LY2109761

For research use only. Not for use in humans.

目录号:S2704

LY2109761 Chemical Structure

CAS No. 700874-71-1

LY2109761是一种新型的,选择性TGF-β receptor type I/II (TβRI/II)双重抑制剂,无细胞试验中Ki分别为38 nM和300 nM,对Smad2的磷酸化产生负面影响。LY2109761可抑制自噬而诱导凋亡。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 3537.29 现货
RMB 2214.81 现货
RMB 8763.3 现货
RMB 20229.3 现货
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客户使用Selleck生产的LY2109761发表文献96篇:

产品安全说明书

TGF-beta/Smad抑制剂选择性比较

生物活性

产品描述 LY2109761是一种新型的,选择性TGF-β receptor type I/II (TβRI/II)双重抑制剂,无细胞试验中Ki分别为38 nM和300 nM,对Smad2的磷酸化产生负面影响。LY2109761可抑制自噬而诱导凋亡。
靶点
TβRI [1]
(Cell-free assay)
TβRII [1]
(Cell-free assay)
38 nM(Ki) 300 nM(Ki)
体外研究

LY2109761 处理FG/GLT或L3.6pl/GLT单层细胞生长,没有抗增殖效果,但是显著抑制L3.6pl/GLT细胞低贴壁生长,这种作用存在剂量依赖性,按2 μM 和 20 μM处理,则抑制分别为~33% 和73%, 与 Gemcitabine联用可强增强这种效果。LY2109761(5 μM)阻断TβRI/II激酶活性,完全抑制基础型和TGF-β1刺激的L3.6pl/GLT cells细胞迁移和入侵,显著增强脱离诱导的凋亡,处理8小时,凋亡达 26%,且完全抑制TGF-β诱导的Smad2磷酸化。[1] 1 nM LY2109761通过提高E-钙粘蛋白表达,而显著阻断迁移和入侵,而不会抑制肝癌细胞的粘附。[2]LY2109761 预处理成胶质细胞瘤细胞,通过阻断TGF-β信号而增强细胞的放射敏感性。LY2109761(10 μM) 作用于GBM衍生的癌干细胞样细胞(CSLC), 降低自我更新和细胞增殖,而与辐射联合处理可显著增强。[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HepG2  MmjZSpVv[3Srb36gRZN{[Xl? NWfaSHJ3OTEEoN88UeKh NXfYWoFYOiCq MYnpcohq[mm2czDheZRweGijZ4mgbY5lfWO2aX;uJIJ6KGejbHHu[4lv M3i3UFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mk[4NFQ3Lz5{NUK2PFA1PjxxYU6=
PC-3 M4mzfmZ2dmO2aX;uJGF{e2G7 MUmwMlIwOi92IN88US=> M{fncVI1KGh? NF\TbJhFVVOR MX;pcohq[mm2czDUS2Yu|rJz4pETbY5lfWOnZDDTcYFlOiCjY4TpeoF1cW:w NYm2e5BNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKxO|MxPTNpPkKyNVc{ODV|PD;hQi=>
PMOs Mnm1SpVv[3Srb36gRZN{[Xl? M2Tnb|AvOi9{L{Sg{txO NX21PW01OjRiaB?= M3zjS2ROW09? NXuxVZpocW6qaXLpeJMhXEeILd8yNgKBm2mwZIXj[YQhW22jZEKgZYN1cX[jdHnvci=> M{PPWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MUezNFU{Lz5{MkG3N|A2OzxxYU6=
PC-3 MkPxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXNNE4zNzJizszN M3n5SVI1KGh? NYrPfYVJTE2VTx?= M1rP[4Jtd2OtczD0bIUhcW6qaXLpeIlwdiCxZjDj[YxtKHC{b3zp[oVz[XSrb36gdJJw\HWlZXSgZpkhXEeILd8yNS=> NHzVTXc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG3N|A2Oyd-MkKxO|MxPTN:L3G+
PMOs Mke3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnG2NE4zNzJizszN NF3XblAzPCCq MmrsSG1UVw>? MUXicI9kc3NidHjlJIlvcGmkaYTpc44hd2ZiY3XscEBxem:uaX\ldoF1cW:wIIDyc4R2[2WmIHL5JHRITi4QskG= MoDMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJzN{OwOVMoRjJ{MUezNFU{RC:jPh?=
U87MG MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrle2VpPS9zMDFOwG0> NYq3O486OiCq M4XVZoVvcGGwY3XzJJJi\Gmxc3Xud4l1cX[rdIm= NFWwbGY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkCwOlk6QCd-MkKwNFY6QTh:L3G+
T98 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnhOml3PS9zMDFOwG0> NHzyT3EzKGh? M{PxZ4VvcGGwY3XzJJJi\Gmxc3Xud4l1cX[rdIm= M1XyU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MEC2PVk5Lz5{MkCwOlk6QDxxYU6=
U87MG MYnBdI9xfG:|aYOgRZN{[Xl? NV6zVFlXOTBizszN M4\TRVIhcA>? NEDXOmZmdmijbnPld{Bz[WSrYYTpc44ucW6mdXPl[EBFVkFiZHHtZYdmKGGwZDDhdI9xfG:|aYOgdoF1\XN? Mom1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJyME[5PVgoRjJ{MEC2PVk5RC:jPh?=
NMA-23 NWXSTo5[SXCxcITvd4l{KEG|c3H5 M3HEVFExKM7:TR?= NEDaeo4zKGh? NV3FO3Vz\W6qYX7j[ZMhemGmaXH0bY9vNWmwZIXj[YQhTE6DIHThcYFo\SCjbnSgZZBweHSxc3nzJJJifGW| MlP5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJyME[5PVgoRjJ{MEC2PVk5RC:jPh?=
HLE  Mm\sSpVv[3Srb36gRZN{[Xl? NXvGWVVUOC5yMT2xNFDDqG6P NIL4dJI1QCCq MYHpcohq[mm2czD0bIUhdWmpcnH0bY9vKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NIHTVVU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEi0OFg4QCd-MkC4OFQ5Pzh:L3G+
HLF MYfGeY5kfGmxbjDBd5NigQ>? NHntfoYxNjBzLUGwNOKhdk1? NGTuUGQ1QCCq MXfpcohq[mm2czD0bIUhdWmpcnH0bY9vKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M325PVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyOES0PFc5Lz5{MEi0OFg4QDxxYU6=
