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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Cited by 28 Publications

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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 NFHJSIJHfW6ldHnvckBie3OjeR?= MmjTTY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCClLV3FWEBscW6jc3WgbY4hSTV2OTDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKEiJRj3pcoR2[2WmIHPlcIwh\3Kxd4ToMEBKSzVyPUCuNFEh|ryP NIXUeoYzOThzMkSxOC=>
human MDCK cells MX;GeY5kfGmxbjDhd5NigQ>? NIPmS5kzPCCq M1njZmlvcGmkaYTpc44hd2ZiTXX0MY1m\GmjdHXkJJNk[XS2ZYLpcochcW5iSFfGMZN1cW23bHH0[YQhcHWvYX6gUWREUyClZXzsd{BxemVvaX7jeYJifGWmIH;2[ZJvcWeqdDDwdolweiC2bzDIS2Yhe3SrbYXsZZRqd25iZn;yJFI1KGi{czDt[YF{fXKnZDDh[pRmeiB{NDD0c{A1QCCqcoOsJGlEPTB;MD6xOVIh|ryP MUeyNlE{QDNyOB?=
mouse BAF3 cells NV;Gb3NJWHKxbHnm[ZJifGmxbjDhd5NigQ>? NYHV[5dqPzJiaB?= Mki2RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDtc5V{\SCEQV[zJINmdGy|IHX4dJJme3OrbnegWHBTNU2ndDDh[pRmeiB5MjDodpMhcW5iYXLz[Y5k\SCxZjDJUE0{NCCLQ{WwQVAvPTNizszN MYeyNVQxPTF{OB?=
human SNU5 cells NYjkSHJPWHKxbHnm[ZJifGmxbjDhd5NigQ>? MUS3NkBp NHzsbopCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPOWVUh[2WubIOgZYZ1\XJiN{KgbJJ{NCCLQ{WwQVAvQCEQvF2= MlnPNlE1ODVzMki=
human MKN45 cells MljHVJJwdGmoZYLheIlwdiCjc4PhfS=> NXXCNFRXPzJiaB?= MV3BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2NTkS1JINmdGy|IHHmeIVzKDd{IHjyd{whUUN3ME2xMlMh|ryP M3TNXFIyPDB3MUK4
human HepG2 cells M3;yeGZ2dmO2aX;uJIF{e2G7 NVmwXWZZUW6qaXLpeIlwdiCxZjDN[ZQudWWmaXH0[YQhfHWvb4Lp[4Vv\XOrczDpckBJT0Zvc4TpcZVt[XSnZDDoeY1idiCKZYDHNkBk\WyuczDhd5Nme3OnZDDhd{BqdXCjaYLt[Y51KGmwIHHuZ4hwemGpZT3pcoRmeGWwZHXueEBoem:5dHigZpkhe2:odDDh[4FzKGe{b4f0bEBie3OjeTygTWM2OD1zLkW2NUDPxE1? MUGyNlE{QDNyOB?=
mouse NIH/3T3 cells M1nHTHBzd2yrZnXyZZRqd25iYYPzZZk> MlvhO|IhcA>? NGL0e4lCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIF7JTE8{XDNiY3XscJMh\XiycnXzd4lv\yCWUGKtUYV1KGGodHXyJFczKGi{czygTWM2OD1{IN88US=> MYCyNVQxPTF{OB?=
human MCF7 cells NVXjbFRoWHKxbHnm[ZJifGmxbjDhd5NigQ>? MVu3NkBp NV7FPYdpSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIFnfGW{IEeyJIhzeyxiSVO1NF03NjJizszN MoHzNlE1ODVzMki=
human SNU1 cells M{\HNnBzd2yrZnXyZZRqd25iYYPzZZk> MlryO|IhcA>? MkG1RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVTmWxJINmdGy|IHHmeIVzKDd{IHjyd{whUUN3ME23JO69VQ>? NYXhVYQ1OjF2MEWxNlg>
human NCI-H1993 cells NI\0RnNRem:uaX\ldoF1cW:wIHHzd4F6 NY\QRXFpPzJiaB?= NYTSeo5vSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDF7OUOgZ4VtdHNiYX\0[ZIhPzJiaILzMEBKSzVyPUeuN{DPxE1? NVu3Z|VxOjF2MEWxNlg>
human MDA-MB-231 cells MnnJVJJwdGmoZYLheIlwdiCjc4PhfS=> MmPiO|IhcA>? M2nXRWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTJ|MTDj[YxteyCjZoTldkA4OiCqcoO= NHX1SmgzOTRyNUGyPC=>
human NCI-H441 cells M3vFWXBzd2yrZnXyZZRqd25iYYPzZZk> Ml3GO|IhcA>? Mn62RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mtTFQ1OSClZXzsd{Bi\nSncjC3NkBpenN? NUTSOYx[OjF2MEWxNlg>
human BxPC3 cells MnPDVJJwdGmoZYLheIlwdiCjc4PhfS=> MYK3NkBp NEXiN3ZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFL4VGM{KGOnbHzzJIFnfGW{IEeyJIhzew>? NEjQeHAzOTRyNUGyPC=>
DLD1 cells NHvZU41HfW6ldHnvckBie3OjeR?= NUfYOpZxOi53IN88US=> Mne3TY5pcWKrdHnvckBw\iCqdX3hckBxOzhvYXzwbIEheGixc4Doc5J6dGG2aX;uJIlvKESOREGgZ4VtdHNiYYSgNk42KM7:TR?= MXKxO|U6PTJ7OR?=
DLD1 cells MmjjSpVv[3Srb36gZZN{[Xl? NFHt[GwzNjVizszN NYnoZlBWOTZiaB?= M4nTTmlvcGmkaYTpc44hd2ZiaIXtZY4hVUWWIILlZ4VxfG:{IHnuJGRNTDFiY3XscJMh[XRiMj61JJVOKGGodHXyJFE3KGi{czDifUBY\XO2ZYLuJIJtd3R? M2TRW|E4PTl3Mkm5

... Click to View More Cell Line Experimental Data

Protocol

Kinase Assay:[1]
+ Expand

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 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

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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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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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