LY2109761 化学構造
分子量: 441.52





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  • 研究分野



製品説明 LY2109761は、新しい選抜TGFβレセプター・タイプIとタイプII(TβRI/II)二重阻害剤で、 Ki がそれぞれ38 nM と 300 nMになる。
ターゲット TβRI TβRII
IC50 38 nM (Ki) 300 nM (Ki) [1]
In vitro試験 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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
HepG2  NYD2RY1PTnWwY4Tpc44hSXO|YYm= MljJNVDDqM7:TdMg NHXyb5kzKGh? NEXDW3dqdmirYnn0d{BifXSxcHjh[5khcW6mdXP0bY9vKGK7IHfhcIFv\2mw MoDZNlUzPjhyNE[=
PC-3 NGnlc4hHfW6ldHnvckBCe3OjeR?= NE[yb3IxNjJxMj:0JO69VQ>? NVzzXFNxOjRiaB?= M4nVUmROW09? NVzNUIx6cW6qaXLpeJMhXEeILd8yNgKBm2mwZIXj[YQhW22jZEKgZYN1cX[jdHnvci=> NFLjcYozOjF5M{C1Ny=>
PMOs NILlVWpHfW6ldHnvckBCe3OjeR?= M{[xe|AvOi9{L{Sg{txO NFL6fI8zPCCq NFHofHZFVVOR M3WwdolvcGmkaYTzJHRITi4QskJihLNqdmS3Y3XkJHNu[WR{IHHjeIl3[XSrb36= NIP2b3kzOjF5M{C1Ny=>
PC-3 NIXYRWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHHHT2gxNjJxMjFOwG0> MVOyOEBp NIDQTJRFVVOR M{m4VIJtd2OtczD0bIUhcW6qaXLpeIlwdiCxZjDj[YxtKHC{b3zp[oVz[XSrb36gdJJw\HWlZXSgZpkhXEeILd8yNS=> NIe4fYozOjF5M{C1Ny=>
PMOs MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEixRYgxNjJxMjFOwG0> MU[yOEBp NWDj[VZ2TE2VTx?= NUjnXnpM[myxY3vzJJRp\SCrbnjpZol1cW:wIH;mJINmdGxicILvcIln\XKjdHnvckBxem:mdXPl[EBjgSCWR1[t{tIy MXqyNlE4OzB3Mx?=
U87MG NIqyOYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoX0OU8yOCEQvF2= NIDtU4szKGh? M1zsT4VvcGGwY3XzJJJi\Gmxc3Xud4l1cX[rdIm= MUOyNlAxPjl7OB?=
T98 M13JU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVS1M|ExKM7:TR?= MWmyJIg> NF3QXm5mdmijbnPld{Bz[WSrb4PlcpNqfGm4aYT5 M3Lo[VIzODB4OUm4
U87MG NIDQRmdCeG:ydH;zbZMhSXO|YYm= Ml7XNVAh|ryP MUGyJIg> MXLlcohidmOnczDyZYRq[XSrb36tbY5lfWOnZDDEUmEh\GGvYXflJIFv\CCjcH;weI9{cXNicnH0[ZM> MoDoNlIxODZ7OUi=
NMA-23 MkHJRZBweHSxc3nzJGF{e2G7 Mn7aNVAh|ryP MmSwNkBp M1fITYVvcGGwY3XzJJJi\GmjdHnvck1qdmS3Y3XkJGRPSSCmYX3h[4Uh[W6mIHHwc5B1d3OrczDyZZRmew>? MYGyNlAxPjl7OB?=
HLE  MVzGeY5kfGmxbjDBd5NigQ>? NWHJOGxHOC5yMT2xNFDDqG6P MnLzOFghcA>? NEXteI1qdmirYnn0d{B1cGVibXnndoF1cW:wIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ M4W4WVIxQDR2OEe4
HLF MVvGeY5kfGmxbjDBd5NigQ>? NV\WcJdQOC5yMT2xNFDDqG6P MlT3OFghcA>? NEPGb4NqdmirYnn0d{B1cGVibXnndoF1cW:wIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ MkDVNlA5PDR6N{i=
10A/HER2YVMA M{LxVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTYUmd2OC5zLUCuOUDPxE1? NWTUfHU6QSCm M3G2RpJm\HWlZYOgeIhmKHOrenWsJIlvfmG|aY\lcoV{eyCjbnSgZ4VtdCCwdX3i[ZIhd2ZiY3;sc45q\XN? NYLrVlQ{OjB|OEOxPVc>
MC38  NXrxcHhDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm[5OUDPxE1? MYe1JIQ> Ml\0bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZI> NYTZS|BvOTl7MEm3OFQ>
U937 MoHPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjxXFhoPS1{MDFOwG0> NWe1NoU6OjRvN{KgbC=> M1PjNolvcGmkaYTzJINmdGxiZ4Lve5RpKHOuaXfoeIx6 Mmr2NVg1QTJzMUO=
HLE  NELVdYlEgXSxdH;4bZR6KEG|c3H5 M2D5cVAvODBzLUKwJO69VQ>? MkPHOFghcA>? M4HaXolv\HWlZYOgZ4VtdCCleYTveI95cXS7IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NYrjeIhDOTh|MUi0OFM>
HLF MkD6R5l1d3SxeHn0fUBCe3OjeR?= MonSNE4xODFvMkCg{txO MWO0PEBp M3XCZYlv\HWlZYOgZ4VtdCCleYTveI95cXS7IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NXS5RYVpOTh|MUi0OFM>

... Click to View More Cell Line Experimental Data

In vivo試験 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]

プロトコル (参考用のみ)

細胞アッセイ: [1]

細胞株 Colo357FG/GLT, and Colo357L3.6pl/GLT
濃度 Dissolved in DMSO, final concentrations ~10 μM
反応時間 48 hours
実験の流れ 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.

動物実験: [1]

動物モデル Athymic nude mice with orthotopic implantation of L3.6pl/GLT cells
製剤 Dissolved in the SX-1292 oral vehicle containing 1% sodium carboxymethylcellulose, 0.5% sodium lauryl sulfate, and 0.05% antifoam
投薬量 50 mg/kg
投与方法 Twice a day p.o.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)



Download LY2109761 SDF
分子量 441.52


CAS No. 700874-71-1
保管 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 2 mg/mL (4.52 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 0.5% CMC+0.25% Tween 80 16 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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.
化学名 7-(2-morpholinoethoxy)-4-(2-(pyridin-2-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)quinoline

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID