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.

Size Price Stock Quantity  
USD 270 In stock
USD 370 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Cited by 13 Publications

5 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.

    The expression of p‐AKT after TGFβ1 or LY2109761 treatment on vector‐ and ADAMTS9‐transfected BT549 and SK‐BR‐3 cells.

    J Cell Mol Med, 2018, 22(2):1257-1271. 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.

    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.

  • 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  NF;UdWxHfW6ldHnvckBCe3OjeR?= NWnucZVxOTEEoN88UeKh NV\sT3B7OiCq NITmTnNqdmirYnn0d{BifXSxcHjh[5khcW6mdXP0bY9vKGK7IHfhcIFv\2mw NIj3NGEzPTJ4OEC0Oi=>
PC-3 MWXGeY5kfGmxbjDBd5NigQ>? Ml[0NE4zNzJxNDFOwG0> MnuxNlQhcA>? NUDCU3R6TE2VTx?= MXHpcohq[mm2czDUS2Yu|rJz4pETbY5lfWOnZDDTcYFlOiCjY4TpeoF1cW:w MkO2NlIyPzNyNUO=
PMOs NF7yZ21HfW6ldHnvckBCe3OjeR?= MkTxNE4zNzJxNDFOwG0> M4n3PFI1KGh? NHfBRZFFVVOR NIfuVI9qdmirYnn0d{BVT0ZvzsKx5qCUcW6mdXPl[EBUdWGmMjDhZ5RqfmG2aX;u MWmyNlE4OzB3Mx?=
PC-3 NHXjUlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTGTVNZOC5{L{Kg{txO NYfyRXM6OjRiaB?= NUi0PHJCTE2VTx?= NHnkU4tjdG:la4OgeIhmKGmwaHnibZRqd25ib3[gZ4VtdCCycn;sbYZmemG2aX;uJJBzd2S3Y3XkJIJ6KFSJRj5OtlE> M1nIZVIzOTd|MEWz
PMOs MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PtUFAvOi9{IN88US=> MVuyOEBp M1zoNGROW09? MljCZoxw[2u|IITo[UBqdmirYnn0bY9vKG:oIHPlcIwheHKxbHnm[ZJifGmxbjDwdo9lfWOnZDDifUBVT0ZvzsKx NXrKSnlmOjJzN{OwOVM>
U87MG NUTCTVkzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV:1M|ExKM7:TR?= NIrLdmwzKGh? NYfHdFlJ\W6qYX7j[ZMhemGmaX;z[Y5{cXSrdnn0fS=> MoLwNlIxODZ7OUi=
T98 NFzKPVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHlOU8yOCEQvF2= MnnMNkBp MmLv[Y5p[W6lZYOgdoFlcW:|ZX7zbZRqfmm2eR?= MYOyNlAxPjl7OB?=
U87MG NWjEXFQxSXCxcITvd4l{KEG|c3H5 MlLXNVAh|ryP MWCyJIg> MYLlcohidmOnczDyZYRq[XSrb36tbY5lfWOnZDDEUmEh\GGvYXflJIFv\CCjcH;weI9{cXNicnH0[ZM> MnrENlIxODZ7OUi=
NMA-23 MWnBdI9xfG:|aYOgRZN{[Xl? MmjSNVAh|ryP M3m4UlIhcA>? Mkji[Y5p[W6lZYOgdoFlcWG2aX;uMYlv\HWlZXSgSG5CKGSjbXHn[UBidmRiYYDvdJRwe2m|IILheIV{ MnHkNlIxODZ7OUi=
HLE  M174UWZ2dmO2aX;uJGF{e2G7 NUDnbIY3OC5yMT2xNFDDqG6P Ml;VOFghcA>? NUfsb5JYcW6qaXLpeJMhfGinIH3p[5JifGmxbjDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NYC3UHYyOjB6NES4O|g>
HLF MWDGeY5kfGmxbjDBd5NigQ>? NEji[o4xNjBzLUGwNOKhdk1? NH\aXYE1QCCq NVrzdWR[cW6qaXLpeJMhfGinIH3p[5JifGmxbjDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= MlOyNlA5PDR6N{i=
10A/HER2YVMA MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUSwMlEuOC53IN88US=> MlzGPUBl MXXy[YR2[2W|IITo[UB{cXqnLDDpcpZie2m4ZX7ld5Mh[W6mIHPlcIwhdnWvYnXyJI9nKGOxbH;ubYV{ NUf5eI5JOjB|OEOxPVc>
MC38  NXLsSlRLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnnDOUDPxE1? M13IcVUh\A>? NFrmR5hqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJJRqdWVvZHXw[Y5l\W62IH3hco5meg>? M{W0bVE6QTB7N{S0
U937 NYOzUZVFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTuOU0zOCEQvF2= Mn\0NlQuPzJiaB?= MUjpcohq[mm2czDj[YxtKGe{b4f0bEB{dGmpaITsfS=> NFLVTngyQDR7MkGxNy=>
HLE  NE[zVmREgXSxdH;4bZR6KEG|c3H5 NX;MNFF3OC5yMEGtNlAh|ryP MWW0PEBp MX\pcoR2[2W|IHPlcIwh[3m2b4TvfIl1gSCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NGnFXY8yQDNzOES0Ny=>
HLF MX\DfZRwfG:6aYT5JGF{e2G7 MnzpNE4xODFvMkCg{txO MofoOFghcA>? NYPxZpo4cW6mdXPld{Bk\WyuIHP5eI91d3irdImgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= NFXMSYEyQDNzOES0Ny=>

... 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 to the product individually and in order(Data is from Selleck tests instead of citations):
0.5% CMC+0.25% Tween 80
For best results, use promptly after mixing.
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

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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

TGF-beta/Smad Signaling Pathway Map

TGF-beta/Smad Inhibitors with Unique Features

Related TGF-beta/Smad Products4

Tags: buy LY2109761 | LY2109761 supplier | purchase LY2109761 | LY2109761 cost | LY2109761 manufacturer | order LY2109761 | LY2109761 distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID