C-Met inhibitor,potent and selective
CAS：658084-23-2
分子式：C28H30CIN5O4S
分子量：568.09
纯度：98%
存储：Store at -20°C

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].

参考文献:
[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.