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    PND-1186 (VS-4718; SR-2156)
    PND-1186 (VS-4718; SR-2156)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0662
    CAS #: 1061353-68-1Purity ≥98%

    Description: PND-1186 (also known as SR2156, PND1186 or VS4718) is a novel, potent, reversible and selective FAK (focal adhesion kinase) inhibitor with potential anticancer activities. It inhibits FAK with an IC50 of 1.5 nM. PND-1186 shows potent anti-proliferative activity in vitro with an IC50 of ~100 nM in breast carcinoma cells, and high in vivo antitumor efficacy against ovarian carcinoma tumors. 

    References: Cancer Biol Ther. 2010 May 15;9(10):764-77; Mol Cancer Ther. 2014 Aug;13(8):2050-61.

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    Molecular Weight (MW)501.5
    FormulaC25H26F3N5O3
    CAS No.1061353-68-1
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 24 mg/mL (47.8 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)2% DMSO+30% PEG 300+5% Tween 80+ddH2O: 5mg/mL 
    SynonymsSR-2156; VS-4718; PND-1186; PND 1186; PND1186; SR 2516; SR2516; VS4718; VS 4718. 

    Chemical Name: 2-((2-((2-methoxy-4-morpholinophenyl)amino)-5-(trifluoromethyl)pyridin-4-yl)amino)-N-methylbenzamide.

    InChi Key: IGUBBWJDMLCRIK-UHFFFAOYSA-N

    InChi Code: InChI=1S/C25H26F3N5O3/c1-29-24(34)17-5-3-4-6-19(17)31-21-14-23(30-15-18(21)25(26,27)28)32-20-8-7-16(13-22(20)35-2)33-9-11-36-12-10-33/h3-8,13-15H,9-12H2,1-2H3,(H,29,34)(H2,30,31,32)

    SMILES Code: O=C(NC)C1=CC=CC=C1NC2=CC(NC3=C(OC)C=C(N4CCOCC4)C=C3)=NC=C2C(F)(F)F


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    In Vitro

    In vitro activity: In vitro, PND-1186 inhibits 4T1 breast carcinoma motility, promotes 4T1 apoptosis in suspended conditions, and decreases 4T1 soft agar colony number and size. In HEY and OVCAR8 cells, VS-4718 promotes G0-G1 cell-cycle arrest followed by cell death.


    Kinase Assay: GST-FAK in vitro kinase activity is measured and compared to His-tagged FAK 411–686 using the K-LISA screening kit and poly(Glu:Tyr) (4:1) copolymer as a substrate immobilized on microtiter plates. IC50 values are determined with various concentrations of test compounds in a buffer containing 50 µM ATP and 10 mM MnCl2, 50 mM HEPES (pH 7.5), 25 mM NaCl, 0.01% BSA, and 0.1 mM Na orthovanadate for 5 min at room temperature. Serial diluted compounds are tested in triplicate. Substrate phosphorylation is measured using horseradish peroxidase-conjugated anti-pTyr antibodies with spetrophotometric color quantitation. IC50 values are determined using the Hill-Slope Model. Kinase selectivity profiling is performed by using the KinaseProfiler service. 


    Cell Assay: For soft agar assays, 48-well plates are coated with a 1:4 mix of 2% agar (EM Science) in 0.2 mL growth media (bottom layer). 5×104 cells are plated per well (in triplicate) in a mixture of 0.3% agar in 0.2 mL growth media (top layer). After agar solidification, 0.2 mL growth media is added containing DMSO or PND-1186 (final concentration for 0.6 mL). In separate experiments, PND-1186 is added after 4 days. After 10 days, colonies are imaged in phase contrast, enumerated by counting 9 fields (3 fields per well), and total area determined using Image J. For all analyses, experimental points are performed in triplicate and repeated at least two times.

    In VivoIn mice bearing 4T1 tumors, PND-1186 (100 mg/kg s.c.) inhibits 4T1 subcutaneous tumor growth by induction of apoptosis. In mice bearing ID8 tumors, PND-1186 (0.5 mg/mL for p.o.) also causes ovarian carcinoma tumor growth inhibition. 
    Animal modelMice bearing ID8 tumors or 4T1 tumors 
    Formulation & DosageDissolved in polyethylene glycol 400 (PEG400) in PBS (1:1) for s.c.; 5% sucrose for p.o.; 100 mg/kg every 12 hours for s.c.; 0.5 mg/mL for p.o.; Administered via s.c. or p.o. 
    References

    Cancer Biol Ther. 2010 May 15;9(10):764-77; Mol Cancer Ther. 2014 Aug;13(8):2050-61.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    PND-1186 (VS-4718)

    PND-1186 inhibitory effects differ from Dasatinib (Src inhibition). Cancer Biol Ther. 2010 May; 9(10): 764–777.

    PND-1186 (VS-4718)

    PND-1186 inhibits ovarian carcinoma tumor growth. Cancer Biol Ther. 2010 May; 9(10): 764–777. Cancer Biol Ther. 2010 May 15;9(10):764-77.

    PND-1186 (VS-4718)

    Selective 4T1 cell apoptosis in suspension at low PND-1186 levels. Cancer Biol Ther. 2010 May 15;9(10):764-77.


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