LY2109761

Catalog No.S2704

LY2109761 Chemical Structure

Molecular Weight(MW): 441.52

LY2109761 is a novel selective TGF-β receptor type I/II (TβRI/II) dual inhibitor with Ki of 38 nM and 300 nM in a cell-free assay, respectively; shown to negatively affect the phosphorylation of Smad2.

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4 Customer Reviews

  • C, Western blot analysis of serum cultured GB2 cells treated with each 20 μm inhibitor. The representative Western blot is shown for each protein and the bar charts represent the quantified values (mean ± s.d.) of three replicates. The fold changes were normalized by the relative densities regarding α-Tubulin.

    Mol Cell Proteomics, 2016, 15(3):1017-31. LY2109761 purchased from Selleck.

    validation of activity and specificity of chemical inhibitors of; ATM, ATR, and DNAPK. H460 cells were treated with 1 uM camptothecin (CPT) or 20 ug/ml bleomycin for 1 h in the presence of the indicated inhibitors: DNAPK-i1—NU7026, DNAPK-i2—NU7441. MSH6,

    Toxicology 2014 326C, 9-17. LY2109761 purchased from Selleck.

  • The inhibition of TGF-β1 signaling pathways suppressed EBV-mediated EMT, and prevented the activation of Syk and Src signaling. The EBV-infected HCECs were treated with 100 nM of the dual TGF-β receptor I and II kinase inhibitor, LY2109761, for 48 hours. The EBV-infected HCECs were cultured with anti-TGF-β1 neutralizing antibody (5 ug/mL) or mouse IgG1 antibody (5 ug/mL) for 48 hours. Photographs were taken at x100 magnification by a digital camera.

    Invest Ophthalmol Vis Sci 2014 55(3), 1770-9. LY2109761 purchased from Selleck.

    PLoS One 2013 8(12), e83521. LY2109761 purchased from Selleck.

Purity & Quality Control

Choose Selective TGF-beta/Smad Inhibitors

Biological Activity

Description LY2109761 is a novel selective TGF-β receptor type I/II (TβRI/II) dual inhibitor with Ki of 38 nM and 300 nM in a cell-free assay, respectively; shown to negatively affect the phosphorylation of Smad2.
Targets
TβRI [1]
(Cell-free assay)
TβRII [1]
(Cell-free assay)
38 nM(Ki) 300 nM(Ki)
In vitro

