SU11274

For research use only.

Catalog No.S1080 Synonyms: PKI-SU11274

52 publications

SU11274 Chemical Structure

CAS No. 658084-23-2

SU11274 (PKI-SU11274) is a selective Met (c-Met) inhibitor with IC50 of 10 nM in cell-free assays, no effects on PGDFRβ, EGFR or Tie2. SU11274 induces autophagy, apoptosis and cell cycle arrest.

Selleck's SU11274 has been cited by 52 publications

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Biological Activity

Description SU11274 (PKI-SU11274) is a selective Met (c-Met) inhibitor with IC50 of 10 nM in cell-free assays, no effects on PGDFRβ, EGFR or Tie2. SU11274 induces autophagy, apoptosis and cell cycle arrest.
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 NET6T3hHfW6ldHnvckBie3OjeR?= MljoTY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCClLV3FWEBscW6jc3WgbY4hSTV2OTDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKEiJRj3pcoR2[2WmIHPlcIwh\3Kxd4ToMEBKSzVyPUCuNFEh|ryP NGTycZYzOThzMkSxOC=>
human MDCK cells MkKzSpVv[3Srb36gZZN{[Xl? MorlNlQhcA>? MkTSTY5pcWKrdHnvckBw\iCPZYStcYVlcWG2ZXSgd4NifHSncnnu[{BqdiCKR1[td5RqdXWuYYTl[EBpfW2jbjDNSGNMKGOnbHzzJJBz\S2rbnP1ZoF1\WRib4\ldo5q\2i2IIDybY9zKHSxIFjHSkB{fGmvdXzheIlwdiCob4KgNlQhcHK|IH3lZZN2emWmIHHmeIVzKDJ2IITvJFQ5KGi{czygTWM2OD1yLkG1NkDPxE1? NVXYTopWOjJzM{izNFg>
mouse BAF3 cells M1T5UnBzd2yrZnXyZZRqd25iYYPzZZk> NW\4ZnhFPzJiaB?= M4PLPGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgcY92e2ViQlHGN{Bk\WyuczDlfJBz\XO|aX7nJHRRWi2PZYSgZYZ1\XJiN{KgbJJ{KGmwIHHid4Vv[2Vib3[gTWwuOyxiSVO1NF0xNjV|IN88US=> NYnpfGJkOjF2MEWxNlg>
human SNU5 cells MVPQdo9tcW[ncnH0bY9vKGG|c3H5 MlT5O|IhcA>? M2\NSmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU17VOUBk\WyuczDh[pRmeiB5MjDodpMtKEmFNUC9NE45KM7:TR?= MUmyNVQxPTF{OB?=
human MKN45 cells MnzjVJJwdGmoZYLheIlwdiCjc4PhfS=> MVK3NkBp MUTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2NTkS1JINmdGy|IHHmeIVzKDd{IHjyd{whUUN3ME2xMlMh|ryP NF;6fXczOTRyNUGyPC=>
human HepG2 cells MmHDSpVv[3Srb36gZZN{[Xl? M2LTSGlvcGmkaYTpc44hd2ZiTXX0MY1m\GmjdHXkJJR2dW:{aXflcoV{cXNiaX6gTGdHNXO2aX31cIF1\WRiaIXtZY4hUGWyR{KgZ4VtdHNiYYPz[ZN{\WRiYYOgbY1x[Wm{bXXueEBqdiCjbnPoc5Ji\2VvaX7k[ZBmdmSnboSg[5Jwf3SqIHL5JJNw\nRiYXfhdkBoem:5dHigZZN{[XluIFnDOVA:OS53NkGg{txO NGTrXokzOjF|OEOwPC=>
mouse NIH/3T3 cells MoG3VJJwdGmoZYLheIlwdiCjc4PhfS=> MXG3NkBp M4TFcmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgcY92e2ViTlnIM|NVOyClZXzsd{BmgHC{ZYPzbY5oKFSSUj3N[ZQh[W[2ZYKgO|IhcHK|LDDJR|UxRTJizszN MkK5NlE1ODVzMki=
human MCF7 cells M1;vOHBzd2yrZnXyZZRqd25iYYPzZZk> M{iwcFczKGh? MUDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkegZ4VtdHNiYX\0[ZIhPzJiaILzMEBKSzVyPU[uNkDPxE1? MnnoNlE1ODVzMki=
human SNU1 cells M{Xz[3Bzd2yrZnXyZZRqd25iYYPzZZk> M4PkbVczKGh? NEXtXGlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPOWVEh[2WubIOgZYZ1\XJiN{KgbJJ{NCCLQ{WwQVch|ryP NVnLWJJrOjF2MEWxNlg>
human NCI-H1993 cells MkfMVJJwdGmoZYLheIlwdiCjc4PhfS=> NFnmPXg4OiCq M13DPGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWgyQTl|IHPlcIx{KGGodHXyJFczKGi{czygTWM2OD15LkOg{txO MVuyNVQxPTF{OB?=
human MDA-MB-231 cells MXLQdo9tcW[ncnH0bY9vKGG|c3H5 M3fJbVczKGh? M1PSUWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTJ|MTDj[YxteyCjZoTldkA4OiCqcoO= MmfNNlE1ODVzMki=
human NCI-H441 cells M4HkfXBzd2yrZnXyZZRqd25iYYPzZZk> MUC3NkBp NE\GUm1CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7DTU1JPDRzIHPlcIx{KGGodHXyJFczKGi{cx?= NGTlWWYzOTRyNUGyPC=>
human BxPC3 cells MXnQdo9tcW[ncnH0bY9vKGG|c3H5 MV63NkBp NGHJbJRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFL4VGM{KGOnbHzzJIFnfGW{IEeyJIhzew>? MnH6NlE1ODVzMki=
DLD1 cells NUDObHVyTnWwY4Tpc44h[XO|YYm= MYSyMlUh|ryP NXXUXIRpUW6qaXLpeIlwdiCxZjDoeY1idiCyM{itZYxxcGFicHjvd5Bpd3K7bHH0bY9vKGmwIFTMSFEh[2WubIOgZZQhOi53IN88US=> MlHwNVc2QTV{OUm=
DLD1 cells NGnteHlHfW6ldHnvckBie3OjeR?= M1rxfFIvPSEQvF2= MnvGNVYhcA>? MmP2TY5pcWKrdHnvckBw\iCqdX3hckBOTVRicnXj[ZB1d3JiaX6gSGxFOSClZXzsd{BifCB{LkWgeW0h[W[2ZYKgNVYhcHK|IHL5JHdme3Sncn6gZoxwfA>? M1fKTlE4PTl3Mkm5