10A/HER2YVMA MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfyNE4yNTBwNTFOwG0> NFi3fJo6KGR? MYHy[YR2[2W|IITo[UB{cXqnLDDpcpZie2m4ZX7ld5Mh[W6mIHPlcIwhdnWvYnXyJI9nKGOxbH;ubYV{ NFj6e4o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEO4N|E6Pyd-MkCzPFMyQTd:L3G+
MC38  NXjHXZV7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;rSVUh|ryP M{nDdlUh\A>? NYrYepJZcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUB1cW2nLXTldIVv\GWwdDDtZY5v\XJ? M2jLVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUC5O|Q1Lz5zOUmwPVc1PDxxYU6=
U937 MkfmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfnOU0zOCEQvF2= MVOyOE04OiCq M{PzRolvcGmkaYTzJINmdGxiZ4Lve5RpKHOuaXfoeIx6 NW\tXWNyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi0PVIyOTNpPkG4OFkzOTF|PD;hQi=>
HLE  NHjpdolEgXSxdH;4bZR6KEG|c3H5 M1GyVFAvODBzLUKwJO69VQ>? M3PyeVQ5KGh? MXjpcoR2[2W|IHPlcIwh[3m2b4TvfIl1gSCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MoixQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh|MUi0OFMoRjF6M{G4OFQ{RC:jPh?=
HLF NXzKe5BsS3m2b4TvfIl1gSCDc4PhfS=> NU\zeXRHOC5yMEGtNlAh|ryP M3jRb|Q5KGh? NIT3TJJqdmS3Y3XzJINmdGxiY4n0c5RwgGm2eTDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NVr0RnBWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUizNVg1PDNpPkG4N|E5PDR|PD;hQi=>
Sf9 M1rwXWZ2dmO2aX;uJIF{e2G7 NH3MXJAyKGi{ Mn\STY5pcWKrdHnvckBw\iCqdX3hckBJcXNvdHHn[4VlKFSJRnLleIFTOSCWMkC0SEBufXSjboSg[ZhxemW|c3XkJIlvKFOoOTDpcpNm[3RiY3XscJMh[W[2ZYKgNUBpeiCkeTDIWHJHKGG|c3H5MEBKSzVyIE2gNE4xODN5IN88UU4> MnXxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2MkKzN|IoRjJ7NEKyN|MzRC:jPh?=
Sf9 MlHPSpVv[3Srb36gZZN{[Xl? NGXp[XRKdmirYnn0bY9vKG:oIGTHSoJmfGFidInw[UBz\WOncITvdkAyKEGOS{WgLHQzODSGKTDlfJBz\XO|ZXSgbY4hW2Z7IHPlcIx{NCCLQ{WwJF0hOC5yNkmg{txONg>? NHXtSWs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEOxOFk1Oyd-MUizNVQ6PDN:L3G+
Mv1Lu-p3TP-Lux MU\BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MkC4RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDtbY5sKE24MVz1MZA{XFBvTIX4JINmdGy|IHL5JIx2[2moZYLhd4UhemWyb4L0[ZIh[XO|YYmsJGlEPTBiPTCwMlE5KM7:TT6= MojaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh|MUS5OFMoRjF6M{G0PVQ{RC:jPh?=
NIH3T3 MlzLRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NITHW3JCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIF7JTFNVOyClZXzsd{BjgSCdM1jdeIh6dWmmaX7lJIF{e2G7LDDJR|UxKD1iMD6yNUDPxE1w NHLING09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEOxOFk1Oyd-MUizNVQ6PDN:L3G+
Calu6 NXvxbJM5TnWwY4Tpc44h[XO|YYm= NHjBdW9KdmirYnn0bY9vKG:oIGTHSoJmfGFidInw[UBz\WOncITvdkAyKGmwIH;yZYxtgSCmb4Pl[EBpfW2jbjDDZYx2PiClZXzsd{B5\W6xZ4Lh[pRm\CCvb4Xz[UBjgSCLVmTJJJBp[XKvYXPvb4lv\XSrYzDhd5NigSxiRVO1NEA:KDBwMkO2JO69VS5? MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDNzNEm0N{c,OTh|MUS5OFM9N2F-
T-cells M2W0XWZ2dmO2aX;uJIF{e2G7 NUPxflByOSCqch?= NXXrRlZmUW6qaXLpeIlwdiCxZjDUS2Zj\XSjUkGgbY4hcHWvYX6gdJJqdWG{eTDUMYNmdGy|IHHzd4V{e2WmIHHzJHRITmKndHGtd5RqdXWuYYTl[EBRW02DRDDwbI9{eGixconsZZRqd25icILlbY5kfWKjdHXkJIZweiBzIHjyJIZwdGyxd3XkJIJ6KFSJRnLleIEh[WSmaYTpc44hdWWjc4Xy[YQh[W[2ZYKgPVAhdWmwczDifUBCdHCqYTDzZ5Jm\W5iYYPzZZktKEmFNUCgQUAxNjN5IN88UU4> MlTlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2MkKzN|IoRjJ7NEKyN|MzRC:jPh?=
Mv1Lu NYPxUVljTnWwY4Tpc44h[XO|YYm= M1LiN|EhcHJ? MWDJcohq[mm2aX;uJI9nKFSJRnLleIFTOSCrbjDtbY5sKE24MVz1JINmdGy|IHHzd4V{e2WmIHHzJHRITmKndHGtd5RqdXWuYYTl[EBRW02DREKgdIhwe3Cqb4L5cIF1cW:wIIDy[Ylv[3WkYYTl[EBnd3JiMTDodkBnd2yub4fl[EBjgSCWR1\i[ZRiKGGmZHn0bY9vKG2nYYP1doVlKGGodHXyJFE2KG2rboOsJGlEPTBiPTCwMlc2KM7:TT6= NUO1W4V6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0NlI{OzJpPkK5OFIzOzN{PD;hQi=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
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.

