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

PHA-665752 

Cat. No.: HY-11107 Purity: 99.27%
Data Sheet SDS Handling Instructions

PHA-665752 is a potent, selective and ATP-competitive c-Met inhibitor with IC50 of 9 nM, >50-fold selectivity for c-Met than RTKs or STKs.

For research use only. We do not sell to patients.
PHA-665752 Chemical Structure

PHA-665752 Chemical Structure

CAS No. : 477575-56-7

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $90 In-stock
10 mg $82 In-stock
50 mg $330 In-stock
100 mg $580 In-stock
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    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.
    • Biological Activity

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    Description

    PHA-665752 is a potent, selective and ATP-competitive c-Met inhibitor with IC50 of 9 nM, >50-fold selectivity for c-Met than RTKs or STKs. IC50 value: 9 nM Target: c-Met in vitro: PHA-665752 significantly inhibits c-Met kinase activity with Ki of 4 nM, and exhibits >50-fold selectivity for c-Met compared with various tyrosine and serine-threonine kinases. PHA-665752 potently inhibits the HGF-stimulated c-Met autophosphorylation with IC50 of 25-50 nM. PHA-665752 also significantly blocks HGF- and c-Met-dependent functions such as cell motility and cell proliferation with IC50 of 40-50 nM and 18-42 nM, respectively. In addition, PHA-665752 potently 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 inhibits cell growth in TPR-MET-transformed BaF3 cells with IC50 of <60 nM, and inhibits constitutive cell motility and migration by 92.5% at 0.2 μM. Inhibition of c-Met by PHA665752 (0.2 μM) also induces cell apoptosis of 33.1% and G1 cell cycle arrest with cells in G1 phase increasing from 42.4% to 77.0%. PHA665752 can cooperate with rapamycin to inhibit cell growth of TPR-MET-transformed BaF3 cells and non-small cell lung cancer H441 cells [2]. in vivo: Administration of PHA-665752 induces a dose-dependent tumor growth inhibition of S114 xenografts by 20 %, 39% and 68%, at dose of 7.5, 15, and 30 mg/kg/day, respectively [1]. PHA665752 treatment significantly reduces the tumor growth of NCI-H69, NCI-H441 and A549 in mouse xenografts by 99%, 75%, and 59%, respectively. PHA665752 also significantly inhibits angiogenesis by >85%, due to decreasing the production of vascular endothelial growth factor and increasing the production of the angiogenesis inhibitor thrombospondin-1 [3].

    References
    Molecular Weight

    641.61

    Formula

    C₃₂H₃₄Cl₂N₄O₄S

    CAS No.

    477575-56-7

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    PHA-665752 is dissolved in DMSO and diluted in phosphate-buffed saline (PBS; 0.05 M, pH 7.4), filtrated through syringe filters (0.45 μm)[4].

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    References

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    PHA-665752
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    HY-11107
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