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Enzymes for Research, Diagnostic and Industrial Use

SU11274

Cat No.
CEI-0071
Description
SU11274 can inhibit c-MET with IC50 of 12 nM.
Alias
PKI-SU11274
CAS No.
658084-23-2
Molecular Weight
568.09
Purity
>99%
Storage
2 years at -20centigrade Powder
Synonyms
PKI-SU11274
Targets
c-MET
Molecular Formula
C28H30CIN5O4S
Chemical Name
(Z)-N-(3-chlorophenyl)-3-((3,5-dimethyl-4-(1-methylpiperazine-4-carbonyl)-1H-pyrrol-2-yl)methylene)-N-methyl-2-oxoindoline-5-sulfonamide
Solubility
DMSO 92 mg/mL Water
In vitro
SU11274 can inhibit c-MET with IC50 of 12 nM. SU11274 differentially affects the kinase activity and subsequent signaling of various mutant forms of Met. SU11274 inhibit Met variants, M1268T and H1112Y, with IC50 of 2 uM, but shows little inhibition to Met variants, L1213V and Y1248H. For cell lines (1) NSCLC As a selective small molecule inhibitor of c-Met, SU11274 inhibited cell viability in c-Met-expressing NSCLC cells. SU11274 abrogated hepatocyte growth factor-induced phosphorylation of c-Met and its downstream signaling. (2) Ovarian carcinoma cells As c-Met is overexpressed in the majority of malignant ovarian epithelial cells, SU11274 can significantly decreased cell motility and invasion of ovarian carcinoma cells by decreasing activated c-Met.
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