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3-[3,5-Dimethyl-4-(4-[ 11 C]methylpiperazinecarbonyl)-1 H-pyrrol-2-ylmethylene]-2-oxo-2,3-dihydro-1 H-indole-5-sulfonic acid (3-chlorophenyl)methylamide

3-[3,5-Dimethyl-4-(4-[ 11 C]methylpiperazinecarbonyl)-1 H-pyrrol-2-ylmethylene]-2-oxo-2,3-dihydro-1 H-indole-5-sulfonic acid (3-chlorophenyl)methylamide

Kam Leung

PMID: 20642006

Abstract:

MET is a proto-oncogene that encodes a protein Met, also known as c-Met or hepatocyte growth factor receptor (HGFR) (1). MET is a membrane receptor with tyrosine kinase activity that is essential for embryonic development and wound healing. MET is normally expressed by stem cells, progenitor cells, and cells of epithelial origin, whereas expression of hepatocyte growth factor (HGF), which is the only known ligand of MET, is restricted to cells of mesenchymal origin. Upon HGF stimulation, MET induces several biological responses that lead to invasive growth (2). Abnormal MET activation in cancer correlates with poor prognosis because deregulated MET triggers tumor growth, induces angiogenesis, and activates metastasis (3). MET is deregulated in many types of human malignancies, including kidney, liver, stomach, breast, and brain cancers (2, 4, 5). Inhibition of MET function has been shown to inhibit pathological angiogenesis as well as tumor growth and metastasis (6). 3-[3,5-Dimethyl-4-(4-methylpiperazinecarbonyl)-1H-pyrrol-2-ylmethylene]-2-oxo-2,3-dihydro-1H-indole-5-sulfonic acid (3-chlorophenyl)methylamide (SU11274) is directed against the MET kinase activity that leads to apoptosis and inhibition of cell growth (7). Wu et al. (8) reported the use of 3-[3,5-dimethyl-4-(4-[11C]methylpiperazinecarbonyl)-1H-pyrrol-2-ylmethylene]-2-oxo-2,3-dihydro-1H-indole-5-sulfonic acid (3-chlorophenyl)methylamide ([11C]SU11274) for positron emission tomography (PET) imaging of MET expression in human lung xenografts in mice.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
LS7931243	1-(3-Chlorophenyl)-1H-pyrazol-4-ylboronic acid			Price

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