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SU11274

In stock
Catalog No.
A2678
C-Met inhibitor,potent and selective
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$169.00
In stock
5mg
$70.00
In stock
25mg
$300.00
In stock
100mg
$800.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

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Background

SU11274 is a potent and selective inhibitor of Met kinase with IC50 value of 10nM [1].

SU11274 shows high selectivity toward Met kinase versus a serine/threonine kinase, cyclin-dependent kinase 2 (CDK2), or other receptor tyrosine kinases, including epidermal growth factor receptor (EGFR) and platelet-derived growth factor receptor β (PDGFRβ) [1].

SU11274  has revealed to inhibit autophosphorylation of Met at kinase tyrosines 1234/1235 in NIH3T3 cells expressing drug-sensitive or drug-resistant MET mutants and human lung cancer cell line H1993, however, concomitantly, increase total MET levels dose-dependently. Cells treated with SU11274 (2 μM for 16 h) has shown a reduction of Met Ubiquitination [2].

References:
[1] Wang X1, Le P, Liang C, Chan J, Kiewlich D, Miller T, Harris D, Sun L, Rice A, Vasile S, Blake RA, Howlett AR, Patel N, McMahon G, Lipson KE. Potent and selective inhibitors of the Met [hepatocyte growth factor/scatter factor (HGF/SF) receptor] tyrosine kinase block HGF/SF-induced tumor cell growth and invasion. Mol Cancer Ther. 2003 Nov;2(11):1085-92.
[2] Leiser D1, Pochon B1, Blank-Liss W1, Francica P1, Glück AA1, Aebersold DM1, Zimmer Y1, Medová M2. Targeting of the MET receptor tyrosine kinase by small molecule inhibitors leads to MET accumulation by impairing the receptor downregulation. FEBS Lett. 2014 Mar 3;588(5):653-8.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt568.09
Cas No.658084-23-2
FormulaC28H30CIN5O4S
Solubility≥28.4mg/mL in DMSO
Chemical Name(3Z)-N-(3-chlorophenyl)-3-[[3,5-dimethyl-4-(4-methylpiperazine-1-carbonyl)-1H-pyrrol-2-yl]methylidene]-N-methyl-2-oxo-1H-indole-5-sulfonamide
SDFDownload SDF
Canonical SMILESCC1=C(NC(=C1C(=O)N2CCN(CC2)C)C)C=C3C4=C(C=CC(=C4)S(=O)(=O)N(C)C5=CC(=CC=C5)Cl)NC3=O
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description SU11274 is a selective inhibitor of MET tyrosine kinase with IC50 value of 10 nM.
Targets MET          
IC50 10 nM          

Quality Control

Quality Control & MSDS

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Chemical structure

SU11274

Related Biological Data

SU11274
SU12274 abrogated the inhibition effects of compound A on pulmonary fibrosis induced by BLM.
Method:HE staining; Animal:Female ICR mice; Dose:SU12274 (0.18 mg/kg, intraperitoneal injection); Incubation Time:Daily, for 21 days.

Related Biological Data

SU11274
SU12274 abrogated the inhibition effects of compound A on pulmonary fibrosis induced by BLM.
Method:Masson's staining; Animal:Female ICR mice; Dose:SU12274 (0.18 mg/kg, intraperitoneal injection); Incubation Time:Daily, for 21 days.

Related Biological Data

SU11274
The c-met antagonist (SU11274) abrogated the inhibition effects of A on both lung index and Hyp level in lung tissues after mice were treated with BLM.

Related Biological Data

SU11274

Related Biological Data

SU11274