R&D Systems Inc. Tocris Bioscience Boston Biochem

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.

Certificate of Analysis / Safety Data Sheet

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

References

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.

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.

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.

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

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

Keywords: PHA 665752, supplier, Potent, selective, cMET, inhibitors, Hepatocyte, Growth, Factors, Receptors, HGFR, Receptor, Tyrosine, Kinases, RTKs, PHA665752, Pfizer

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