LY2109761

For research use only. Not for use in humans.

Catalog No.S2704

46 publications

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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Selleck's LY2109761 has been cited by 46 publications

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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  NIL5XnlHfW6ldHnvckBCe3OjeR?= M1r3SVExyqEQvF5CpC=> NXHqelZqOiCq NFjvSHhqdmirYnn0d{BifXSxcHjh[5khcW6mdXP0bY9vKGK7IHfhcIFv\2mw MUOyOVI3QDB2Nh?=
PC-3 M4XyNWZ2dmO2aX;uJGF{e2G7 M33ZWFAvOi9{L{Sg{txO M1vXVFI1KGh? MUnEUXNQ MnHmbY5pcWKrdIOgWGdHNc7{MfMAl4lv\HWlZXSgV41i\DJiYXP0bZZifGmxbh?= Ml7wNlIyPzNyNUO=
PMOs MVfGeY5kfGmxbjDBd5NigQ>? M4PCXFAvOi9{L{Sg{txO MYeyOEBp NIjy[nlFVVOR MnSzbY5pcWKrdIOgWGdHNc7{MfMAl4lv\HWlZXSgV41i\DJiYXP0bZZifGmxbh?= NFvXZXUzOjF5M{C1Ny=>
PC-3 NUPsN5hRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUmwMlIwOiEQvF2= M17oXFI1KGh? M1TRW2ROW09? MU\icI9kc3NidHjlJIlvcGmkaYTpc44hd2ZiY3XscEBxem:uaX\ldoF1cW:wIIDyc4R2[2WmIHL5JHRITi4QskG= NW\oU5VyOjJzN{OwOVM>
PMOs M3;ORmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jiSFAvOi9{IN88US=> M4TaN|I1KGh? MkjiSG1UVw>? NH[2W3JjdG:la4OgeIhmKGmwaHnibZRqd25ib3[gZ4VtdCCycn;sbYZmemG2aX;uJJBzd2S3Y3XkJIJ6KFSJRj5OtlE> NXvKepEzOjJzN{OwOVM>
U87MG NXjKUpY1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYO5eJhGPS9zMDFOwG0> NEH0dmEzKGh? MUHlcohidmOnczDyZYRqd3OnboPpeIl3cXS7 M13QU|IzODB4OUm4
T98 NULxN|hUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\WZ|k2NzFyIN88US=> M1Ttb|IhcA>? Ml7S[Y5p[W6lZYOgdoFlcW:|ZX7zbZRqfmm2eR?= MV:yNlAxPjl7OB?=
U87MG M36ycmFxd3C2b4Ppd{BCe3OjeR?= NIfUTIcyOCEQvF2= MX6yJIg> NIWzbGlmdmijbnPld{Bz[WSrYYTpc44ucW6mdXPl[EBFVkFiZHHtZYdmKGGwZDDhdI9xfG:|aYOgdoF1\XN? MX:yNlAxPjl7OB?=
NMA-23 NIHJdoNCeG:ydH;zbZMhSXO|YYm= MUKxNEDPxE1? MVmyJIg> MWTlcohidmOnczDyZYRq[XSrb36tbY5lfWOnZDDEUmEh\GGvYXflJIFv\CCjcH;weI9{cXNicnH0[ZM> MXuyNlAxPjl7OB?=
HLE  MVPGeY5kfGmxbjDBd5NigQ>? MoLjNE4xOS1zMEFCpI5O Mki1OFghcA>? MYTpcohq[mm2czD0bIUhdWmpcnH0bY9vKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MVSyNFg1PDh5OB?=
HLF MkLXSpVv[3Srb36gRZN{[Xl? NX3OcpF2OC5yMT2xNFDDqG6P NEXXNo81QCCq NF3ZSVZqdmirYnn0d{B1cGVibXnndoF1cW:wIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NXrHcYZCOjB6NES4O|g>
10A/HER2YVMA NXe0eGVOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVewMlEuOC53IN88US=> M4LCWVkh\A>? MU\y[YR2[2W|IITo[UB{cXqnLDDpcpZie2m4ZX7ld5Mh[W6mIHPlcIwhdnWvYnXyJI9nKGOxbH;ubYV{ NInFWZYzODN6M{G5Oy=>
MC38  MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rENVUh|ryP M3TYUlUh\A>? NH7IfHFqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJJRqdWVvZHXw[Y5l\W62IH3hco5meg>? MVexPVkxQTd2NB?=
U937 NVny[IpFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjWT4M2NTJyIN88US=> M3;SNlI1NTd{IHi= MoXNbY5pcWKrdIOgZ4VtdCCpcn;3eIghe2yrZ3j0cJk> M3zIV|E5PDl{MUGz
HLE  MUDDfZRwfG:6aYT5JGF{e2G7 MVuwMlAxOS1{MDFOwG0> Mki5OFghcA>? MlzKbY5lfWOnczDj[YxtKGO7dH;0c5hqfHliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MYmxPFMyQDR2Mx?=
HLF MYfDfZRwfG:6aYT5JGF{e2G7 MmTTNE4xODFvMkCg{txO NEPVcFA1QCCq MnO3bY5lfWOnczDj[YxtKGO7dH;0c5hqfHliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MVKxPFMyQDR2Mx?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-Smad2 / Smad ; 

PubMed: 29416682     


The expression of p-Smad-2 was down regulated by LY2109761 at the dose ranging from 0.1 to 100 μM.

E-cadherin; 

PubMed: 29416682     


The migration-related protein E-cadherin was signifcantly promoted by LY2109761 in a dose dependent manner, ranging from 1 to 100 μM/L.

β-catenin / MMP-9 / MMP-2 / nm23 / uPA / COX-2 ; 

PubMed: 19909744     


Protein lysates from livers of control mice and LY2109761-treated mice were analyzed by western blotting as indicated. β-actin was used as loading control. NS: non-specific band.

CDK2 / CDK4 / Cyclin D1 / p-Rb ; 

PubMed: 19909744     


Protein lysates from livers of control mice and LY2109761-treated mice were analyzed by western blotting as indicated. β-actin was used as loading control. NS: non-specific band.

29416682 19909744
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]
- Collapse
  • 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]
- Collapse
  • 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
Smiles C1C[N]2N=C(C3=NC=CC=C3)C(=C2C1)C4=CC=NC5=C4C=CC(=C5)OCCN6CCOCC6

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID