PHA 665752

Cat. No. 2693

PHA 665752 C32H34Cl2N4O4S [477575-56-7]

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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 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.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Technical Data

Soluble to 100 mM in DMSO
>98 %
Store at +4°C

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.

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch
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Safety Data Sheet: View Safety Data Sheet

Tu et al (2010) Efficacy of c-Met inhibitor for advanced prostate cancer. BMC Cancer 10 556. PMID: 20946682.

Puri et al (2007) A selective small molecule inhibitor of c-Met, PHA665752, inhibits tumorigenicity and angiogenesis in mouse lung cancer xenografts. Cancer Res. 67 3529. PMID: 17440059.

Smolen et al (2006) Amplification of MET may identify a subset of cancers with extreme sensitivity to the selective tyrosine kinase inhibitor PHA-665752. Proc.Natl.Acad.Sci.USA 103 2316.

Christensen et al (2003) A selective small molecule inhibitor of c-Met kinase inhibits c-Met-dependent phenotypes in vitro and exhibits cytoreductive antitumour activity in vivo. Cancer Res. 63 7345. PMID: 14612533.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for PHA 665752 include:

Valente et al (2016) Hepatocyte Growth Factor Effects on Mesenchymal Stem Cells Derived from Human Arteries: A Novel Strategy to Accelerate Vascular Ulcer Wound Healing. J Clin Invest 2016 3232859. PMID: 26788066.

Ito et al (2015) Influenza induces IL-8 and GM-CSF secretion by human alveolar epithelial cells through HGF/c-Met and TGF-α/EGFR signaling. Stem Cells Int 308 L1178. PMID: 26033355.

Jiang et al (2015) YangZheng XiaoJi exerts anti-tumour growth effects by antagonising the effects of HGF and its receptor, cMET, in human lung cancer cells. Am J Physiol Lung Cell Mol Physiol 13 280. PMID: 26310485.

Saito et al (2015) The role of HGF/MET and FGF/FGFR in fibroblast-derived growth stimulation and lapatinib-resistance of esophageal squamous cell carcinoma. BMC Cancer 15 82. PMID: 25884729.

Breindel et al (2013) EGF receptor activates MET through MAPK to enhance non-small cell lung carcinoma invasion and brain metastasis. Cancer Res 73 5053. PMID: 23794705.

Grugan et al (2013) A common p53 mutation (R175H) activates c-Met receptor tyrosine kinase to enhance tumor cell invasion. J Transl Med 14 853. PMID: 23792586.

Katayama et al (2013) Cytotoxic activity of tivantinib (ARQ 197) is not due solely to c-MET inhibition. Cancer Res 73 3087. PMID: 23598276.

Wu et al (2013) C1GALT1 enhances proliferation of hepatocellular carcinoma cells via modulating MET glycosylation and dimerization. Cancer Res 73 5580. PMID: 23832667.

Accornero et al (2012) Met receptor acts uniquely for survival and morphogenesis of EGFR-dependent normal mammary epithelial and cancer cells. PLoS One 7 e44982. PMID: 23028720.

Goodnough et al (2012) Inhibition of hepcidin transcription by growth factors. Hepatology 56 291. PMID: 22278715.

Muller et al (2012) Passenger deletions generate therapeutic vulnerabilities in cancer. Nature 488 337. PMID: 22895339.

Jiao et al (2011) Targeting HSP90 in ovarian cancers with multiple receptor tyrosine kinase coactivation. Mol Cancer 10 125. PMID: 21962244.

Okamoto et al (2011) Differential roles of STAT3 depending on the mechanism of STAT3 activation in gastric cancer cells. Br J Cancer 105 407. PMID: 21730976.

Qi et al (2011) Multiple mutations and bypass mechanisms can contribute to development of acquired resistance to MET inhibitors. Cancer Res 71 1081. PMID: 21266357.

Tanizaki et al (2011) Differential roles of trans-phosphorylated EGFR, HER2, HER3, and RET as heterodimerisation partners of MET in lung cancer with MET amplification. Br J Cancer 105 807. PMID: 21847121.

Yang et al (2011) Using tandem mass spectrometry in targeted mode to identify activators of class IA PI3K in cancer. Cancer Res 71 5965. PMID: 21775521.

Costa et al (2010) Fumarase tumor suppressor gene and MET oncogene cooperate in upholding transformation and tumorigenesis. FASEB J 24 2680. PMID: 20354140.

Hoot et al (2010) HGF upregulation contributes to angiogenesis in mice with keratinocyte-specific Smad2 deletion. J Clin Invest 120 3606. PMID: 20852387.

Kongkham et al (2010) Inhibition of the MET Receptor Tyrosine Kinase as a Novel Therapeutic Strategy in Medulloblastoma. Nat Commun 3 336. PMID: 21151472.

Qin et al (2010) Failure to ubiquitinate c-Met leads to hyperactivation of mTOR signaling in a mouse model of autosomal dominant polycystic kidney disease. Transl Oncol 120 3617. PMID: 20852388.

Kawaguchi et al (2009) Combined inhibition of MET and EGFR suppresses proliferation of malignant mesothelioma cells. Carcinogenesis 30 1097. PMID: 19380521.

Sierra et al (2008) Tumor angiogenesis and progression are enhanced by Sema4D produced by tumor-associated macrophages. J Exp Med 205 1673. PMID: 18559453.

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Keywords: PHA 665752, supplier, Potent, selective, cMET, inhibitors, inhibits, Hepatocyte, Growth, Factors, Receptors, HGFR, Receptor, Tyrosine, Kinases, RTKs, PHA665752, Pfizer, Tocris Bioscience, MET Receptor Inhibitor products

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