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  M3\KfmZ2dmO2aX;uJGF{e2G7 M3LXbFExyqEQvF5CpC=> Mne2NkBp MVnpcohq[mm2czDheZRweGijZ4mgbY5lfWO2aX;uJIJ6KGejbHHu[4lv M4LkcVI2OjZ6MES2
PC-3 MlfVSpVv[3Srb36gRZN{[Xl? NInWO4ExNjJxMj:0JO69VQ>? NUK5bphrOjRiaB?= MYrEUXNQ Mnz1bY5pcWKrdIOgWGdHNc7{MfMAl4lv\HWlZXSgV41i\DJiYXP0bZZifGmxbh?= NFfMenUzOjF5M{C1Ny=>
PMOs NYiwdJJyTnWwY4Tpc44hSXO|YYm= MYewMlIwOi92IN88US=> NHjkXmIzPCCq MnT3SG1UVw>? MWPpcohq[mm2czDUS2Yu|rJz4pETbY5lfWOnZDDTcYFlOiCjY4TpeoF1cW:w MXKyNlE4OzB3Mx?=
PC-3 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\q[lMxNjJxMjFOwG0> NXvuTXFkOjRiaB?= Mlz2SG1UVw>? MojrZoxw[2u|IITo[UBqdmirYnn0bY9vKG:oIHPlcIwheHKxbHnm[ZJifGmxbjDwdo9lfWOnZDDifUBVT0ZvzsKx M3\PV|IzOTd|MEWz
PMOs MknGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnuNFFbOC5{L{Kg{txO MkO3NlQhcA>? M2jNZ2ROW09? MoexZoxw[2u|IITo[UBqdmirYnn0bY9vKG:oIHPlcIwheHKxbHnm[ZJifGmxbjDwdo9lfWOnZDDifUBVT0ZvzsKx NF7MOpUzOjF5M{C1Ny=>
U87MG MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHubXVDPS9zMDFOwG0> M1KwNVIhcA>? NXTJdFdr\W6qYX7j[ZMhemGmaX;z[Y5{cXSrdnn0fS=> NYf0OJJYOjJyME[5PVg>
T98 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1Hke|UwOTBizszN NHvQS2MzKGh? NV7aW2l{\W6qYX7j[ZMhemGmaX;z[Y5{cXSrdnn0fS=> M3;xflIzODB4OUm4
U87MG MWfBdI9xfG:|aYOgRZN{[Xl? M3jM[|ExKM7:TR?= NILGSG8zKGh? MXTlcohidmOnczDyZYRq[XSrb36tbY5lfWOnZDDEUmEh\GGvYXflJIFv\CCjcH;weI9{cXNicnH0[ZM> MYOyNlAxPjl7OB?=
NMA-23 M1\y[mFxd3C2b4Ppd{BCe3OjeR?= NY\ocnR2OTBizszN NH3lTXYzKGh? M4TPe4VvcGGwY3XzJJJi\GmjdHnvck1qdmS3Y3XkJGRPSSCmYX3h[4Uh[W6mIHHwc5B1d3OrczDyZZRmew>? MnrvNlIxODZ7OUi=
HLE  NU\JTI94TnWwY4Tpc44hSXO|YYm= MmXYNE4xOS1zMEFCpI5O NF;iWpY1QCCq NFrFcFJqdmirYnn0d{B1cGVibXnndoF1cW:wIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NWDCdZhlOjB6NES4O|g>
HLF NW\od3JCTnWwY4Tpc44hSXO|YYm= M1Txe|AvODFvMUCwxsBvVQ>? NUXSdIVQPDhiaB?= M1zMXolvcGmkaYTzJJRp\SCvaXfyZZRqd25iaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MYOyNFg1PDh5OB?=
10A/HER2YVMA NVjFTII3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlL0NE4yNTBwNTFOwG0> MXu5JIQ> NWTvT2sxemWmdXPld{B1cGVic3n6[UwhcW64YYPpeoVv\XO|IHHu[EBk\WyuIH71cYJmeiCxZjDjc4xwdmmncx?= NXfB[od1OjB|OEOxPVc>
MC38  M1m2Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn24OUDPxE1? M376SVUh\A>? MYHpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIITpcYUu\GWyZX7k[Y51KG2jbn7ldi=> NYXSd|hGOTl7MEm3OFQ>
U937 M{LkOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnBepd3PS1{MDFOwG0> NFTUPXEzPC15MjDo NWXNZoV[cW6qaXLpeJMh[2WubDDndo94fGhic3zp[4h1dHl? NInXTmoyQDR7MkGxNy=>
HLE  MlX1R5l1d3SxeHn0fUBCe3OjeR?= M3T5dFAvODBzLUKwJO69VQ>? NW\CZ5pKPDhiaB?= M3XBeIlv\HWlZYOgZ4VtdCCleYTveI95cXS7IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NXTZeJkzOTh|MUi0OFM>
HLF M3T0fGN6fG:2b4jpeJkhSXO|YYm= MWiwMlAxOS1{MDFOwG0> MmDPOFghcA>? NULzRXpucW6mdXPld{Bk\WyuIHP5eI91d3irdImgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MmWyNVg{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)
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

文献中の引用 (6)



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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID