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

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.

Certificate of Analysis / Safety Data Sheet

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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.

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

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.

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.

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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