    PND-1186 hydrochloride
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