Sotrastaurin

For research use only. Not for use in humans.

目录号：S2791 别名： AEB071

Sotrastaurin 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发表文献48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 M2PsW2Z2dmO2aX;uJGF{e2G7 MkLKNVAxKG6P NVzrRm1oOyCq Mn20SG1UVw>? NUHPXWpkcW6qaXLpeJMhelKQQTDzfY51cGW|aYO= NHzEbIo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NU[5NVE2QCd-MkW2PVEyPTh:L3G+
HUVECs  NFnJN4NHfW6ldHnvckBCe3OjeR?= NYXaUlNjPTBybl2= MXmxJIg> MYTS[YR2[2W|IFTUXE1VemmpZ3Xy[YQhTW6mb4To[Yxq[WxiRInz[pVv[3Srb36= NX7udVBNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW2N|Q2OzhpPkK1OlM1PTN6PD;hQi=>
A549 M{TSPGZ2dmO2aX;uJGF{e2G7 M1rCdFAvOcLizszN M{m3VlI1KGh? NV;vbGt[\GWlcnXhd4V{KHSqZTDy[YxifGm4ZTDQT2Mu|rFibHX2[Ywhd25iY3XscEBu\W2kcnHu[UBkd3S{ZXH0[YQhSVNvSW[= NXLRZY02RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyNVgyPjFpPkK1NlE5OTZzPD;hQi=>
A549 NVvkT41VTnWwY4Tpc44hSXO|YYm= MX2wMlHDqM7:TR?= M2PvdlI1KGh? NYnlV4tjemWmdXPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdHNib3[gUW1RNTJuIF3NVE06KGGwZDDpcpRm\3KrbjFOtlE> MkPyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{MUixOlEoRjJ3MkG4NVYyRC:jPh?=
A549 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHmc2h1OC5zwrFOwG0> NW\RWVU{OjRiaB?= NHvLTXFmdmijbnPld{Boem:5dHigbY5pcWKrdHnvckBkd3S{ZXH0[YQhf2m2aDDBV{1KXg>? MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJzOEG2NUc,OjV{MUixOlE9N2F-
Mel202 NGTBeWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1Tpb|AvPSEQvF2= NV76UnhWOyCq M1PKfmROW09? M1K5OIVvcGGwY3XzJGlTNWmwZIXj[YQhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6 NGXDfFE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW5OVM5PSd-MkS1PVU{QDV:L3G+
92.1 M2L3PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTKZnVSOC53IN88US=> MXyzJIg> NXX5dJc{TE2VTx?= M1vreYVvcGGwY3XzJGlTNWmwZIXj[YQhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6 MmTnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3OUWzPFUoRjJ2NUm1N|g2RC:jPh?=
OCM3 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmmzNE42KM7:TR?= MVmzJIg> MUHEUXNQ NXvsPXJn\W6qYX7j[ZMhUVJvaX7keYNm\CC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHl? NF\Uem89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW5OVM5PSd-MkS1PVU{QDV:L3G+
Mel202 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnsS28xNjVizszN MVuzJIg> MnfuSG1UVw>? NH7BfIpqdmO{ZXHz[ZMhUVJvaX7keYNm\CClZXzsJIN6[2ynIHHydoV{fMLi M3HFdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NUm1N|g2Lz5{NEW5OVM5PTxxYU6=
92.1 M3nFUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3:0[|AvPSEQvF2= NVPDN3JjOyCq NYq3TYVWTE2VTx?= M3jNb4lv[3KnYYPld{BKWi2rbnT1Z4VlKGOnbHygZ5lkdGViYYLy[ZN1yqB? NF:5UnA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW5OVM5PSd-MkS1PVU{QDV:L3G+
OCM3 NH;NVXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\P[|AvPSEQvF2= NWPvOFY1OyCq M{LaZWROW09? MUTpcoNz\WG|ZYOgTXIucW6mdXPl[EBk\WyuIHP5Z4xmKGG{cnXzeOKh NGTiU4g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW5OVM5PSd-MkS1PVU{QDV:L3G+
Jeko-1 NUCxTXdVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoS3NE01KM7:TR?= NH;rdGpFVVOR MUnpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4MkmzOUc,OjR|NkK5N|U9N2F-
Mino MknlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjyOnQxNTRizszN NI\O[IhFVVOR Mkn3bY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NVr1RnV7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlI6OzVpPkK0N|YzQTN3PD;hQi=>
Rec-1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDQR4VROC12IN88US=> MmK4SG1UVw>? M2q4UolvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4MkmzOUc,OjR|NkK5N|U9N2F-
SP49 NH\1eHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHaWWoxNTRizszN NUHWO5dRTE2VTx?= M{LMNolvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> M3i1e|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{[yPVM2Lz5{NEO2Nlk{PTxxYU6=
Jeko-1 MmfrSpVv[3Srb36gRZN{[Xl? M{TPeVIvPSEQvF5CpC=> M4HxXlEzKGh? MUfEUXNQ MY\kc5dvemWpdXzheIV{KE6ILd86RkB1[XKpZYSg[4Vv\XN? M{LIVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{[yPVM2Lz5{NEO2Nlk{PTxxYU6=
