SU11274

SKU: orb1301028

Description

SU11274 is a potent and selective Met kinase inhibitor with an IC50 of 10 nM. It demonstrates minimal activity against related kinases such as PGDFRβ, EGFR, and Tie2. This inhibitor is widely used in cancer research for in vitro and in vivo studies investigating Met-driven tumorigenesis and metastasis.

Research Area

Cardiovascular Research, Cell Biology, Signal Transduction

Key Properties

• CAS Number: 658084-23-2
• MW: 568.09
• Purity: 99.44%
• Formula: C₂₈H₃₀ClN₅O₄S
• SMILES: C(=C\1/C=2C(NC1=O)=CC=C(S(N(C)C3=CC(Cl)=CC=C3)(=O)=O)C2)\C4=C(C)C(C(=O)N5CCN(C)CC5)=C(C)N4
• Target: FGFR,c-Met/HGFR,VEGFR,Apoptosis,Autophagy,CDK
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (5.81 mM);Ethanol:2 mg/mL (3.52 mM);DMSO:48.33 mg/mL (85.07 mM)

Bioactivity

• Target 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.
• 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)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CDK2, c-Met/HGFR, cMet, c-Met, cMet/HGFR, Autophagy, Apoptosis, Met, Met Kinase Inhibitor, HGFR, Flk1, FGFR1, PKI-SU 11274, PKI-SU11274, PKI-SU-11274, RON, SU11274, SU-11274, SU 11274

Compound Identifiers

PubChem CID

9549297