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61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 M{LTVGZ2dmO2aX;uJGF{e2G7 MVKxNFAhdk1? NGf3XIc{KGh? NGq1N2lFVVOR M2fLbolvcGmkaYTzJJJTVkFic4nueIhme2m| NVzSNYdiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW2PVEyPThpPkK1OlkyOTV6PD;hQi=>
HUVECs  MWjGeY5kfGmxbjDBd5NigQ>? MUK1NFBvVQ>? M3z5SFEhcA>? MYTS[YR2[2W|IFTUXE1VemmpZ3Xy[YQhTW6mb4To[Yxq[WxiRInz[pVv[3Srb36= NXjUc2dCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW2N|Q2OzhpPkK1OlM1PTN6PD;hQi=>
A549 MW\GeY5kfGmxbjDBd5NigQ>? NGPBXJUxNjIEoN88US=> Ml;1NlQhcA>? MXXk[YNz\WG|ZYOgeIhmKHKnbHH0bZZmKFCNQz5OtUBt\X[nbDDvckBk\WyuIH3lcYJz[W6nIHPveJJm[XSnZDDBV{1KXg>? M4n3T|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkG4NVYyLz5{NUKxPFE3OTxxYU6=
A549 MkfiSpVv[3Srb36gRZN{[Xl? MlnlNE4yyqEQvF2= M{\xN|I1KGh? NW\yb4E1emWmdXPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdHNib3[gUW1RNTJuIF3NVE06KGGwZDDpcpRm\3KrbjFOtlE> M2XYdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkG4NVYyLz5{NUKxPFE3OTxxYU6=
A549 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUWwMlHDqM7:TR?= M4\6eFI1KGh? M4jYTYVvcGGwY3XzJIdzd3e2aDDpcohq[mm2aX;uJINwfHKnYYTl[EB4cXSqIFHTMWlX M4rRZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkG4NVYyLz5{NUKxPFE3OTxxYU6=
Mel202 MmX2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3PS25WOC53IN88US=> M1TwN|MhcA>? NF\pdopFVVOR MkDE[Y5p[W6lZYOgTXIucW6mdXPl[EBz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJk> M{jnZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NUm1N|g2Lz5{NEW5OVM5PTxxYU6=
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OCM3 NYHDRZpyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NITYd|IxNjVizszN NVvIb5hDOyCq MmLPSG1UVw>? MVTlcohidmOnczDJVk1qdmS3Y3XkJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fS=> M2HMblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NUm1N|g2Lz5{NEW5OVM5PTxxYU6=
Mel202 M3XLRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;sVHgxNjVizszN MoLhN{Bp M123XWROW09? M4D4colv[3KnYYPld{BKWi2rbnT1Z4VlKGOnbHygZ5lkdGViYYLy[ZN1yqB? NXjaN5pyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1PVU{QDVpPkK0OVk2Ozh3PD;hQi=>
92.1 NHy0eYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkDYNE42KM7:TR?= M1XPSlMhcA>? NGXZTolFVVOR M{XxZ4lv[3KnYYPld{BKWi2rbnT1Z4VlKGOnbHygZ5lkdGViYYLy[ZN1yqB? M1uxUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NUm1N|g2Lz5{NEW5OVM5PTxxYU6=
OCM3 NIXae5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHwe5NFOC53IN88US=> MmP0N{Bp NVXLeVRNTE2VTx?= NFr6UWNqdmO{ZXHz[ZMhUVJvaX7keYNm\CClZXzsJIN6[2ynIHHydoV{fMLi NX\IUnpjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1PVU{QDVpPkK0OVk2Ozh3PD;hQi=>
Jeko-1 MnrXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWnYPWlMOC12IN88US=> NHrISlNFVVOR M{POcolvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> MnfwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NkK5N|UoRjJ2M{[yPVM2RC:jPh?=
Mino MlnJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;Md|AuPCEQvF2= M2G2TGROW09? Ml3ubY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MkLMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NkK5N|UoRjJ2M{[yPVM2RC:jPh?=
Rec-1 NWPZR2VJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2THRVAuPCEQvF2= NIC0UVVFVVOR MWTpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NH[z[5A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2Nlk{PSd-MkSzOlI6OzV:L3G+
SP49 Mk\MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUOwMVQh|ryP Mn:2SG1UVw>? NWrvdI93cW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NVr3WmpnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlI6OzVpPkK0N|YzQTN3PD;hQi=>
