SU11274

Catalog No.S1080 Synonyms: PKI-SU11274

For research use only.

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.

SU11274 Chemical Structure

CAS No. 658084-23-2

Selleck's SU11274 has been cited by 55 publications

Purity & Quality Control

Choose Selective c-Met Inhibitors

Other c-Met Products

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 NV75cIN7TnWwY4Tpc44h[XO|YYm= M2K1RWlvcGmkaYTpc44hd2ZiaIXtZY4hemWlb33ibY5idnRiYz3NSXQhc2mwYYPlJIlvKEF3NEmgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCKR1[tbY5lfWOnZDDj[YxtKGe{b4f0bEwhUUN3ME2wMlAyKM7:TR?= NXi3PGJCOjF6MUK0NVQ>
human MDCK cells MXrGeY5kfGmxbjDhd5NigQ>? MmjlNlQhcA>? NHizSldKdmirYnn0bY9vKG:oIF3leE1u\WSrYYTl[EB{[2G2dHXybY5oKGmwIFjHSk1{fGmvdXzheIVlKGi3bXHuJG1FS0tiY3XscJMheHKnLXnuZ5Vj[XSnZDDveoVzdmmpaISgdJJqd3JidH:gTGdHKHO2aX31cIF1cW:wIH\vdkAzPCCqcoOgcYVie3W{ZXSgZYZ1\XJiMkSgeI8hPDhiaILzMEBKSzVyPUCuNVUzKM7:TR?= M4DYSVIzOTN6M{C4
mouse BAF3 cells NFTOSWJRem:uaX\ldoF1cW:wIHHzd4F6 MXu3NkBp MoDGRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDtc5V{\SCEQV[zJINmdGy|IHX4dJJme3OrbnegWHBTNU2ndDDh[pRmeiB5MjDodpMhcW5iYXLz[Y5k\SCxZjDJUE0{NCCLQ{WwQVAvPTNizszN M2\ibVIyPDB3MUK4
human SNU5 cells M3zhenBzd2yrZnXyZZRqd25iYYPzZZk> MUS3NkBp NInmSpdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPOWVUh[2WubIOgZYZ1\XJiN{KgbJJ{NCCLQ{WwQVAvQCEQvF2= MkPONlE1ODVzMki=
human MKN45 cells NGDkWVZRem:uaX\ldoF1cW:wIHHzd4F6 NEDWTXg4OiCq MnvtRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPS160OUBk\WyuczDh[pRmeiB5MjDodpMtKEmFNUC9NU4{KM7:TR?= NGTwPHczOTRyNUGyPC=>
human HepG2 cells NGO3dlJHfW6ldHnvckBie3OjeR?= NIHCWJRKdmirYnn0bY9vKG:oIF3leE1u\WSrYYTl[EB1fW2xcnnn[Y5me2m|IHnuJGhITi2|dHnteYxifGWmIHj1cYFvKEincFeyJINmdGy|IHHzd4V{e2WmIHHzJIlueGGrcn3lcpQhcW5iYX7jbI9z[WenLXnu[IVx\W6mZX70JIdzd3e2aDDifUB{d2[2IHHnZZIh\3Kxd4ToJIF{e2G7LDDJR|UxRTFwNU[xJO69VQ>? MlvwNlIyOzh|MEi=
mouse NIH/3T3 cells NXvEd5hCWHKxbHnm[ZJifGmxbjDhd5NigQ>? NILNSZI4OiCq NWHVPI1MSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBud3W|ZTDOTWgwO1R|IHPlcIx{KGW6cILld5NqdmdiVGDSMW1mfCCjZoTldkA4OiCqcoOsJGlEPTB;MjFOwG0> NVvnbpV{OjF2MEWxNlg>
human MCF7 cells M1XTeHBzd2yrZnXyZZRqd25iYYPzZZk> MXG3NkBp MYfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkegZ4VtdHNiYX\0[ZIhPzJiaILzMEBKSzVyPU[uNkDPxE1? NFW5RnMzOTRyNUGyPC=>
human SNU1 cells NX3ONmZuWHKxbHnm[ZJifGmxbjDhd5NigQ>? M4joUFczKGh? MnfiRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVTmWxJINmdGy|IHHmeIVzKDd{IHjyd{whUUN3ME23JO69VQ>? NHPzSHgzOTRyNUGyPC=>
human NCI-H1993 cells NV7yNZJEWHKxbHnm[ZJifGmxbjDhd5NigQ>? NWDJcIxFPzJiaB?= NYDBbmUzSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDF7OUOgZ4VtdHNiYX\0[ZIhPzJiaILzMEBKSzVyPUeuN{DPxE1? MlruNlE1ODVzMki=
human MDA-MB-231 cells NVjNbYRVWHKxbHnm[ZJifGmxbjDhd5NigQ>? MXi3NkBp NX\MR4RXSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHHmeIVzKDd{IHjydy=> NGT4UIMzOTRyNUGyPC=>
human NCI-H441 cells NVXRZ4JjWHKxbHnm[ZJifGmxbjDhd5NigQ>? M2nCT|czKGh? M3;ISWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWg1PDFiY3XscJMh[W[2ZYKgO|IhcHK| M1nrdFIyPDB3MUK4
human BxPC3 cells NW[wdFIzWHKxbHnm[ZJifGmxbjDhd5NigQ>? MXi3NkBp M3zyPWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQojQR|Mh[2WubIOgZYZ1\XJiN{KgbJJ{ MWeyNVQxPTF{OB?=
DLD1 cells NWXFR3V6TnWwY4Tpc44h[XO|YYm= MXqyMlUh|ryP NFjIWlZKdmirYnn0bY9vKG:oIHj1cYFvKHB|OD3hcJBp[SCyaH;zdIhwenmuYYTpc44hcW5iRFzENUBk\WyuczDheEAzNjVizszN MneyNVc2QTV{OUm=
DLD1 cells MoLWSpVv[3Srb36gZZN{[Xl? M175PVIvPSEQvF2= NFL2WIgyPiCq MWrJcohq[mm2aX;uJI9nKGi3bXHuJG1GXCC{ZXPldJRweiCrbjDEUGQyKGOnbHzzJIF1KDJwNTD1UUBi\nSncjCxOkBpenNiYomgW4V{fGW{bjDicI91 NGj0e|QyPzV7NUK5PS=>
Assay
Methods Test Index PMID
Growth inhibition assay Cell viability 23341789
Western blot p-Met / Met / p-AKT / AKT / p-ERK / ERK ; PUMA / Bcl-2 / Bax 23341789
Immunofluorescence p-SphK1 27864331

Protocol (from reference)

Kinase Assay:[1]
  • 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]
  • 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.

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

Chemical Information

Molecular Weight 568.09
Formula

C28H30CIN5O4S

CAS No. 658084-23-2
Storage 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.

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.

Tags: buy SU11274 | SU11274 supplier | purchase SU11274 | SU11274 cost | SU11274 manufacturer | order SU11274 | SU11274 distributor