SU11274
Catalog No.S1080 Synonyms: PKI-SU11274
Molecular Weight(MW): 568.09
SU11274 is a selective Met inhibitor with IC50 of 10 nM in cell-free assays, no effects on PGDFRβ, EGFR or Tie2.
6 Customer Reviews
-
Inhibition of c-MET sensitizes PTEN deficient tumor cells to EGFR TKI-induced apoptosis. PTEN deficient TGFα-EGFRWT;InkΔ2/3-/-;PTENlox GBM tumor cells were treated with gefitinib (10 uM) and/or the c-MET kinase inhibitor SU11274 (10 uM). Immunoblot analysis of total cell lysates from TGFα-EGFRWT;InkΔ2/3-/-;PTENlox GBM tumor cells treated with the indicated inhibitors using c-MET and c-MET phosphotyrosine 1234,1235 antibodies. Anti β-tubulin probing is used as an internal loading control.
Oncogene 2012 31(25), 3039-50. SU11274 purchased from Selleck.
Human umbilical vein endothelial cells (HUVECs) were stained for cortactin (green)/vinculin (red; top) and for zyxin (green)/actin (red; bottom). On RCαβ treatment for 30 to 40 minutes, vinculin disappeared from large focal adhesions underneath the cell body, whereas it appeared in small focal contacts around the cell perimeter. In addition, cortactin was found in the cortical actin network within nascent lamellipodia. Furthermore, zyxin, a marker of focal adhesions, and stress fibers disappeared on RCαβ treatment. Pretreatment of HUVECs with 10 umol/L SU11274 reduced the effect of 200 nmol/L RCαβ, whereas 200 ng/mL hepatocyte growth factor (HGF) elicited similar responses to RCαβ, indicating a signaling path involving cMet. Scale bars, 10 um.
Arterioscler Thromb Vasc Biol 2013 33(3), 544-54. SU11274 purchased from Selleck.
-
Effect of crizotinib, tivantinib, and SU11274 on levels of c-MET phosphorylation and downstream signaling pathway in SW1736 and TL3 thyroid cancer cells. Cells were prestarved in culture medium containing 0.5% FBS (24 hour) ?either crizotinib or tivantinib (0.1, 1.0, and 10 umol/L) or SU11274 (10 umol/L), and stimulated with 20 ng/mL recombinant human HGF for 10 minutes before lysates were made for Western blotting. A series of c-MET downstream signaling pathway proteins and phosphor proteins were detected using Western blotting. β-Actin was used as a loading balance control.
Mol Cancer Ther 2014 13(1), 134-43. SU11274 purchased from Selleck.
Expression of miR-200c and miR-27b after hepatocyte growth factor (HGF) stimulation using qRT-PCR analysis. This downregulation of miR-220c and miR-27b was almost completely inhibited by adding MET kinase-specific inhibitor SU11274 before HGF stimulation.
Cancer Sci 2011 102, 2164-71. SU11274 purchased from Selleck.
-
HLMVECs grown to -95% confluence on slide chambers were pretreated with 1 uM SU11274 for 1 h prior to stimulation with HGF (20 ng/ml) for 15 min. Cells were washed, fixed, and stained for actin and cortactin co-localization in lamellipodia as described under "Experimental Procedures." Nuclei were stained with DAPI. Shown are representative immunofluorescence images from three independent experiments. Actin and cortactin co-localization in lamellipodia was quantified using image analysis as described under "Experimental Procedures."
J Biol Chem 2014 289(19), 13476-91. SU11274 purchased from Selleck.
Western blot analysis of c-Met, MAPK and Akt. 0-20μM SU11724 was added.
Dr. Zhang of Tianjin Medical University. SU11274 purchased from Selleck.
Purity & Quality Control
Choose Selective c-Met Inhibitors
Biological Activity
| Description | SU11274 is a selective Met inhibitor with IC50 of 10 nM in cell-free assays, no effects on PGDFRβ, EGFR or Tie2. | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Targets |
|
||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| In vitro |
SU11274 exhibits greater than 50-fold selectivity for Met versus Flk and more than 500 times selectivity versus other tyrosine kinases such as FGFR-1, c-src, PDGFbR, and EGFR. SU11274 inhibits the phosphorylation of key regulators of the PI3K pathway, including AKT, FKHR, or GSK3β. SU11274 treatment inhibits the growth of TPR-MET-transformed BaF3 cells in a dose-dependent manner with IC50 of <3 μM in the absence of interleukin 3, without growth inhibition of BaF3 cells transformed by other oncogenic tyrosine kinases, including BCR-ABL, TEL-JAK2, TEL-ABL, and TEL-PDGFβR. In addition to cell growth, SU11274 treatment significantly inhibits the migration of BaF3. TPR-MET cells by 44.8% and 80% at 1 μM and 5 μM, respectively. SU11274 inhibits HGF-dependent phosphorylation of Met as well as HGF-dependent cell proliferation and motility with an IC50 of 1-1.5 μM. In H69 and H345 cells which have functional Met receptor, SU11274 inhibits the HGF-induced cell growth with IC50 of 3.4 μM and 6.5 μM, respectively. SU11274 induces G1 cell cycle arrest with cells in G1 phase increased from 42.4% to 70.6% at 5 μM, and induces caspase-dependent apoptosis by 24% at 1 μM. [2] SU11274 inhibits cell viability in c-Met-expressing non-small cell lung cancer (NSCLC) cells with IC50 values of 0.8-4.4 μM, and abrogates hepatocyte growth factor-induced phosphorylation of c-Met and its downstream signaling. [3] |
||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Cell Data |
|
Protocol
| Kinase Assay:[1] |
+ Expand
In vitro Met kinase assay: A chimeric protein is constructed containing the cytoplasmic domain of human c-Met fused to Glutathione S-transferase (GST) and expressed in SF9 cells. The c-Met kinase GST-fusion protein is used for an ELISA-based Met biochemical assay using the random copolymer poly(Glu:Tyr) (4:1) immobilized on microtiter plates as a substrate. IC50 value is determined with various concentrations of SU11274 in a buffer containing 5 μM ATP and 10 mM MnCl2, 50 mM HEPES (pH 7.5), 25 mM NaCl, 0.01% BSA, and 0.1 mM Na orthovanadate. The kinase reaction is performed for 5 minutes at room temperature. The extent of substrate phosphorylation is measured using horseradish peroxidase-conjugated anti-pTyr antibodies. |
|---|---|
| Cell Research:[2] |
+ Expand
|
Solubility (25°C)
| In vitro | DMSO | 92 mg/mL (161.94 mM) |
|---|---|---|
| Ethanol | 2 mg/mL (3.52 mM) | |
| Water | Insoluble | |
| In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 30% PEG400+0.5% Tween80+5% propylene glycol For best results, use promptly after mixing. |
30 mg/mL |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 568.09 |
|---|---|
| Formula | C28H30CIN5O4S |
| CAS No. | 658084-23-2 |
| Storage | powder |
| in solvent | |
| Synonyms | PKI-SU11274 |
Bio Calculators
Molarity Calculator
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Dilution Calculator
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Molarity Calculator
Tech Support
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.
Frequently Asked Questions
-
Question 1:
What is the solubility of S1080 SU11274 in acetone?
-
Answer:
The solubility of S1080 SU11274 in acetone is 7 mg/mL.