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.

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.

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.

19909744 29416682
体内研究 LY2109761 (50 mg/kg) 单独处理,或与Gemcitabine (25 mg/kg) 联用处理L3.6pl/GLT 移植瘤小鼠模型,显著降低肿瘤体积,分别降低~70%和~90%, 延长寿命,半数生存期分别为45.0 天和77.5天,且降低自发性腹腔转移。[1]与体外作用效果一致, LY2109761单独或与辐射联合处理原位 CSLC成胶质细胞瘤模型,显著抑制肿瘤生长,分别抑制43.4% 和76.3%,降低肿瘤侵袭和肿瘤血管密度,且作用于U87MG移植瘤小鼠模型,显著增强辐射诱导的肿瘤生长延迟。[3]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验:[1]
- 合并
  • Cell lines: Colo357FG/GLT, 和 Colo357L3.6pl/GLT
  • Concentrations: 溶于DMSO, 终浓度为~10 μM
  • Incubation Time: 48小时
  • Method: 使用剂量不断增高的LY2109761 (~10 μM) 处理细胞48 小时。移除含药物的培养基,使用PBS冲洗细胞两次,然后加入新鲜培养基。温育5天后,通过MTT法获得相对存活细胞数。
    (Only for Reference)
动物实验:[1]
- 合并
  • Animal Models: 原位移植L3.6pl/GLT 细胞的无胸腺裸鼠
  • Dosages: 50 mg/kg
  • Administration: 口服处理,每天两次
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 2 mg/mL (4.52 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
0.5% CMC+0.25% Tween 80 (suspensions)
16 mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 441.52
化学式

C26H27N5O2

CAS号 700874-71-1
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID