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.
- 1. Anil Kumar Yadav, et al. "PHA-665752's Antigrowth and Proapoptotic Effects on HSC-3 Human Oral Cancer Cells." Int J Mol Sci. 2024 Mar 1;25(5):2871. PMID: 38474118
- 2. Yu-meng Miao, Ya-jing Zhang, et al. "Oral administration of curcumin ameliorates pulmonary fibrosis in mice through 15d-PGJ2-mediated induction of hepatocyte growth factor in the colon." Acta Pharmacologica Sinica (2020);21 July 2020. PMID: 32694760
- 3. Tong X, Liang R, et al. "Suhuang Antitussive Capsules-Ameliorative Effects on LPS-Induced Sputum Obstruction in Mice Through Promoting HGF Secretion." Front Pharmacol, 10, 1422 2019 Dec 19. PMID: 31920638
- 4. Guan C, Qiao S, et al. "Orally administered berberine ameliorates bleomycin-induced pulmonary fibrosis in mice through promoting activation of PPAR-γ and subsequent expression of HGF in colons." Toxicol Appl Pharmacol. 2018 Mar 15;343:1-15. PMID: 29408570
- 5. Xia Y, Xia YF, et al. "Madecassoside ameliorates bleomycin-induced pulmonary fibrosis in mice through promoting the generation of hepatocyte growth factor via PPAR-γ in colon." Br J Pharmacol. 2016 Apr;173(7):1219-35. PMID: 26750154
| 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
- View current batch:
Chemical structure
Related Biological Data
Related Biological Data
Related Biological Data
Related Biological Data
Related Biological Data
Related Biological Data
Related Biological Data
