SU11274

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

SU11274 (PKI-SU11274) 是一种有效的、选择性的、ATP 竞争性的 c-Met 激酶抑制剂，IC50 为 20 nM。

SU11274 (PKI-SU11274) is a potent, selective, ATP-competitive c-Met kinase inhibitor with IC50 of 20 nM, >50-fold selectivity over Bcr-Abl, JAK2, PDGFβR; induces G(1) cell cycle arrest and apoptosis with increased Annexin V staining and caspase 3 activity, specifically regulates cell growth in TPR-MET-transformed BaF3 cells with IC50 of <3 uM, differentially affects the kinase activity and subsequent signaling of various mutant forms of Met (M1268T and H1112Y).

SU11274 exhibits greater than 50-fold selectivity for Met versus Flk and more than 500 times selectivity versus other tyrosine kinases such as FGFR-1, c-src, PDGFbR, and EGFR. SU11274 inhibits the phosphorylation of key regulators of the PI3K pathway, including AKT, FKHR, or GSK3β. SU11274 treatment inhibits the growth of TPR-MET-transformed BaF3 cells in a dose-dependent manner with IC50 of < 3 μM in the absence of interleukin 3, without growth inhibition of BaF3 cells transformed by other oncogenic tyrosine kinases, including BCR-ABL, TEL-JAK2, TEL-ABL, and TEL-PDGFβR. In addition to cell growth, SU11274 treatment significantly inhibits the migration of BaF3. TPR-MET cells by 44.8% and 80% at 1 μM and 5 μM, respectively. SU11274 inhibits HGF-dependent phosphorylation of Met as well as HGF-dependent cell proliferation and motility with an IC50 of 1-1.5 μM. In H69 and H345 cells which have functional Met receptor, SU11274 inhibits the HGF-induced cell growth with IC50 of 3.4 μM and 6.5 μM, respectively. SU11274 induces G1 cell cycle arrest with cells in G1 phase increased from 42.4% to 70.6% at 5 μM, and induces caspase-dependent apoptosis by 24% at 1 μM. SU11274 inhibits cell viability in c-Met-expressing non-small cell lung cancer (NSCLC) cells with IC50 values of 0.8-4.4 μM, and abrogates hepatocyte growth factor-induced phosphorylation of c-Met and its downstream signaling.

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SU 11274 | PKI-SU11274 | SU-11274

Angiogenesis

c-Met/HGFR

CDK2|FGFR1|Flk1|Met|RON

Cancer

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658084-23-2

568.0869

C28H30ClN5O4S

>98% (HPLC)

10 mM in DMSO

O=S(C1=CC2=C(NC(/C2=C\C3=C(C)C(C(N4CCN(C)CC4)=O)=C(C)N3)=O)C=C1)(N(C5=CC=CC(Cl)=C5)C)=O

1H-Indole-5-sulfonamide, N-(3-chlorophenyl)-3-[[3,5-dimethyl-4-[(4-methyl-1-piperazinyl)carbonyl]-1H-pyrrol-2-yl]methylene]-2,3-dihydro-N-methyl-2-oxo-, (3Z)-

(-20℃)

With Ice Pack

≥ 2 years