LY2109761 化学構造
分子量: 441.52



Quality Control & MSDS


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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  NICxNoRHfW6ldHnvckBCe3OjeR?= NV:5eWI{OTEEoN88UeKh M{TPUlIhcA>? MnzkbY5pcWKrdIOgZZV1d3CqYXf5JIlv\HWldHnvckBjgSCpYXzhcodqdg>? M3z0WlI2OjZ6MES2
PMOs NFPYOGhHfW6ldHnvckBCe3OjeR?= MmfrNE4zNzJxNDFOwG0> MnvvNlQhcA>? NGS5S5ZFVVOR M3S3WYlvcGmkaYTzJHRITi4QskJihLNqdmS3Y3XkJHNu[WR{IHHjeIl3[XSrb36= MXSyNlE4OzB3Mx?=
PC-3 NUH0fplJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vFdlAvOi9{IN88US=> MVOyOEBp MX;EUXNQ MojyZoxw[2u|IITo[UBqdmirYnn0bY9vKG:oIHPlcIwheHKxbHnm[ZJifGmxbjDwdo9lfWOnZDDifUBVT0ZvzsKx M{LLbFIzOTd|MEWz
PMOs NGLjeXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{P2PFAvOi9{IN88US=> Mn7FNlQhcA>? M1;YdmROW09? MWXicI9kc3NidHjlJIlvcGmkaYTpc44hd2ZiY3XscEBxem:uaX\ldoF1cW:wIIDyc4R2[2WmIHL5JHRITi4QskG= NH23XI4zOjF5M{C1Ny=>
U87MG NFnHZlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NELpc4U2NzFyIN88US=> NIHJN4ozKGh? MWnlcohidmOnczDyZYRqd3OnboPpeIl3cXS7 MVKyNlAxPjl7OB?=
T98 NXHmTY9xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHr5cYM2NzFyIN88US=> NFXybVEzKGh? NFToemdmdmijbnPld{Bz[WSrb4PlcpNqfGm4aYT5 M{nZVFIzODB4OUm4
U87MG MUHBdI9xfG:|aYOgRZN{[Xl? NXvNcFNHOTBizszN NYjOTlFQOiCq M1XxRoVvcGGwY3XzJJJi\GmjdHnvck1qdmS3Y3XkJGRPSSCmYX3h[4Uh[W6mIHHwc5B1d3OrczDyZZRmew>? MoX1NlIxODZ7OUi=
NMA-23 MlfRRZBweHSxc3nzJGF{e2G7 MmLiNVAh|ryP M3rIR|IhcA>? MY\lcohidmOnczDyZYRq[XSrb36tbY5lfWOnZDDEUmEh\GGvYXflJIFv\CCjcH;weI9{cXNicnH0[ZM> MmTvNlIxODZ7OUi=
HLE  MYHGeY5kfGmxbjDBd5NigQ>? M2DzSVAvODFvMUCwxsBvVQ>? MUG0PEBp NUHPTFZvcW6qaXLpeJMhfGinIH3p[5JifGmxbjDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= MYmyNFg1PDh5OB?=
HLF MVXGeY5kfGmxbjDBd5NigQ>? NWnz[ZBNOC5yMT2xNFDDqG6P MnvBOFghcA>? NEnVeopqdmirYnn0d{B1cGVibXnndoF1cW:wIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ MkTsNlA5PDR6N{i=
10A/HER2YVMA NXXIVo9nT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlThNE4yNTBwNTFOwG0> MnfvPUBl MkHOdoVlfWOnczD0bIUhe2m8ZTygbY53[XOrdnXu[ZN{KGGwZDDj[YxtKG63bXLldkBw\iClb3zvcolmew>? MlTlNlA{QDNzOUe=
MC38  NGTXTXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3Dcm9vPSEQvF2= MkL4OUBl MVvpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIITpcYUu\GWyZX7k[Y51KG2jbn7ldi=> Mn[5NVk6ODl5NES=
U937 NGrTfIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2XobFUuOjBizszN M2D6XFI1NTd{IHi= NG\KVXpqdmirYnn0d{Bk\WyuIHfyc5d1cCC|bHnnbJRtgQ>? NVTzVI1JOTh2OUKxNVM>
HLE  M3fJeGN6fG:2b4jpeJkhSXO|YYm= NEfYUXIxNjByMT2yNEDPxE1? NXv3dZNSPDhiaB?= M2j2NIlv\HWlZYOgZ4VtdCCleYTveI95cXS7IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ MkHTNVg{OTh2NEO=

... 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)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
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

文献中の引用 (6)



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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID