Sotrastaurin (AEB071)

For research use only. Not for use in humans.

目录号：S2791

Sotrastaurin (AEB071) Chemical Structure

CAS No. 425637-18-9

Sotrastaurin (AEB071) 是一种有效的，选择性的泛PKC抑制剂，最有效作用于PKCθ，无细胞试验中Ki为0.22 nM；对PKCζ没有活性。Phase 2。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1566.89 现货
RMB 1414.55 现货
RMB 5468.97 现货
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客户使用Selleck生产的Sotrastaurin (AEB071)发表文献51篇：

产品安全说明书

PKC抑制剂选择性比较

生物活性

产品描述 Sotrastaurin (AEB071) 是一种有效的，选择性的泛PKC抑制剂，最有效作用于PKCθ，无细胞试验中Ki为0.22 nM；对PKCζ没有活性。Phase 2。
特性 同以往的PKC抑制剂不同，AEB071并不会在激活诱导的细胞死亡模型中增强鼠T细胞原幼细胞的凋亡。
靶点
PKCθ [1]
(Cell-free assay)		 PKCβ1 [1]
(Cell-free assay)		 PKCα [1]
(Cell-free assay)		 PKCη [1]
(Cell-free assay)		 PKCδ [1]
(Cell-free assay)
0.22 nM(Ki) 0.64 nM(Ki) 0.95 nM(Ki) 1.8 nM(Ki) 2.1 nM(Ki)
体外研究

