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Home »
Pharmacology » Enzyme-Linked Receptors » Receptor Tyrosine Kinases (RTKs) » MET Receptors » PHA 665752
PHA 665752Cat No. 2693 |
Price and Availability |
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Chemical Name: (2R)-1-[[5-[(Z)-[5-[[(2,6-Dichlorophenyl)methyl]sulfony l]-1,2-dihydro-2-oxo-3H-indol-3-ylidene]methyl]-2,4-dim ethyl-1H-pyrrol-3-yl]carbonyl]-2-(1-pyrrolidinylmethyl) pyrrolidine |
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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 IncTechnical 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 and MSDS.
Resources
Certificate of Analysis / MSDS
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Material Safety Data Sheet: View current batch
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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. 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.If you know of a useful citation for this product please let us know.
Keywords: PHA 665752, Potent, selective, cMET, inhibitors, Hepatocyte, Growth, Factor, Receptors, HGFR, Receptor, Tyrosine, Kinases, RTKs, PHA665752, Pfizer
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