SU11274

Catalog No.S1080 Synonyms: PKI-SU11274

SU11274 Chemical Structure

Molecular Weight(MW): 568.09

SU11274 is a selective Met inhibitor with IC50 of 10 nM in cell-free assays, no effects on PGDFRβ, EGFR or Tie2.

Size Price Stock Quantity  
In DMSO USD 300 In stock
USD 70 In stock
USD 120 In stock
USD 470 In stock
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6 Customer Reviews

  • Inhibition of c-MET sensitizes PTEN deficient tumor cells to EGFR TKI-induced apoptosis. PTEN deficient TGFα-EGFRWT;InkΔ2/3-/-;PTENlox GBM tumor cells were treated with gefitinib (10 uM) and/or the c-MET kinase inhibitor SU11274 (10 uM). Immunoblot analysis of total cell lysates from TGFα-EGFRWT;InkΔ2/3-/-;PTENlox GBM tumor cells treated with the indicated inhibitors using c-MET and c-MET phosphotyrosine 1234,1235 antibodies. Anti β-tubulin probing is used as an internal loading control.

    Oncogene 2012 31(25), 3039-50. SU11274 purchased from Selleck.

    Human umbilical vein endothelial cells (HUVECs) were stained for cortactin (green)/vinculin (red; top) and for zyxin (green)/actin (red; bottom). On RCαβ treatment for 30 to 40 minutes, vinculin disappeared from large focal adhesions underneath the cell body, whereas it appeared in small focal contacts around the cell perimeter. In addition, cortactin was found in the cortical actin network within nascent lamellipodia. Furthermore, zyxin, a marker of focal adhesions, and stress fibers disappeared on RCαβ treatment. Pretreatment of HUVECs with 10 umol/L SU11274 reduced the effect of 200 nmol/L RCαβ, whereas 200 ng/mL hepatocyte growth factor (HGF) elicited similar responses to RCαβ, indicating a signaling path involving cMet. Scale bars, 10 um.

    Arterioscler Thromb Vasc Biol 2013 33(3), 544-54. SU11274 purchased from Selleck.

  • Effect of crizotinib, tivantinib, and SU11274 on levels of c-MET phosphorylation and downstream signaling pathway in SW1736 and TL3 thyroid cancer cells. Cells were prestarved in culture medium containing 0.5% FBS (24 hour) ?either crizotinib or tivantinib (0.1, 1.0, and 10 umol/L) or SU11274 (10 umol/L), and stimulated with 20 ng/mL recombinant human HGF for 10 minutes before lysates were made for Western blotting. A series of c-MET downstream signaling pathway proteins and phosphor proteins were detected using Western blotting. β-Actin was used as a loading balance control.

    Mol Cancer Ther 2014 13(1), 134-43. SU11274 purchased from Selleck.

    HLMVECs grown to -95% confluence on slide chambers were pretreated with 1 uM SU11274 for 1 h prior to stimulation with HGF (20 ng/ml) for 15 min. Cells were washed, fixed, and stained for actin and cortactin co-localization in lamellipodia as described under "Experimental Procedures." Nuclei were stained with DAPI. Shown are representative immunofluorescence images from three independent experiments. Actin and cortactin co-localization in lamellipodia was quantified using image analysis as described under "Experimental Procedures."

    J Biol Chem 2014 289(19), 13476-91. SU11274 purchased from Selleck.

  • Expression of miR-200c and miR-27b after hepatocyte growth factor (HGF) stimulation using qRT-PCR analysis. This downregulation of miR-220c and miR-27b was almost completely inhibited by adding MET kinase-specific inhibitor SU11274 before HGF stimulation.

    Cancer Sci 2011 102, 2164-71. SU11274 purchased from Selleck.

    Western blot analysis of c-Met, MAPK and Akt. 0-20μM SU11724 was added.

     

     

    Dr. Zhang of Tianjin Medical University. SU11274 purchased from Selleck.

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Biological Activity

Description SU11274 is a selective Met inhibitor with IC50 of 10 nM in cell-free assays, no effects on PGDFRβ, EGFR or Tie2.
Targets
Met [1]
(Cell-free assay)
0.01 μM
In vitro

