SU11274
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.
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Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 568.09 |
Cas No. | 658084-23-2 |
Formula | C28H30CIN5O4S |
Solubility | ≥28.4 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O |
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 |
SDF | Download SDF |
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 |
Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Cell experiment:[1] | |
Cell lines |
Human lung cancer cell line H1993 and NIH3T3 cells expressing drug-sensitive or drug-resistant MET mutants |
Reaction Conditions |
0 ~ 2 μM SU11274 for 16 h incubation |
Applications |
SU11274 efficiently inhibited MET autophosphorylation at kinase tyrosines 1234/1235 in five out of seven cell lines that had been tested, but, concomitantly, dose-dependently increased total MET levels. Small molecule tyrosine kinase inhibitors such as SU11274 could be potentially used to explore a variety of biological events associated with MET tyrosine kinase autophosphorylation (Tyr1234/1235 residues), including cell proliferation, survival, anchorage-independent growth and changes in cellular morphology. |
Note |
The technical data provided above is for reference only. |
References: 1. Leiser D, Pochon B, Blank-Liss W, et al. Targeting of the MET receptor tyrosine kinase by small molecule inhibitors leads to MET accumulation by impairing the receptor downregulation. FEBS Letters, 2014, 588(5): 653-658. |
Description | SU11274 is a selective inhibitor of MET tyrosine kinase with IC50 value of 10 nM. | |||||
Targets | MET | |||||
IC50 | 10 nM |
Quality Control & MSDS
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