Jeko-1 MYPGeY5kfGmxbjDBd5NigQ>? NWXHbFY5Oi53IN88UeKh NWrvSWNXOTJiaB?= MlHkSG1UVw>? NV;zOG9j\G:5boLl[5Vt[XSnczDOSk3PwkJidHHy[4V1KGenbnXz M3vFbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{[yPVM2Lz5{NEO2Nlk{PTxxYU6=
Mino Mm\YSpVv[3Srb36gRZN{[Xl? MX[yMlUh|ryPwrC= NXzKOotJOTJiaB?= NFT1[5NFVVOR MVvkc5dvemWpdXzheIV{KE6ILd86RkB1[XKpZYSg[4Vv\XN? M2Hjd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{[yPVM2Lz5{NEO2Nlk{PTxxYU6=
Rec-1 MVrGeY5kfGmxbjDBd5NigQ>? NWDxOZp[Oi53IN88UeKh NUK3NpgyOTJiaB?= MYfEUXNQ MnPz[I94dnKnZ4XsZZRmeyCQRj5OvmIhfGG{Z3X0JIdmdmW| MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4MkmzOUc,OjR|NkK5N|U9N2F-
SP49 MmTWSpVv[3Srb36gRZN{[Xl? MXyyMlUh|ryPwrC= MXSxNkBp NF;TVFVFVVOR NWLMdYhJ\G:5boLl[5Vt[XSnczDOSk3PwkJidHHy[4V1KGenbnXz NILoWlc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2Nlk{PSd-MkSzOlI6OzV:L3G+
CD3+ T  M2PaWWZ2dmO2aX;uJGF{e2G7 NIXEVncxNTVyMDDuUS=> NGjSTFAyKGh? NFPCb|RqdmirYnn0d{BPTi4QulKgdIhwe3Cqb4L5cIF1cW:wIHnuJIEh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ Mkf1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3N{OyPFMoRjJ|NUezNlg{RC:jPh?=
Mel202 Mn[4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVfZdYllOC13IN88US=> M1XGeFczKGh? NVTHVpFGTE2VTx?= MlrQbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> M4fGT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkWzPVY5Lz5{Mk[1N|k3QDxxYU6=
Omm1.3 NUfHWmFjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWCwMVUh|ryP MnTwO|IhcA>? M3Lrb2ROW09? NHPwVlhqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 M2rZblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkWzPVY5Lz5{Mk[1N|k3QDxxYU6=
92.1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LubVAuPSEQvF2= NV;kb29pPzJiaB?= M2HqSWROW09? NWLa[XVRcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ3M{m2PEc,OjJ4NUO5Olg9N2F-
Mel202 M3P3UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvDfYc3PSEQvF2= MlrnNlQhcA>? MWjEUXNQ M3vRS4lv\HWlZYOgS|Eh[XK{ZYP0xsA> MonVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4NUO5OlgoRjJ{NkWzPVY5RC:jPh?=
Omm1.3 NW\GVVRLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUG1JO69VQ>? NFuxOm4zPCCq MnjYSG1UVw>? NE\ndJlqdmS3Y3XzJGcyKGG{cnXzeOKh NUH1d2Q2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2OVM6PjhpPkKyOlU{QTZ6PD;hQi=>
92.1 NYnLTHh[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLuW3o2KM7:TR?= NF;rNlUzPCCq NX3YNJNSTE2VTx?= NH7OSWlqdmS3Y3XzJGcyKGG{cnXzeOKh NEDXVms9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[1N|k3QCd-MkK2OVM6Pjh:L3G+
Mel202 NE[xSnBCeG:ydH;zbZMhSXO|YYm= MU[1JO69VQ>? Ml[5O|IhcA>? NWrrfJFxTE2VTx?= NWr5SHRJcW6mdXPld{BieG:ydH;zbZMhe2yrZ3j0cJk> NYjCSWlSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2OVM6PjhpPkKyOlU{QTZ6PD;hQi=>
Omm1.3 NXv3OGNKSXCxcITvd4l{KEG|c3H5 MV21JO69VQ>? MVu3NkBp NWnlPYRwTE2VTx?= M3ryRolv\HWlZYOgZZBweHSxc3nz M4\SNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkWzPVY5Lz5{Mk[1N|k3QDxxYU6=
92.1 NWL6bIFZSXCxcITvd4l{KEG|c3H5 NF\hSFU2KM7:TR?= MnzBO|IhcA>? NF34ZnJFVVOR Ml71bY5lfWOnczDhdI9xfG:|aYOgd4lodmmoY3HueIx6 M13MeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkWzPVY5Lz5{Mk[1N|k3QDxxYU6=
Mel202 Mn3CSpVv[3Srb36gRZN{[Xl? MXO1JO69VQ>? NWHaWo5NOjRiaB?= M4\QeYlvcGmkaYTzJIV5eHKnc4Ppc44h[W6mIIDoc5NxcG:{eXzheIlwdiCxZjDQT2MhcXOxZn;ycZM> M3;JUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkWzPVY5Lz5{Mk[1N|k3QDxxYU6=
Omm1.3 NGGxcHRHfW6ldHnvckBCe3OjeR?= NUT2dINLPSEQvF2= MYKyOEBp M1vYZYlvcGmkaYTzJIV5eHKnc4Ppc44h[W6mIIDoc5NxcG:{eXzheIlwdiCxZjDQT2MhcXOxZn;ycZM> MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ3M{m2PEc,OjJ4NUO5Olg9N2F-
92.1 NF;WOWVHfW6ldHnvckBCe3OjeR?= M4fkOFUh|ryP MVmyOEBp NFLr[JVqdmirYnn0d{BmgHC{ZYPzbY9vKGGwZDDwbI9{eGixconsZZRqd25ib3[gVGtEKGm|b3\vdo1{ NXjzWXB5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2OVM6PjhpPkKyOlU{QTZ6PD;hQi=>
