SU11274 (Synonyms: Met Kinase Inhibitor) |
Catalog No.GC11089
One-Click Copy Product Info
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C-Met inhibitor,potent and selective
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 658084-23-2
Sample solution is provided at 25 µL, 10mM.
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.
Kinase experiment: | 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 experiment: | Cells are exposed to various concentrations of SU11274 in the presence or absence of HGF for 24, 48, and 72 hours. The number of viable cells is determined using the MTT assay or trypan blue exclusion. Cell Cycle and apoptosis are measured by fluorescence-activated cell sorter analysis via propidium iodide staining and Annexin V-positive staining, respectively. |
References: [1]. Wang X, et al. 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, 2(11):1085-1092. | |
| Cas No. | 658084-23-2 | SDF | |
| Synonyms | Met Kinase Inhibitor | ||
| 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 | ||
| Canonical SMILES | CC1=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 | ||
| Formula | C28H30CIN5O4S | M.Wt | 568.09 |
| Solubility | ≥ 28.4mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7603 mL | 8.8014 mL | 17.6028 mL |
| 5 mM | 352.1 μL | 1.7603 mL | 3.5206 mL |
| 10 mM | 176 μL | 880.1 μL | 1.7603 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 38 reference(s) in Google Scholar.)