PHA 665752

  ( 31 citations )    
Product Datasheet
Catalog Number:2693
Chemical Name:(2R)-1-[[5-[(Z)-[5-[[(2,6-Dichlorophenyl)methyl]sulfonyl]-1,2-dihydro-2-oxo-3H-indol-3-ylidene]methyl]-2,4-dimethyl-1H-pyrrol-3-yl]carbonyl]-2-(1-pyrrolidinylmethyl)pyrrolidine
Product Details
Citations (31)
Supplemental Products
Reviews
Biological Activity
Potent, selective and ATP-competitive inhibitor of MET kinase (IC50 values are 9, 68, 200, 1400, 3000, 3800 and 6000 nM for MET, Ron, Flk-1, c-abl, FGFR1, EGFR and c-src respectively and > 10000 nM for IGF-IR, PDGFR, AURORA2, PKA, PKBα, p38α, MK2 and MK3). Antitumor agent; inhibits tumorigenicity and angiogenesis in mouse lung cancer xenografts.
Technical Data
  • M.Wt:
    641.61
  • Formula:
    C32H34Cl2N4O4S
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
    >98
  • Storage:
    Store at +4°C
  • CAS No:
    477575-56-7
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Additional Information
Licensing Caveats:
Sold for research purposes under agreement from Pfizer Inc.
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Citations:

The citations listed below are publications that use Tocris products. Selected citations for PHA 665752 include:

31 Citations: Showing 1 - 10
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  1. Longitudinal tracking of subpopulation dynamics and molecular changes during LNCaP cell castration and identification of inhibitors that could target the PSA-/lo castration-resistant cells.
    Authors: Rycaj Et al.
    Oncotarget  2016;7:14220
  2. Hepatocyte Growth Factor Effects on Mesenchymal Stem Cells Derived from Human Arteries: A Novel Strategy to Accelerate Vascular Ulcer Wound Healing.
    Authors: Valente Et al.
    J Clin Invest  2016;2016:3232859
  3. Influenza induces IL-8 and GM-CSF secretion by human alveolar epithelial cells through HGF/c-Met and TGF-α/EGFR signaling.
    Authors: Ito Et al.
    Stem Cells Int  2015;308:L1178
  4. The role of HGF/MET and FGF/FGFR in fibroblast-derived growth stimulation and lapatinib-resistance of esophageal squamous cell carcinoma.
    Authors: Saito Et al.
    BMC Cancer  2015;15:82
  5. Effects of AKT inhibition on HGF-mediated erlotinib resistance in non-small cell lung cancer cell lines.
    Authors: Holland Et al.
    J Cancer Res Clin Oncol  2015;141:615
  6. YangZheng XiaoJi exerts anti-tumour growth effects by antagonising the effects of HGF and its receptor, cMET, in human lung cancer cells.
    Authors: Jiang Et al.
    Am J Physiol Lung Cell Mol Physiol  2015;13:280
  7. Disentangling the Complexity of HGF Signaling by Combining Qualitative and Quantitative Modeling.
    Authors: D'Alessandro Et al.
    PLoS Comput Biol  2015;11:e1004192
  8. Multipoint targeting of the PI3K/mTOR pathway in mesothelioma.
    Authors: Zhou Et al.
    Br J Cancer  2014;110:2479
  9. C1GALT1 enhances proliferation of hepatocellular carcinoma cells via modulating MET glycosylation and dimerization.
    Authors: Wu Et al.
    Cancer Res  2013;73:5580
  10. EGF receptor activates MET through MAPK to enhance non-small cell lung carcinoma invasion and brain metastasis.
    Authors: Breindel Et al.
    Cancer Res  2013;73:5053
  11. Cytotoxic activity of tivantinib (ARQ 197) is not due solely to c-MET inhibition.
    Authors: Katayama Et al.
    Cancer Res  2013;73:3087
  12. Multipotent Human Mesenchymal Stromal Cells Mediate Expansion of Myeloid-Derived Suppressor Cells via Hepatocyte Growth Factor/c-Met and STAT3.
    Authors: Yen Et al.
    Stem Cell Reports  2013;1:139
  13. A common p53 mutation (R175H) activates c-Met receptor tyrosine kinase to enhance tumor cell invasion.
    Authors: Grugan Et al.
    J Transl Med  2013;14:853
  14. Met receptor acts uniquely for survival and morphogenesis of EGFR-dependent normal mammary epithelial and cancer cells.
    Authors: Accornero Et al.
    PLoS One  2012;7:e44982
  15. Inhibition of hepcidin transcription by growth factors.
    Authors: Goodnough Et al.
    Hepatology  2012;56:291
  16. Passenger deletions generate therapeutic vulnerabilities in cancer.
    Authors: Muller Et al.
    Nature  2012;488:337
  17. Using tandem mass spectrometry in targeted mode to identify activators of class IA PI3K in cancer.
    Authors: Yang Et al.
    Cancer Res  2011;71:5965
  18. Multiple mutations and bypass mechanisms can contribute to development of acquired resistance to MET inhibitors.
    Authors: Qi Et al.
    Cancer Res  2011;71:1081
  19. Targeting HSP90 in ovarian cancers with multiple receptor tyrosine kinase coactivation.
    Authors: Jiao Et al.
    Mol Cancer  2011;10:125
  20. Differential roles of trans-phosphorylated EGFR, HER2, HER3, and RET as heterodimerisation partners of MET in lung cancer with MET amplification.
    Authors: Tanizaki Et al.
    Br J Cancer  2011;105:807
  21. Differential roles of STAT3 depending on the mechanism of STAT3 activation in gastric cancer cells.
    Authors: Okamoto Et al.
    Br J Cancer  2011;105:407
  22. Induction of MET by ionizing radiation and its role in radioresistance and invasive growth of cancer.
    Authors: Bacco Et al.
    J Natl Cancer Inst  2011;103:645
  23. MET and KRAS gene amplification mediates acquired resistance to MET tyrosine kinase inhibitors.
    Authors: Cepero Et al.
    Cancer Res  2010;70:7580
  24. Inhibition of the MET Receptor Tyrosine Kinase as a Novel Therapeutic Strategy in Medulloblastoma.
    Authors: Kongkham Et al.
    Nat Commun  2010;3:336
  25. Fumarase tumor suppressor gene and MET oncogene cooperate in upholding transformation and tumorigenesis.
    Authors: Costa Et al.
    FASEB J  2010;24:2680
  26. Failure to ubiquitinate c-Met leads to hyperactivation of mTOR signaling in a mouse model of autosomal dominant polycystic kidney disease.
    Authors: Qin Et al.
    Transl Oncol  2010;120:3617
  27. HGF upregulation contributes to angiogenesis in mice with keratinocyte-specific Smad2 deletion.
    Authors: Hoot Et al.
    J Clin Invest  2010;120:3606
  28. A gene-alteration profile of human lung cancer cell lines.
    Authors: Blanco Et al.
    Hum Mutat  2009;30:1199
  29. Combined inhibition of MET and EGFR suppresses proliferation of malignant mesothelioma cells.
    Authors: Kawaguchi Et al.
    Carcinogenesis  2009;30:1097
  30. Novel multicellular organotypic models of normal and malignant breast: tools for dissecting the role of the microenvironment in breast cancer progression.
    Authors: Holliday Et al.
    Breast Cancer Res  2009;11:R3
  31. Tumor angiogenesis and progression are enhanced by Sema4D produced by tumor-associated macrophages.
    Authors: Sierra Et al.
    J Exp Med  2008;205:1673
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