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Growth inhibition assay
Cell viability ; 

PubMed: 23341789     


Results of cell counting in A549 and Calu-1 cells treated with 1 and 10 µM SU11274 for 48 hr and 96 hr. Points, mean value of three experiments; bar, standard error, this data presented p < 0.05; CT, control. 

23341789
Western blot
p-Met / Met / p-AKT / AKT / p-ERK / ERK ; 

PubMed: 23341789     


A549 and Calu-1 cells were treated with 10 µM SU11274 for indicated time. Whole cell lysates were prepared and separated by 8% sodium dodecyl sulfate-polyacrylamide gel electrophoresis, and immunoblotted for MET, Akt, Erk and their phosphorylated forms. β-actin was used as a loading control.

PUMA / Bcl-2 / Bax ; 

PubMed: 23341789     


Expression of Bax, PUMA, and Bcl-2 in SU11274-treated A549 cells. Cells were treated with 10 µM SU11274 for the indicated times.

23341789
Immunofluorescence
p-SphK1; 

PubMed: 27864331     


HLMVECs grown on slide chambers to ∼95% confluence were pretreated with SU11274 (1 μM, 30 min) prior to stimulation with HGF (20 ng/ml) for 30 min and probed with anti-actin and anti-p-SphK1 (ser225) antibodies, and lamellipodia were examined by immunofluorescence microscopy with 60× oil objective. Co-localization of actin (red) and p-SphK1 (green) in lamellipodia (merge, yellow) was visualized by immunofluorescent staining. Shown are representative images from three independent experiments. Insets depict enhanced actin and p-SphK1 accumulation in lamellipodia that was blocked by SU11274 treatment of cells. 

27864331

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]
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  • 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)
Water Insoluble
Ethanol '2 mg/mL
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing.
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
in solvent
Synonyms PKI-SU11274
Smiles CC1=C(NC(=C1C(=O)N2CCN(CC2)C)C)C=C3C4=C(C=CC(=C4)S(=O)(=O)N(C)C5=CC(=CC=C5)Cl)NC3=O

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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