在人和鼠的早期T细胞中，毫微摩尔级浓度的AEB071 (< 10μM)则能有效消除早期T细胞激活的信号如白介素-2分泌物和CD25表达。在没发生非特异性抗增殖的效应的细胞中，AEB071 (200 nM)能抑制CD3/CD28抗体和同种抗原诱导的T瞎报增殖反应。AEB071(<3 μM)可以显著抑制淋巴细胞功能相关抗原1介导的T细胞的粘附作用。[1] AEB071(< 20 μM)特异性地降低CD79突变体ABC DLBCL细胞系的增殖，随之能减少NF-κB信号活性。3 μM 浓度的AEB071可诱导CD79突变细胞在G1阻断和/或细胞坏死。[2]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
T cell MYHGeY5kfGmxbjDBd5NigQ>? M1PGXlExOCCwTR?= MVWzJIg> MVfEUXNQ MULpcohq[mm2czDyVm5CKHO7boTo[ZNqew>? NVrF[XFWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW2PVEyPThpPkK1OlkyOTV6PD;hQi=>
HUVECs  Mon4SpVv[3Srb36gRZN{[Xl? M3TKV|UxOG6P NWXVUGZsOSCq NVy1O4Z3WmWmdXPld{BFXFhvVILp[4dmemWmIFXu[I91cGWuaXHsJGR6e2[3bnP0bY9v NGfCeGw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NU[zOFU{QCd-MkW2N|Q2Ozh:L3G+
A549 NXHsRpllTnWwY4Tpc44hSXO|YYm= Mki4NE4yyqEQvF2= MnrpNlQhcA>? NHnybWxl\WO{ZXHz[ZMhfGinIILlcIF1cX[nIGDLR{3PuSCuZY\lcEBwdiClZXzsJI1mdWK{YX7lJINwfHKnYYTl[EBCWy2LVh?= MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJzOEG2NUc,OjV{MUixOlE9N2F-
A549 NHvMeG5HfW6ldHnvckBCe3OjeR?= M1naOlAvOcLizszN NUTYSpY5OjRiaB?= NF3kUJdz\WS3Y3XzJJRp\SCneIDy[ZN{cW:wIHzleoVteyCxZjDNUXAuOixiTV3QMVkh[W6mIHnueIVoemmwIN8yNS=> NIL4doE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKxPFE3OSd-MkWyNVgyPjF:L3G+
A549 M3PDbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{PoTlAvOcLizszN MlLoNlQhcA>? NWfwPVdV\W6qYX7j[ZMh\3Kxd4ToJIlvcGmkaYTpc44h[2:2cnXheIVlKHerdHigRXMuUVZ? M{OyclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkG4NVYyLz5{NUKxPFE3OTxxYU6=
Mel202 NFPrWWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fsfVAvPSEQvF2= NVzJSZU2OyCq NGfqdGNFVVOR MVzlcohidmOnczDJVk1qdmS3Y3XkJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fS=> MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV7NUO4OUc,OjR3OUWzPFU9N2F-
92.1 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\zbVAvPSEQvF2= NYrKW|RsOyCq NFzU[mFFVVOR NUe5UZlv\W6qYX7j[ZMhUVJvaX7keYNm\CC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHl? MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV7NUO4OUc,OjR3OUWzPFU9N2F-
OCM3 NXXrRlduT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFznOXUxNjVizszN M2jyWlMhcA>? NHrhcIRFVVOR NEfQXYJmdmijbnPld{BKWi2rbnT1Z4VlKHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gQ>? NXGzS3E6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1PVU{QDVpPkK0OVk2Ozh3PD;hQi=>
Mel202 NHjNeGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIGzNJUxNjVizszN NF\z[Ys{KGh? M13HR2ROW09? M3y1SYlv[3KnYYPld{BKWi2rbnT1Z4VlKGOnbHygZ5lkdGViYYLy[ZN1yqB? MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV7NUO4OUc,OjR3OUWzPFU9N2F-
92.1 NY\PWnBiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYewMlUh|ryP M3LKclMhcA>? M3fremROW09? NH;t[pFqdmO{ZXHz[ZMhUVJvaX7keYNm\CClZXzsJIN6[2ynIHHydoV{fMLi M2H0WVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NUm1N|g2Lz5{NEW5OVM5PTxxYU6=
OCM3 MmLFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rIVlAvPSEQvF2= M{fnO|MhcA>? MWTEUXNQ NVf4ZoxDcW6lcnXhd4V{KEmULXnu[JVk\WRiY3XscEBkgWOuZTDhdpJme3UEoB?= NI\aRXI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW5OVM5PSd-MkS1PVU{QDV:L3G+
Jeko-1 MonIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzDZWMxNTRizszN NIrhfoZFVVOR MWrpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NHPQOnM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2Nlk{PSd-MkSzOlI6OzV:L3G+
Mino NVn4Vm9HT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jFWVAuPCEQvF2= Ml3LSG1UVw>? Moj4bY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NVfKcmV4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlI6OzVpPkK0N|YzQTN3PD;hQi=>
Rec-1 Mm\3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXpUXpPOC12IN88US=> MoLSSG1UVw>? NXnxSYpWcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NGrZ[JE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2Nlk{PSd-MkSzOlI6OzV:L3G+
SP49 NHW3dZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfWRXFuOC12IN88US=> NU[xW5EzTE2VTx?= MoCwbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NEOxOI09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2Nlk{PSd-MkSzOlI6OzV:L3G+
Jeko-1 MX7GeY5kfGmxbjDBd5NigQ>? Mn3rNk42KM7:TdMg NYWy[lM4OTJiaB?= NFvDelBFVVOR MYXkc5dvemWpdXzheIV{KE6ILd86RkB1[XKpZYSg[4Vv\XN? M{n5flxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{[yPVM2Lz5{NEO2Nlk{PTxxYU6=
Mino MmfXSpVv[3Srb36gRZN{[Xl? NYHZcGpjOi53IN88UeKh NVHwXWRoOTJiaB?= NGKyZmJFVVOR M{fzU4Rwf26{ZXf1cIF1\XNiTl[t{tpDKHSjcnfleEBo\W6ncx?= MlHkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NkK5N|UoRjJ2M{[yPVM2RC:jPh?=
Rec-1 MUPGeY5kfGmxbjDBd5NigQ>? NEC0OI8zNjVizszNxsA> MXuxNkBp MXTEUXNQ MUHkc5dvemWpdXzheIV{KE6ILd86RkB1[XKpZYSg[4Vv\XN? NITOVVE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2Nlk{PSd-MkSzOlI6OzV:L3G+
SP49 NW\aZWY3TnWwY4Tpc44hSXO|YYm= MlrZNk42KM7:TdMg MWKxNkBp NVfJPY9wTE2VTx?= M3zI[YRwf26{ZXf1cIF1\XNiTl[t{tpDKHSjcnfleEBo\W6ncx?= M1rnSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{[yPVM2Lz5{NEO2Nlk{PTxxYU6=
CD3+ T  MUPGeY5kfGmxbjDBd5NigQ>? NEfmT4kxNTVyMDDuUS=> MUCxJIg> M2PuSolvcGmkaYTzJG5HNc78QjDwbI9{eGixconsZZRqd25iaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MkLKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3N{OyPFMoRjJ|NUezNlg{RC:jPh?=
Mel202 M1\lVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXGNE02KM7:TR?= MoryO|IhcA>? Mlr6SG1UVw>? NHjhUZRqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 M1jBVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkWzPVY5Lz5{Mk[1N|k3QDxxYU6=
Omm1.3 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mme1NE02KM7:TR?= MXW3NkBp M1\YdWROW09? M4\LOolvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> MkW2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4NUO5OlgoRjJ{NkWzPVY5RC:jPh?=
92.1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3DNE02KM7:TR?= Moj0O|IhcA>? MmnwSG1UVw>? MXrpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NGjqZ2k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[1N|k3QCd-MkK2OVM6Pjh:L3G+
Mel202 MoLUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3:5Z|Uh|ryP M4XQclI1KGh? NULReoliTE2VTx?= MWXpcoR2[2W|IFexJIFzemW|dNMg MmjVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4NUO5OlgoRjJ{NkWzPVY5RC:jPh?=
Omm1.3 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DIe|Uh|ryP NWfVNpE{OjRiaB?= NHXjW4xFVVOR M1HucYlv\HWlZYOgS|Eh[XK{ZYP0xsA> NIDZ[oY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[1N|k3QCd-MkK2OVM6Pjh:L3G+
92.1 NHzoVVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfT[oszPSEQvF2= Mn\tNlQhcA>? NWTqZ3dOTE2VTx?= NIT2cW5qdmS3Y3XzJGcyKGG{cnXzeOKh MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ3M{m2PEc,OjJ4NUO5Olg9N2F-
Mel202 M1[1UmFxd3C2b4Ppd{BCe3OjeR?= NU\WPJVvPSEQvF2= NIHWSmc4OiCq NU\sRmk5TE2VTx?= M{jtNIlv\HWlZYOgZZBweHSxc3nzJJNtcWeqdHz5 M4T4elxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkWzPVY5Lz5{Mk[1N|k3QDxxYU6=
Omm1.3 M4rQe2Fxd3C2b4Ppd{BCe3OjeR?= NVzn[II4PSEQvF2= M3PWcVczKGh? MnPoSG1UVw>? MmfJbY5lfWOnczDhdI9xfG:|aYO= MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ3M{m2PEc,OjJ4NUO5Olg9N2F-
92.1 NUnoVllPSXCxcITvd4l{KEG|c3H5 M2O4XlUh|ryP Mn3LO|IhcA>? M3npW2ROW09? NELKOI5qdmS3Y3XzJIFxd3C2b4Ppd{B{cWewaX\jZY51dHl? Mmn2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4NUO5OlgoRjJ{NkWzPVY5RC:jPh?=
Mel202 MUPGeY5kfGmxbjDBd5NigQ>? MYi1JO69VQ>? NWDyd5NkOjRiaB?= MnP0bY5pcWKrdIOg[ZhxemW|c3nvckBidmRicHjvd5Bpd3K7bHH0bY9vKG:oIGDLR{Bqe2:ob4Ltdy=> MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ3M{m2PEc,OjJ4NUO5Olg9N2F-
