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
Biological ActivityPHA 665752 is a 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.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
A selective small molecule inhibitor of c-Met kinase inhibits c-Met-dependent phenotypes in vitro and exhibits cytoreductive antitumour activity in vivo.
Christensen et al.
Cancer Res., 2003;63:7345
A selective small molecule inhibitor of c-Met, PHA665752, inhibits tumorigenicity and angiogenesis in mouse lung cancer xenografts.
Puri et al.
Cancer Res., 2007;67:3529
Efficacy of c-Met inhibitor for advanced prostate cancer.
Tu et al.
BMC Cancer, 2010;10:556
Amplification of MET may identify a subset of cancers with extreme sensitivity to the selective tyrosine kinase inhibitor PHA-665752.
Smolen et al.
Citations for PHA 665752
The citations listed below are publications that use Tocris products. Selected citations for PHA 665752 include:
34 Citations: Showing 1 - 10
Hepatocyte Growth Factor Regulates Macrophage Transition to the M2 Phenotype and Promotes Murine Skeletal Muscle Regeneration.
Authors: Choi Et al.
Front Physiol 2019;10:914
Genomic and Molecular Screenings Identify Different Mechanisms for Acquired Resistance to MET Inhibitors in Lung Cancer Cells.
Authors: Gimenez-Xavier Et al.
Mol Cancer Ther 2017;16:1366
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.
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
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
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
Effects of AKT inhibition on HGF-mediated erlo. resistance in non-small cell lung cancer cell lines.
Authors: Holland Et al.
J Cancer Res Clin Oncol 2015;141:615
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
Disentangling the Complexity of HGF Signaling by Combining Qualitative and Quantitative Modeling.
Authors: D'Alessandro Et al.
PLoS Comput Biol 2015;11:e1004192
Multipoint targeting of the PI3K/mTOR pathway in mesothelioma.
Authors: Zhou Et al.
Br J Cancer 2014;110:2479
C1GALT1 enhances proliferation of hepatocellular carcinoma cells via modulating MET glycosylation and dimerization.
Authors: Wu Et al.
Cancer Res 2013;73:5580
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
Cytotoxic activity of tivantinib (ARQ 197) is not due solely to c-MET inhibition.
Authors: Katayama Et al.
Cancer Res 2013;73:3087
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
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
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
Inhibition of hepcidin transcription by growth factors.
Authors: Goodnough Et al.
Passenger deletions generate therapeutic vulnerabilities in cancer.
Authors: Muller Et al.
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
Multiple mutations and bypass mechanisms can contribute to development of acquired resistance to MET inhibitors.
Authors: Qi Et al.
Cancer Res 2011;71:1081
Targeted inhibition of multiple receptor tyrosine kinases in mesothelioma.
Authors: Ou Et al.
Targeting HSP90 in ovarian cancers with multiple receptor tyrosine kinase coactivation.
Authors: Jiao Et al.
Mol Cancer 2011;10:125
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
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
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
MET and KRAS gene amplification mediates acquired resistance to MET tyrosine kinase inhibitors.
Authors: Cepero Et al.
Cancer Res 2010;70:7580
Inhibition of the MET Receptor Tyrosine Kinase as a Novel Therapeutic Strategy in Medulloblastoma.
Authors: Kongkham Et al.
Nat Commun 2010;3:336
Fumarase tumor suppressor gene and MET oncogene cooperate in upholding transformation and tumorigenesis.
Authors: Costa Et al.
FASEB J 2010;24:2680
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
HGF upregulation contributes to angiogenesis in mice with keratinocyte-specific Smad2 deletion.
Authors: Hoot Et al.
J Clin Invest 2010;120:3606
A gene-alteration profile of human lung cancer cell lines.
Authors: Blanco Et al.
Hum Mutat 2009;30:1199
Combined inhibition of MET and EGFR suppresses proliferation of malignant mesothelioma cells.
Authors: Kawaguchi Et al.
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
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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