LY2109761 treatment induces a dose-dependent low-anchorage growth inhibition of L3.6pl/GLT cells, leading to ~33% or 73% inhibition at 2 μM and 20 μM, respectively, which can be strongly enhanced when combined with gemcitabine in combination index value of 0.36581. Blocking TβRI/II kinase activity with LY2109761 (5 μM) completely suppresses both the basal and TGF-β1-stimulated migration and invasion of L3.6pl/GLT cells, significantly enhances the detachment-induced apoptosis by 26% at 8 hours treatment, and completely suppresses TGF-β–induced Smad2 phosphorylation. [1] LY2109761 treatment at 1 nM is sufficient to significantly block the migration and invasion but not adhesion of hepatocellular carcinoma cells by increasing E-cadherin expression. [2] LY2109761 pretreatment enhances radiosensitivity of glioblastoma cells via TGF-β signaling blockage. LY2109761 (10 μM) reduces the self-renewal and proliferation of GBM-derived cancer stem–like cells (CSLC), which can be significantly enhanced when combined with radiation. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HepG2  MoDVSpVv[3Srb36gRZN{[Xl? NGPkb|UyOMLizszNxsA> MVOyJIg> MWnpcohq[mm2czDheZRweGijZ4mgbY5lfWO2aX;uJIJ6KGejbHHu[4lv NYWzTlVGOjV{NkiwOFY>
PC-3 MVXGeY5kfGmxbjDBd5NigQ>? MorlNE4zNzJxNDFOwG0> MYiyOEBp NX;mOmVJTE2VTx?= M{jpZYlvcGmkaYTzJHRITi4QskJihLNqdmS3Y3XkJHNu[WR{IHHjeIl3[XSrb36= MkP3NlIyPzNyNUO=
PMOs NV\K[GFrTnWwY4Tpc44hSXO|YYm= NU\GSGlTOC5{L{KvOEDPxE1? NE\JVmozPCCq NWXHUXRyTE2VTx?= NWP2RpR4cW6qaXLpeJMhXEeILd8yNgKBm2mwZIXj[YQhW22jZEKgZYN1cX[jdHnvci=> NG\ISVgzOjF5M{C1Ny=>
PC-3 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlj6NE4zNzJizszN M1TYOlI1KGh? NH7DTpNFVVOR M2XOfIJtd2OtczD0bIUhcW6qaXLpeIlwdiCxZjDj[YxtKHC{b3zp[oVz[XSrb36gdJJw\HWlZXSgZpkhXEeILd8yNS=> NFn4RVAzOjF5M{C1Ny=>
PMOs MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3oNE4zNzJizszN MlTVNlQhcA>? M3zrO2ROW09? M1u2coJtd2OtczD0bIUhcW6qaXLpeIlwdiCxZjDj[YxtKHC{b3zp[oVz[XSrb36gdJJw\HWlZXSgZpkhXEeILd8yNS=> M162fVIzOTd|MEWz
U87MG Mn;MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjK[po2NzFyIN88US=> MW[yJIg> MVvlcohidmOnczDyZYRqd3OnboPpeIl3cXS7 MWKyNlAxPjl7OB?=
T98 MoTDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1KxclUwOTBizszN NY[xemp6OiCq M2nicIVvcGGwY3XzJJJi\Gmxc3Xud4l1cX[rdIm= NVjp[FRFOjJyME[5PVg>
U87MG M2\mV2Fxd3C2b4Ppd{BCe3OjeR?= NH36PVMyOCEQvF2= NVvidWhWOiCq NETQUFBmdmijbnPld{Bz[WSrYYTpc44ucW6mdXPl[EBFVkFiZHHtZYdmKGGwZDDhdI9xfG:|aYOgdoF1\XN? Ml;jNlIxODZ7OUi=
NMA-23 MU\BdI9xfG:|aYOgRZN{[Xl? MX[xNEDPxE1? NIHUZZYzKGh? NWPDRnhK\W6qYX7j[ZMhemGmaXH0bY9vNWmwZIXj[YQhTE6DIHThcYFo\SCjbnSgZZBweHSxc3nzJJJifGW| MmC4NlIxODZ7OUi=
HLE  NIK5R4hHfW6ldHnvckBCe3OjeR?= MnLoNE4xOS1zMEFCpI5O M4rQXlQ5KGh? MVfpcohq[mm2czD0bIUhdWmpcnH0bY9vKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M1q3XFIxQDR2OEe4
HLF MVPGeY5kfGmxbjDBd5NigQ>? MWOwMlAyNTFyMNMgcm0> NG\OSnA1QCCq MVLpcohq[mm2czD0bIUhdWmpcnH0bY9vKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M4L1c|IxQDR2OEe4
10A/HER2YVMA Ml:xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\0[4QxNjFvMD61JO69VQ>? NWXJeZF3QSCm NXX2[HJWemWmdXPld{B1cGVic3n6[UwhcW64YYPpeoVv\XO|IHHu[EBk\WyuIH71cYJmeiCxZjDjc4xwdmmncx?= MnPjNlA{QDNzOUe=
MC38  NXPnRlQyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzLNZo2KM7:TR?= M3iz[lUh\A>? M3zq[4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGgeIlu\S2mZYDlcoRmdnRibXHucoVz M2\jS|E6QTB7N{S0
U937 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFjTcpU2NTJyIN88US=> NHnj[|QzPC15MjDo M3;rdolvcGmkaYTzJINmdGxiZ4Lve5RpKHOuaXfoeIx6 Mlu0NVg1QTJzMUO=
HLE  NHHWcZJEgXSxdH;4bZR6KEG|c3H5 NHTVbocxNjByMT2yNEDPxE1? NGXKSWg1QCCq MXrpcoR2[2W|IHPlcIwh[3m2b4TvfIl1gSCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NH[1[GYyQDNzOES0Ny=>
HLF NGrme5JEgXSxdH;4bZR6KEG|c3H5 NIjiPW4xNjByMT2yNEDPxE1? NULadlBjPDhiaB?= Ml;rbY5lfWOnczDj[YxtKGO7dH;0c5hqfHliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NXvCfHhbOTh|MUi0OFM>

... Click to View More Cell Line Experimental Data

In vivo Administration of LY2109761 (50 mg/kg) alone or in combination with gemcitabine (25 mg/kg) significantly reduces the tumor volume by ~70% and ~90%, respectively, prolongs the survival with the median survival duration of 45.0 days and 77.5 days, respectively, and reduces spontaneous abdominal metastases in the L3.6pl/GLT Xenograft mice model. [1] In consistent with the in vitro effect, administration of LY2109761 alone or in combination with radiation, markedly inhibits tumor growth in the orthotopical CSLC glioblastoma model by 43.4% and 76.3%, respectively, decreases tumor invasion and tumor microvessel density, and significantly enhances radiation-induced tumor growth delay in the U87MG xenograft mice model. [3]

Protocol

Cell Research:[1]
+ Expand
  • Cell lines: Colo357FG/GLT, and Colo357L3.6pl/GLT
  • Concentrations: Dissolved in DMSO, final concentrations ~10 μM
  • Incubation Time: 48 hours
  • Method: Cells are exposed to increasing doses of LY2109761 (~10 μM) for 48 hours. The medium containing drugs is removed, the cells are washed twice with PBS, and fresh medium is added. After 5 days of incubation, the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay is used to obtain relative variable cell numbers.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: Athymic nude mice with orthotopic implantation of L3.6pl/GLT cells
  • Formulation: Dissolved in the SX-1292 oral vehicle containing 1% sodium carboxymethylcellulose, 0.5% sodium lauryl sulfate, and 0.05% antifoam
  • Dosages: 50 mg/kg
  • Administration: Twice a day p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 2 mg/mL (4.52 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
0.5% CMC+0.25% Tween 80
16 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 441.52
Formula

C26H27N5O2

CAS No. 700874-71-1
Storage powder
in solvent
Synonyms N/A

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID