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SU11274

Catalog No. T6154 CAS 658084-23-2

Synonyms: Met Kinase Inhibitor, PKI-SU11274

SU11274 (Met Kinase Inhibitor)(IC50=10 nM) is a specific Met inhibitor. It shows no significant effects on PGDFRβ, EGFR or Tie2.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

SU11274, CAS 658084-23-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 39.00
2 mg	In stock	$ 54.00
5 mg	In stock	$ 98.00
10 mg	In stock	$ 153.00
25 mg	In stock	$ 297.00
50 mg	In stock	$ 490.00
100 mg	In stock	$ 725.00
1 mL * 10 mM (in DMSO)	In stock	$ 153.00

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Purity: 98.62%

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Description	SU11274 (Met Kinase Inhibitor)(IC50=10 nM) is a specific Met inhibitor. It shows no significant effects on PGDFRβ, EGFR or Tie2.
Targets&IC50	MET:0.01 μM
In vivo	SU11274 inhibits the phosphorylation of key regulators in the PI3K pathway, including AKT, FKHR, and GSK3β. It also inhibits the HGF-dependent phosphorylation of Met and the subsequent HGF-dependent cellular proliferation and activity, with an IC50 ranging from 1 to 1.5 μM. In BaF3 cells transformed by TPR-MET, the presence of interleukin-3 and treatment with SU11274 suppress cell growth in a dose-dependent manner. However, SU11274 (IC50 <3 μM) does not inhibit the growth of BaF3 cells transformed by other oncogenic tyrosine kinases, including BCR-ABL, TEL-JAK2, TEL-ABL, and TEL-PDGFβR. Treatment with SU11274 also significantly inhibits cell migration in BaF3.TPR-MET cells with inhibitions of 44.8% and 80% at concentrations of 1 μM and 5 μM, respectively. In H69 and H345 cells, which possess functional Met receptors, SU11274 inhibits HGF-induced cell growth with IC50 values of 3.4 μM and 6.5 μM, respectively. In non-small cell lung cancer (NSCLC) cells expressing c-Met, SU11274 inhibits cell viability with an IC50 of 0.8-4.4 μM and abrogates the phosphorylation of c-Met and its downstream signaling induced by hepatocyte growth factor.
Kinase Assay	In vitro Met kinase assay: A chimeric protein is constructed containing the cytoplasmic domain of human c-Met fused to Glutathione S-transferase (GST) and expressed in SF9 cells. The c-Met kinase GST-fusion protein is used for an ELISA-based Met biochemical assay using the random copolymer poly(Glu:Tyr) (4:1) immobilized on microtiter plates as a substrate. IC50 value is determined with various concentrations of SU11274 in a buffer containing 5 μM ATP and 10 mM MnCl2, 50 mM HEPES (pH 7.5), 25 mM NaCl, 0.01% BSA, and 0.1 mM Na orthovanadate. The kinase reaction is performed for 5 minutes at room temperature. The extent of substrate phosphorylation is measured using horseradish peroxidase-conjugated anti-pTyr antibodies.
Cell Research	Cells are exposed to various concentrations of SU11274 in the presence or absence of HGF for 24, 48, and 72 hours. The number of viable cells is determined using the MTT assay or trypan blue exclusion. Cell Cycle and apoptosis are measured by fluorescence-activated cell sorter analysis via propidium iodide staining and Annexin V-positive staining, respectively. (Only for Reference)

Synonyms	Met Kinase Inhibitor, PKI-SU11274
Molecular Weight	568.09
Formula	C28H30ClN5O4S
CAS No.	658084-23-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 2 mg/mL (3.52 mM)

DMSO: 85 mg/mL (149.6 mM)

References and Literature

1. Wang X, et al. Mol Cancer Ther, 2003, 2(11):1085-1092. 2. Sattler M, et al. Cancer Res, 2003, 63(17), 5462-5469. 3. Ma PC, et al. Cancer Res, 2005, 65(4), 1479-1488.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Kinase Inhibitor Library Inhibitor Library Tyrosine Kinase Inhibitor Library Bioactive Compound Library Anti-Fibrosis Compound Library Reprogramming Compound Library Osteogenesis Compound Library Anti-Aging Compound Library Angiogenesis related Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

SU11274 658084-23-2 Angiogenesis Apoptosis Autophagy Cell Cycle/Checkpoint Tyrosine Kinase/Adaptors c-Met/HGFR FGFR VEGFR CDK SU-11274 PKI-SU-11274 Inhibitor Met Kinase Inhibitor PKI-SU11274 inhibit SU 11274 PKI-SU 11274 inhibitor

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