HBL1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PQOFAvOTZvMkCg{txO MUi1JIQ> M3vLUWlEPTB;MD61JO69VQ>? M4DxW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{K0PVIxLz5{MUOyOFkzODxxYU6=
TMD8 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUGwMlE3NTJyIN88US=> NXjaeGlzPSCm NEDUS3hKSzVyPUCuNkDPxE1? MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN{NEmyNEc,OjF|MkS5NlA9N2F-
OCI-Ly10 NFXYOWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLsNE4yPi1{MDFOwG0> NYLsXYNUPSCm MULJR|UxRTFwMzFOwG0> M4DWZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{K0PVIxLz5{MUOyOFkzODxxYU6=
U2932 Ml7zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HNcFAvOTZvMkCg{txO MXW1JIQ> NGDFWWxKSzVyPUGwJO69VQ>? M1G5T|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{K0PVIxLz5{MUOyOFkzODxxYU6=
OCI-Ly3 NIXQcpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYCwMlE3NTJyIN88US=> Ml25OUBl MXjJR|Ux97zgMkCg{txO NH;IblQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUOyOFkzOCd-MkGzNlQ6OjB:L3G+
SuDHL2 NGjLd5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDsWpFqOC5zNj2yNEDPxE1? NEPUe4I2KGR? MoK0TWM2OO,:nkKwJO69VQ>? MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN{NEmyNEc,OjF|MkS5NlA9N2F-
SuDHL4 NF7jR|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7zRZExNjF4LUKwJO69VQ>? NXTXWY5GPSCm M{\ETGlEPTExvK6yNEDPxE1? M4Hvc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{K0PVIxLz5{MUOyOFkzODxxYU6=
DB MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml[yNE4yPi1{MDFOwG0> MYG1JIQ> M3jYNWlEPTExvK6yNEDPxE1? M2[yO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{K0PVIxLz5{MUOyOFkzODxxYU6=
Jurkat IL-2 NHLHRnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjQXo9KSzVyPU[uO|EhyrFiMz63OkDPxE1? MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl2MEK1PUc,OTl7NECyOVk9N2F-
PBMC IL-2 MkG3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTRwOESgxtEhOS55MDCg{txO MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl2MEK1PUc,OTl7NECyOVk9N2F-
Jurkat M2DoS2Z2dmO2aX;uJIF{e2G7 NEDuRWRKdmirYnn0bY9vKG:oIGTDVk9ETDJ6LX3l[IlifGWmIHj1cYFvKFRiY3XscEBi[3SrdnH0bY9vKGmwIFr1dotifCClZXzsd{BmgHC{ZYPzbY5oKGi3bXHuJGlNOiCycn;tc5RmeiCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZktKEmFNUCgQUAxNjB3NDFOwG0v M3j0[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OEK3PFMyLz5zOUiyO|g{OTxxYU6=
Jurkat T MYnGeY5kfGmxbjDhd5NigQ>? NWnnepg1PSCqcoO= NFz0ZXdKdmirYnn0bY9vKG:oIGDLR5Rp\XSjIHnuJIh2dWGwIFr1dotifCCWIHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBidnSrLVPEN{9ETDJ6IHHueIljd2S7LXnu[JVk\WRiVD3j[YxtKGGldHn2ZZRqd25iYomgcYVie3W{aX7nJIRm[3KnYYPlJIlvKEmOLUKgd4VkemW2aX;uJIFnfGW{IEWgbJJ{KGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfUwhUUN3MDC9JFAvODhzIN88UU4> MkLGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhzM{G3NVQoRjJ6MUOxO|E1RC:jPh?=
B-cells MVTGeY5kfGmxbjDhd5NigQ>? NUixWHA4UW6qaXLpeIlwdiCxZjDQT2Nj\XSjIHnuJI1wfXOnIFKgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKEmpTT3zeIlufWyjdHXkJINmdGxicILvcIln\XKjdHnvckwhUUN3MDC9JFAvOjN2IN88UU4> NXHRW5NCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixN|E4OTRpPkK4NVMyPzF2PD;hQi=>
bone marrow cells NFjN[VNCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NXvqXXNFPCCmYYnz NHPIUnBCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JGNDSSCvb4Xz[UBjd26nIH3hdpJwfyClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJHs{UF22aIntbYRqdmViaX7jc5Jxd3KjdHnvckBi\nSncjC0JIRigXNuIFnDOVAhRSB|Lkeg{txONg>? M2C4d|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OEK3PFMyLz5zOUiyO|g{OTxxYU6=

... 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