Omm1.3 MlvwSpVv[3Srb36gRZN{[Xl? NHHwPI42KM7:TR?= MXGyOEBp NWW0OpNrcW6qaXLpeJMh\XiycnXzd4lwdiCjbnSgdIhwe3Cqb4L5cIF1cW:wIH;mJHBMSyCrc3;mc5Juew>? NGTkSVY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[1N|k3QCd-MkK2OVM6Pjh:L3G+
92.1 NHH4WoZHfW6ldHnvckBCe3OjeR?= NW\sVW5mPSEQvF2= M1f4S|I1KGh? NEHFZ5NqdmirYnn0d{BmgHC{ZYPzbY9vKGGwZDDwbI9{eGixconsZZRqd25ib3[gVGtEKGm|b3\vdo1{ M1WzSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkWzPVY5Lz5{Mk[1N|k3QDxxYU6=
HBL1 Mo\VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHM[HVZOC5zNj2yNEDPxE1? MknOOUBl MXrJR|UxRTBwNTFOwG0> NFPPfJc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUOyOFkzOCd-MkGzNlQ6OjB:L3G+
TMD8 MofsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTufIMxNjF4LUKwJO69VQ>? MkjaOUBl MXLJR|UxRTBwMjFOwG0> MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN{NEmyNEc,OjF|MkS5NlA9N2F-
OCI-Ly10 NHfXVWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHPNE4yPi1{MDFOwG0> M1e0[lUh\A>? NHnUbpZKSzVyPUGuN{DPxE1? MkX0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|MkS5NlAoRjJzM{K0PVIxRC:jPh?=
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OCI-Ly3 MnPiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn:xNE4yPi1{MDFOwG0> MnvjOUBl NFuxO4RKSzVy78{eNlAh|ryP MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN{NEmyNEc,OjF|MkS5NlA9N2F-
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SuDHL4 M3mxO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWW2bnhuOC5zNj2yNEDPxE1? NG\n[5c2KGR? NELrTGxKSzVy78{eNlAh|ryP M165SVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{K0PVIxLz5{MUOyOFkzODxxYU6=
DB MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHXpc|AxNjF4LUKwJO69VQ>? NIe1XmM2KGR? M3X0NGlEPTExvK6yNEDPxE1? M{Xs[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{K0PVIxLz5{MUOyOFkzODxxYU6=
Jurkat IL-2 M3nkRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NETXTW9KSzVyPU[uO|EhyrFiMz63OkDPxE1? MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl2MEK1PUc,OTl7NECyOVk9N2F-
PBMC IL-2 Mmi1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTRwOESgxtEhOS55MDCg{txO NH:yXYw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm0NFI2QSd-MUm5OFAzPTl:L3G+
Jurkat MYXGeY5kfGmxbjDhd5NigQ>? NUX5VVVwUW6qaXLpeIlwdiCxZjDUR3IwS0R{OD3t[YRq[XSnZDDoeY1idiCWIHPlcIwh[WO2aY\heIlwdiCrbjDKeZJs[XRiY3XscJMh\XiycnXzd4lv\yCqdX3hckBKVDJicILvcY91\XJiYomgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6NCCLQ{WwJF0hOC5yNUSg{txONg>? MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTh{N{izNUc,OTl6Mke4N|E9N2F-
Jurkat T Ml;2SpVv[3Srb36gZZN{[Xl? NIDFeYE2KGi{cx?= M{\ybWlvcGmkaYTpc44hd2ZiUFvDeIhmfGFiaX6gbJVu[W5iSoXyb4F1KFRiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJIFvfGlvQ1SzM2NFOjhiYX70bYJw\HlvaX7keYNm\CCWLXPlcIwh[WO2aY\heIlwdiCkeTDt[YF{fXKrbneg[IVkemWjc3WgbY4hUUxvMjDz[YNz\XSrb36gZYZ1\XJiNTDodpMh[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5MEBKSzVyIE2gNE4xQDFizszNMi=> M1q1S|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MUOxO|E1Lz5{OEGzNVcyPDxxYU6=
B-cells NXHQTXBPTnWwY4Tpc44h[XO|YYm= NH\4doRKdmirYnn0bY9vKG:oIGDLR4JmfGFiaX6gcY92e2ViQjDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4hUWePLYP0bY12dGG2ZXSgZ4VtdCCycn;sbYZmemG2aX;uMEBKSzVyIE2gNE4zOzRizszNMi=> MkDwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhzM{G3NVQoRjJ6MUOxO|E1RC:jPh?=
bone marrow cells NHvyO4pCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MoHKOEBl[Xm| MXfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IFPCRUBud3W|ZTDic45mKG2jcoLve{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIGuzTH11cHmvaXTpcoUhcW6lb4Lwc5JifGmxbjDh[pRmeiB2IHThfZMtKEmFNUCgQUA{NjdizszNMi=> MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTh{N{izNUc,OTl6Mke4N|E9N2F-

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
pPKCδ/θ / phosphorylated MARCKS / p53 / MDM2 / PUMA / p21; 

PubMed: 29593251     


Cell lines OMM2.3, OMM2.5 and OMM1 were treated with 8 µM Nutlin-3 and 4 µM Sotrastaurin. MEL290 was incubated with 2 µM Nutlin-3 and 4 µM Sotrastaurin, cell line MM28 with 8 µM Nutlin-3 and 1 µM Sotrastaurin, and cell lines MEL202, MEL270 and MM66 with 2䲧疝Ỵ疞㧀疜膉痘 瘿�෋ᾰƌ෋à 㺣痖帉痖Ѐ瑖堘𢡄빢᎒෋à鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸堞圔堙빢᎒圞堙圭堙𢡄玚Wᾰƌ ᾰƌ戤瘯Ɖ뙠ෆ䐺痖暼瘿뙠ෆᾰƌ 뙠ෆÐ㺣痖뙠ෆ€𢡄뙤ෆ€䀷痗뙤ෆ౴뙤ෆ㵶痗뙤ෆ뺖᎒泌Itemｾ᎒Count﫨呂뚔ෆ猴፲뙤ෆ፲씢痗猸፲髸莤䥷堙᎒ｾ᎒�堞ﻮ᎒፲露𢡄堚Ѽ齃礤v�堞ﻮ᎒猢Wｾ᎒䨼Ą鹿齃

Cyclin D1 / p27(Kip1) ; 

PubMed: 22653968     


AEB071 selectively increased p27 and decreased cyclin D1 expression in GNAQ mutant UM cells. Cells were treated with 0, 2, or 5 μM AEB071 for 72 hours and analyzed by immunoblot. WT = GNAQ wild type; MT = GNAQ mutation.

Bcl-xl / XIAP / Survivin ; 

PubMed: 22653968     


AEB071 decreased the expression of antiapoptotic proteins Bcl-xL, XIAP, and survivin in GNAQ mutated cells. WT = GNAQ wild type; MT = GNAQ mutation.

PKCα / PKCδ / PKCβ / PKCε / PKCθ ; 

PubMed: 22653968     


AEB071 inhibited PKC expression in UM cells. Cells were treated with 5 μM AEB071 for 24 hours in the presence of 10% FBS and subjected to immunoblot analysis. PKCδ, ε and θ levels in AEB treated cells relative to control (DMSO treated) cells are also show䲧疝Ỵ疞㧀疜膉痘 瘿⟸෕ᾰƌ෕Ð 㺣痖帉痖Ѐ瑖堘𢡄빢᎒෕Ð鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸堞圔堙빢᎒圞堙圭堙𢡄玚Wᾰƌ ᾰƌ戤瘯Ɖ삨Ղ䐺痖暼瘿삨Ղᾰƌ 삨Ղà㺣痖삨Ղ€𢡄사Ղ€䀷痗사Ղ౴사Ղ㵶痗사Ղ뺖᎒泌Itemｾ᎒Count﫨呂샜Ղ猴፲사Ղ፲씢痗猸፲髸莤䥷堙᎒

p-Marcks / p-ERK / p-AKT / p-S6 / Marcks / ERK / AKT / S6; 

PubMed: 22653968     


AEB071 inhibits PKC and mTOR pathways but not AKT. Western Blot of MARCKS, ERK, ribosomal S6 and AKT phosphorylation following drug treatments for 24 hrs. α-Tubulin was used as a loading control.

29593251 22653968
Growth inhibition assay
Cell viability ; 

PubMed: 22653968     


AEB071 selectively reduced viability of UM cells harboring GNAQ mutations. Cells were treated with varying amount of AEB071 for 72 hours. Data are presented as mean±SD of 4 or 5 independent experiments. NM = normal melanocytes; WT = GNAQ wild type; MT = G䲧疝Ỵ疞㧀疜膉

22653968
体内研究 AEB071(80 mg/kg) 可以在体内显著抑制SCID的皮下TMD8移植模型肿瘤的生长。[2] 每日两次口服10 mg/kg 和30 mg/kg AEB071，能延长心脏移植的大鼠的存活率，这种作用是剂量依赖抑制免疫力的效应。[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)

动物实验：[3]
- 合并
  • Animal Models: 雄性 Wistar/F大鼠
  • Dosages: 10 mg/kg 和 30 mg/kg
  • Administration: 口服一次
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 87 mg/mL (198.41 mM)
Water Insoluble
Ethanol '2 mg/mL
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)：
2% DMSO+30% PEG 300+ddH2O
 10mg/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 438.48
化学式

C25H22N6O2
CAS号 425637-18-9
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 只
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、SDS / 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、SDS / 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
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02273219 Unknown status Drug: AEB071|Drug: BYL719 Uveal Melanoma Richard D. Carvajal|Columbia University November 2014 Phase 1
NCT01801358 Terminated Drug: AEB071|Drug: MEK162 Uveal Melanoma Array Biopharma now a wholly owned subsidiary of Pfizer|Array BioPharma August 2013 Phase 1|Phase 2
NCT01430416 Completed Drug: AEB071 Uveal Melanoma Novartis Pharmaceuticals|Novartis December 20 2011 Phase 1
NCT01402440 Terminated Drug: AEB071 Diffuse Large B-Cell Lymphoma Novartis Pharmaceuticals|Novartis November 2011 Phase 1

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1：

    Could you give me the information about how to prepare Sotrastaurin for oral administration in mice?

  • 回答：

    S2791 Sotrastaurin can be dissolved in 2% DMSO/30% PEG 300/ddH2O at 10 mg/ml as a clear solution which can be used for injection, and in 2% DMSO/corn oil at 10 mg/ml as a suspension for oral administration.

Selleck产品目录册

PKC Signaling Pathway Map

PKC Inhibitors with Unique Features

  • 选择性强的PKC抑制剂

    Enzastaurin (LY317615) : PKCβ-selective, IC50=6 nM.

  • 活性最高的PKC抑制剂

    Go 6983 : PKCα, IC50=7 nM; PKCβ, IC50=7 nM; PKCγ, IC50=6 nM; PKCδ, IC50=10 nM.

  • 用于临床的PKC抑制剂

    Dequalinium Chloride : Phase III for Bacterial Vaginosis.

相关PKC产品

  • SD-208 New

    SD-208是一种选择性TGF-βRI (ALK5)抑制剂，with IC50为48 nM，选择性比TGF-βRII高100多倍。

  • Staurosporine (AM-2282)

    Staurosporine (AM-2282, Antibiotic AM-2282, STS)是一种有效的PKC抑制剂，在无细胞试验中作用于PKCα，PKCγ 和PKCη，IC50分别为2 nM，5 nM 和 4 nM，对PKCδ(20 nM)和PKCε(73 nM作用较弱，对PKCζ (1086 nM)的活性很低。同时 对其他的激酶PKA, PKG, S6K, CaMKII, 等也显示抑制活性。Phase 3。

  • Go 6983

    Go 6983 (GOE 6983, Gö 6983)是一种pan-PKC抑制剂，作用于PKCα， PKCβ， PKCγ和PKCδ，IC50分别为7 nM， 7 nM， 6 nM和10 nM，对PKCζ作用稍弱，抑制PKCμ活性。

  • Enzastaurin (LY317615)

    Enzastaurin (LY317615)是一种有效的PKCβ选择性抑制剂，无细胞试验中IC50为6 nM，比作用于PKCα，PKCγ和PKCε选择性高6到20倍。Phase 3。

  • Bisindolylmaleimide I (GF109203X)

    Bisindolylmaleimide I (GF109203X, GO 6850)是一种有效的PKC抑制剂，作用于PKCα，PKCβI，PKCβII和PKCγ，无细胞试验中IC50分别为20 nM， 17 nM， 16nM和20 nM，作用于PKC比作用于EGFR，PDGFR和胰岛素受体选择性高3000倍以上。

  • Go6976

    Go6976 (PD406976)是一种强效的PKC抑制剂，其对PKC (老鼠大脑), PKCα, and PKCβ1的IC50分别为7.9nM，2.3 nM, 和 6.2 nM 。此外，也是JAK2 和 Flt3的强抑制剂。

  • Dequalinium Chloride

    Dequalinium Chloride是一种PKC抑制剂，IC50为7-18 μM，同时也是一种选择性蜂毒明肽敏感型钾离子通道阻断剂，IC50为1.1 μM.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID