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SU11274 | cMET inhibitor

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Price:
$129.00
Catalog #:
C7811-5
Quantity:


Product Description

SU-11274 is an oxindole-based, ATP-competitive, Met inhibitor with activity of 20 nM and is >500-fold selective against a variety of other kinases such as PDGFR, EGFR, cdk2, src, and FGFR. [1] SU11274 induces G1 cell cycle arrest and apoptosis with increased caspase 3 activity. Reduction of phosphorylation in the PI3K and Ras pathway components, such as Akt, GSK-3, and FKHR. [1] SU11274 inhibits cell viability, c-Met/HGF and downstream cell proliferation in c-Met-expressing NSCLC cells. [2]

More recently, SU11274 has been extensively studied for the treatment of hepatocellular carcinoma (HCC). In particular, cells postiive for des-gamma-carboxyprothrombin (DCP), an agent that interacts with c-Met to activate HCC cell growth, were inhibited by SU11274. [3]


Technical information:

Chemical Formula:   C28H30CIN5O4S
CAS #:   658084-23-2
Molecular Weight:   568.09
Purity:   >98%
Appearance:   Yellow
Chemical Name:   (Z)-N-(3-chlorophenyl)-3-((3,5-dimethyl-4-(1-methylpiperazine-4-carbonyl)-1H-pyrrol-2-yl)methylene)-N-methyl-2-oxoindoline-5-sulfonamide
Solubility:   Up to 100 mM in DMSO
Synonyms:   SU11274, SU-11274

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


Reference:

1. Sattler et al., A novel small molecule met inhibitor induces apoptosis in cells transformed by the oncogenic TPR-MET tyrosine kinase. Cancer Res. 2003, 63, 5462-5469. Pubmed ID: 14500382
2. Ma et al., Functional expression and mutations of c-Met and its therapeutic inhibition with SU11274 and small interfering RNA in non-small cell lung cancer. Cancer Res. 2005, 65, 1479-1488. Pubmed ID: 15735036
3. Inagaki et al., Effect of c-Met inhibitor SU11274 on hepatocellular carcinoma cell growth. BioScience Trends 2011, 5(2), 52-56. Pubmed ID: 21572247

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

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