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. [2] 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. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A549 cells Mk\KSpVv[3Srb36gZZN{[Xl? NYLzbI95UW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDjMW1GXCCtaX7hd4UhcW5iQUW0PUBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIFjHSk1qdmS3Y3XkJINmdGxiZ4Lve5RpNCCLQ{WwQVAvODFizszN MWSyNVgyOjRzNB?=
human MDCK cells M{ntV2Z2dmO2aX;uJIF{e2G7 NIm3cIszPCCq NIfHcJhKdmirYnn0bY9vKG:oIF3leE1u\WSrYYTl[EB{[2G2dHXybY5oKGmwIFjHSk1{fGmvdXzheIVlKGi3bXHuJG1FS0tiY3XscJMheHKnLXnuZ5Vj[XSnZDDveoVzdmmpaISgdJJqd3JidH:gTGdHKHO2aX31cIF1cW:wIH\vdkAzPCCqcoOgcYVie3W{ZXSgZYZ1\XJiMkSgeI8hPDhiaILzMEBKSzVyPUCuNVUzKM7:TR?= NEPtbXkzOjF|OEOwPC=>
mouse BAF3 cells NFPyUIhRem:uaX\ldoF1cW:wIHHzd4F6 NF7Ld2w4OiCq M4r5dGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgcY92e2ViQlHGN{Bk\WyuczDlfJBz\XO|aX7nJHRRWi2PZYSgZYZ1\XJiN{KgbJJ{KGmwIHHid4Vv[2Vib3[gTWwuOyxiSVO1NF0xNjV|IN88US=> MWqyNVQxPTF{OB?=
human SNU5 cells NXnoSnhNWHKxbHnm[ZJifGmxbjDhd5NigQ>? NXLSTVJHPzJiaB?= NWLwSHNHSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTUnU2KGOnbHzzJIFnfGW{IEeyJIhzeyxiSVO1NF0xNjhizszN M4SyelIyPDB3MUK4
human MKN45 cells NEDI[5NRem:uaX\ldoF1cW:wIHHzd4F6 MkHPO|IhcA>? NVftZZpnSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNT241PSClZXzsd{Bi\nSncjC3NkBpenNuIFnDOVA:OS5|IN88US=> M4Pie|IyPDB3MUK4
human HepG2 cells NE\ad5VHfW6ldHnvckBie3OjeR?= MXLJcohq[mm2aX;uJI9nKE2ndD3t[YRq[XSnZDD0eY1wemmpZX7ld4l{KGmwIFjHSk1{fGmvdXzheIVlKGi3bXHuJGhmeEd{IHPlcIx{KGG|c3Xzd4VlKGG|IHntdIFqem2nboSgbY4h[W6laH;yZYdmNWmwZHXw[Y5l\W62IHfyc5d1cCCkeTDzc4Z1KGGpYYKg[5Jwf3SqIHHzd4F6NCCLQ{WwQVEvPTZzIN88US=> NVHYOlQ1OjJzM{izNFg>
mouse NIH/3T3 cells M3fSeHBzd2yrZnXyZZRqd25iYYPzZZk> MYC3NkBp NVPQZWY{SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBud3W|ZTDOTWgwO1R|IHPlcIx{KGW6cILld5NqdmdiVGDSMW1mfCCjZoTldkA4OiCqcoOsJGlEPTB;MjFOwG0> MkLQNlE1ODVzMki=
human MCF7 cells MonVVJJwdGmoZYLheIlwdiCjc4PhfS=> MYS3NkBp NHzNUIdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlch[2WubIOgZYZ1\XJiN{KgbJJ{NCCLQ{WwQVYvOiEQvF2= NGPJdVYzOTRyNUGyPC=>
human SNU1 cells NH;LZWpRem:uaX\ldoF1cW:wIHHzd4F6 NGrQSmk4OiCq NHrwdVZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPOWVEh[2WubIOgZYZ1\XJiN{KgbJJ{NCCLQ{WwQVch|ryP NGHTeJgzOTRyNUGyPC=>
human NCI-H1993 cells M{DPNHBzd2yrZnXyZZRqd25iYYPzZZk> MX63NkBp NVi3bGlMSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDF7OUOgZ4VtdHNiYX\0[ZIhPzJiaILzMEBKSzVyPUeuN{DPxE1? NIPKU3QzOTRyNUGyPC=>
human MDA-MB-231 cells Mm\BVJJwdGmoZYLheIlwdiCjc4PhfS=> NITGS2w4OiCq M2m4VGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTJ|MTDj[YxteyCjZoTldkA4OiCqcoO= NX;PeW85OjF2MEWxNlg>
human NCI-H441 cells Mo\nVJJwdGmoZYLheIlwdiCjc4PhfS=> MXG3NkBp MWjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST3IOFQyKGOnbHzzJIFnfGW{IEeyJIhzew>? MnzNNlE1ODVzMki=
human BxPC3 cells NH3neFhRem:uaX\ldoF1cW:wIHHzd4F6 M2XISVczKGh? NX3OXlI1SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDCfHBEOyClZXzsd{Bi\nSncjC3NkBpenN? M4DleFIyPDB3MUK4
DLD1 cells NYrHXmZDTnWwY4Tpc44h[XO|YYm= MVqyMlUh|ryP NH3obHZKdmirYnn0bY9vKG:oIHj1cYFvKHB|OD3hcJBp[SCyaH;zdIhwenmuYYTpc44hcW5iRFzENUBk\WyuczDheEAzNjVizszN MWOxO|U6PTJ7OR?=
DLD1 cells MUfGeY5kfGmxbjDhd5NigQ>? NETCeG4zNjVizszN Mm\ENVYhcA>? NG\zS45KdmirYnn0bY9vKG:oIHj1cYFvKE2HVDDy[YNmeHSxcjDpckBFVERzIHPlcIx{KGG2IEKuOUB2VSCjZoTldkAyPiCqcoOgZpkhX2W|dHXyckBjdG:2 NYTrT5ZlOTd3OUWyPVk>

... Click to View More Cell Line Experimental Data

Protocol

Kinase Assay:[1]
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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:[2]
+ Expand
  • Cell lines: BaF3.TPR-MET, H69 and H345 cells
  • Concentrations: Dissolved in DMSO, final concentrations ~10 μM
  • Incubation Time: 24, 48, and 72 hours
  • Method: 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)

Solubility (25°C)

In vitro DMSO 92 mg/mL (161.94 mM)
Ethanol 2 mg/mL (3.52 mM)
Water Insoluble
In vivo Add solvents individually and in order:
30% PEG400+0.5% Tween80+5% propylene glycol
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 568.09
Formula

C28H30CIN5O4S

CAS No. 658084-23-2
Storage powder
Synonyms PKI-SU11274

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Frequently Asked Questions

  • Question 1:

    What is the solubility of S1080 SU11274 in acetone?

  • Answer:

    The solubility of S1080 SU11274 in acetone is 7 mg/mL.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID