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Category:
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Enzyme-Linked Receptors Receptor Tyrosine Kinases (RTKs)HGF
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Cat.No.
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Product Name
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2693 |
PHA 665752
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Price and Availability
Click here for full price details of
PHA 665752
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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 cMET kinase (IC50 values are 9, 68, 200, 1400, 3000, 3800 and
6000 nM for cMET, Ron, Flk-1, c-abl, FGFR1, EGFR and c-src respectively and
> 10000 nM for IGF1R, PDGFR, AURORA2, PKA, PKBα, p38α, MK2 and
MK3). Antitumor agent; inhibits tumourigenicity and angiogenesis in mouse lung
cancer xenografts.
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Technical Data:
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Resources:
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Certificate of Analysis / MSDS:
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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.
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or by Research Area
Keywords: PHA 665752, Receptor Tyrosine Kinases (RTKs), Potent & Selective CMET Inhibitor, PHA665752, Tocris Bioscience
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Literature in this Area Cancer Research Guide | Our unique collection of more than 300 products related to cancer research, including the very latest exclusive research tools. | | Request Copy / View PDF |
Product Feature
Kinase Inhibitors
Key kinase Inhibitors available from Tocris include:
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