1. Protein Tyrosine Kinase/RTK
    Autophagy
  2. c-Met/HGFR
    Autophagy
  3. PHA-665752

PHA-665752 

Cat. No.: HY-11107 Purity: 96.50%
Handling Instructions

PHA-665752 is a potent, selective and ATP-competitive inhibitor of c-Met Kinase, with an IC50 of 9 nM. Has therapeutic potential of targeting c-Met in human cancers.

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

PHA-665752 Chemical Structure

PHA-665752 Chemical Structure

CAS No. : 477575-56-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 108 In-stock
Estimated Time of Arrival: December 31
10 mg USD 98 In-stock
Estimated Time of Arrival: December 31
50 mg USD 396 In-stock
Estimated Time of Arrival: December 31
100 mg USD 696 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 5 publication(s) in Google Scholar

Top Publications Citing Use of Products

    PHA-665752 purchased from MCE. Usage Cited in: Oncotarget. 2017 Jun 13;8(24):38717-38730.

    KU812/IR cells are exposed to the indicated concentrations of Imatinib or PHA665752. After incubation for 48 h, the cytoplasmic fractions are extracted and then subjected to SDS-PAGE/immunoblotting with anti-phospho-MET, anti-phospho-ABL1, anti-phospho-ERK1/2, anti-phospho-AKT, anti-phospho-JNK, anti-MET, anti-ABL1, anti-ERK1/2, anti-AKT, and anti-JNK antibodies. Anti-β-ACTIN antibody is used as internal standards.
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    Description

    PHA-665752 is a potent, selective and ATP-competitive inhibitor of c-Met Kinase, with an IC50 of 9 nM. Has therapeutic potential of targeting c-Met in human cancers[1].

    IC50 & Target

    IC50: 9 nM (c-Met)[1]

    In Vitro

    PHA-665752 is a potent and ATP-competitive inhibitor of c-Met kinase activity with a Ki of 4 nM and an IC50 of 9 nM[1].
    PHA-665752 exhibits >50-fold selectivity for c-Met enzyme compared with the majority of kinases evaluated[1].
    PHA-665752 shows potent inhibition of c-Met RTK autophosphorylation in NIH3T3 cells engineered to express high levels of c-Met and hepatocyte growth factor (HGF)[1].
    PHA-665752 inhibits HGF-stimulated or constitutive phosphorylation of mediators of downstream of c-Met such as Gab-1, ERK, Akt, STAT3, PLC-γ, and FAK in multiple tumor cell lines[1].
    PHA-665752 (0-1.25 μM; 18 hours) potently inhibits HGF and c-Met-driven phenotypes such as cell growth (proliferation and survival), cell motility, invasion, and/or morphology of a variety of tumor cells[1].
    PHA-665752 (0-1.25 μM; 72 hours) induces apoptosis in both the presence and absence of HGF at concentrations that inhibited tyrosine phosphorylation of c-Met in GTL-16 cells[1].
    PHA-665752 (0.0125-0.2 μM; 4 hours) potent inhibits HGF-induced c-Met phosphorylation in A549 cells[1].

    Cell Proliferation Assay[1]

    Cell Line: S114 cells, GTL-16 cells, NCI-H441 cells, or BxPC-3 cells
    Concentration: 0 μM, 0.002 μM, 0.01 μM, 0.05 μM, 0.25 μM, 1.25 μM
    Incubation Time: 18 hours
    Result: Potently inhibited HGF and c-Met-driven cell growth.

    Apoptosis Analysis[1]

    Cell Line: GTL-16 cells
    Concentration: 0 μM, 0.002 μM, 0.01 μM, 0.05 μM, 0.25 μM, 1.25 μM
    Incubation Time: 72 hours
    Result: Induced apoptosis in both the presence and absence of HGF at concentrations that inhibited tyrosine phosphorylation of c-Met in GTL-16 cells. Immunoblot Analysis.

    Western Blot Analysis[1]

    Cell Line: A549 cells
    Concentration: 0.0125 μM, 0.025 μM,0.05 μM,0.1 μM,0.2 μM
    Incubation Time: 4 hours
    Result: Potent inhibited HGF-induced c-Met phosphorylation in A549 cells.
    In Vivo

    PHA-665752 (7.5-30 mg/kg/day; i.v. ; for 9 days) exhibits statistically significant dose-dependent tumor growth inhibition of 68%, 39%, and 20% of vehicle control at the 30 mg/kg/day, 15 mg/kg/day, and 7.5 mg/kg/day doses, respectively[1].
    PHA-665752 shows a potent cytoreductive activity in a gastric carcinoma xenograft model[1].

    Animal Model: Female athymic mice (nu/nu, 8–12 weeks) bearing S114 or GTL-16 tumor xenografts[1]
    Dosage: 7.5 mg/kg/day, 15 mg/kg/day, 30 mg/kg/day
    Administration: Intravenous injection; for 9 days
    Result: Demonstrated statistically significant dose-dependent tumor growth inhibition.
    Molecular Weight

    641.61

    Formula

    C₃₂H₃₄Cl₂N₄O₄S

    CAS No.

    477575-56-7

    SMILES

    O=C(C1=C(NC(/C=C2C(NC3=C\2C=C(C=C3)S(=O)(CC4=C(C=CC=C4Cl)Cl)=O)=O)=C1C)C)N5[[email protected]](CCC5)CN6CCCC6

    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 : 50 mg/mL (77.93 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.5586 mL 7.7929 mL 15.5858 mL
    5 mM 0.3117 mL 1.5586 mL 3.1172 mL
    10 mM 0.1559 mL 0.7793 mL 1.5586 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: ≥ 2.5 mg/mL (3.90 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (3.90 mM); Clear solution

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

    Purity: 96.50%

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    Product Name:
    PHA-665752
    Cat. No.:
    HY-11107
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