Mino MXzGeY5kfGmxbjDBd5NigQ>? MWSyMlUh|ryPwrC= MVSxNkBp MXjEUXNQ NVzVd|k3\G:5boLl[5Vt[XSnczDOSk3PwkJidHHy[4V1KGenbnXz M{O5U|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{[yPVM2Lz5{NEO2Nlk{PTxxYU6=
Rec-1 NXnrU5NvTnWwY4Tpc44hSXO|YYm= NX\GOXdkOi53IN88UeKh NF\yTlcyOiCq NHTkO4hFVVOR MYDkc5dvemWpdXzheIV{KE6ILd86RkB1[XKpZYSg[4Vv\XN? NHTuN5M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2Nlk{PSd-MkSzOlI6OzV:L3G+
SP49 NILMUZBHfW6ldHnvckBCe3OjeR?= NXTZdZd5Oi53IN88UeKh MYSxNkBp M13tTmROW09? M4XCVoRwf26{ZXf1cIF1\XNiTl[t{tpDKHSjcnfleEBo\W6ncx?= MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4MkmzOUc,OjR|NkK5N|U9N2F-
CD3+ T  MYLGeY5kfGmxbjDBd5NigQ>? NI\6V5oxNTVyMDDuUS=> NFTqRYUyKGh? MmDjbY5pcWKrdIOgUmYu|rqEIIDoc5NxcG:{eXzheIlwdiCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NIOyXnc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{W3N|I5Oyd-MkO1O|MzQDN:L3G+
Mel202 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkC1NE02KM7:TR?= M{XBO|czKGh? Mlf3SG1UVw>? Ml;YbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NWSzTYhXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2OVM6PjhpPkKyOlU{QTZ6PD;hQi=>
Omm1.3 M4Lye2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LpXVAuPSEQvF2= M3\CcVczKGh? MWjEUXNQ M2OzZ4lvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NVz1dnY6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2OVM6PjhpPkKyOlU{QTZ6PD;hQi=>
92.1 NEHZPZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYqwMVUh|ryP NH21WJM4OiCq MX3EUXNQ MUfpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NIDzflY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[1N|k3QCd-MkK2OVM6Pjh:L3G+
Mel202 MmnUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXO1JO69VQ>? MWOyOEBp Mo\MSG1UVw>? NEjxbldqdmS3Y3XzJGcyKGG{cnXzeOKh NGLkNHk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[1N|k3QCd-MkK2OVM6Pjh:L3G+
Omm1.3 M37NTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1THS|Uh|ryP NH3QfVMzPCCq NFnsR2lFVVOR NH\RbldqdmS3Y3XzJGcyKGG{cnXzeOKh NUD1NHN5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2OVM6PjhpPkKyOlU{QTZ6PD;hQi=>
92.1 MmLsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUO1JO69VQ>? MofxNlQhcA>? NF63WGRFVVOR MmnObY5lfWOnczDHNUBienKnc4VCpC=> NWXUR5ppRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2OVM6PjhpPkKyOlU{QTZ6PD;hQi=>
Mel202 NETYVopCeG:ydH;zbZMhSXO|YYm= NWPXTnluPSEQvF2= NF[0U4Q4OiCq MlvBSG1UVw>? MXjpcoR2[2W|IHHwc5B1d3OrczDzcIlocHSueR?= Mlv4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4NUO5OlgoRjJ{NkWzPVY5RC:jPh?=
Omm1.3 M1jzS2Fxd3C2b4Ppd{BCe3OjeR?= NXfmWYJwPSEQvF2= MXS3NkBp NVvXN21[TE2VTx?= MlL0bY5lfWOnczDhdI9xfG:|aYO= M2nSRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkWzPVY5Lz5{Mk[1N|k3QDxxYU6=
92.1 MnviRZBweHSxc3nzJGF{e2G7 NWHSOXo2PSEQvF2= NUDO[41oPzJiaB?= NFnQU2ZFVVOR M4WzPYlv\HWlZYOgZZBweHSxc3nzJJNq\26rZnPhcpRtgQ>? NWf4c3hSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2OVM6PjhpPkKyOlU{QTZ6PD;hQi=>
Mel202 NVXJWpRQTnWwY4Tpc44hSXO|YYm= NVrPR3A6PSEQvF2= NGXmcmszPCCq MW\pcohq[mm2czDlfJBz\XO|aX;uJIFv\CCyaH;zdIhwenmuYYTpc44hd2ZiUFvDJIl{d2[xcn3z MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ3M{m2PEc,OjJ4NUO5Olg9N2F-
Omm1.3 MX3GeY5kfGmxbjDBd5NigQ>? MWq1JO69VQ>? NF[3ZlAzPCCq MlXxbY5pcWKrdIOg[ZhxemW|c3nvckBidmRicHjvd5Bpd3K7bHH0bY9vKG:oIGDLR{Bqe2:ob4Ltdy=> NFjad2k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[1N|k3QCd-MkK2OVM6Pjh:L3G+
92.1 M4DWSmZ2dmO2aX;uJGF{e2G7 NYPZTolEPSEQvF2= NUjLS2ZYOjRiaB?= M2PrWYlvcGmkaYTzJIV5eHKnc4Ppc44h[W6mIIDoc5NxcG:{eXzheIlwdiCxZjDQT2MhcXOxZn;ycZM> NXj6cY9vRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2OVM6PjhpPkKyOlU{QTZ6PD;hQi=>
HBL1 NGLXeoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\jd4FCOC5zNj2yNEDPxE1? NI\tdlE2KGR? NXjlenY3UUN3ME2wMlUh|ryP NY\Tb3huRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzNlQ6OjBpPkKxN|I1QTJyPD;hQi=>
TMD8 Ml3iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHCNE4yPi1{MDFOwG0> NYDHcVhwPSCm MlPpTWM2OD1yLkKg{txO NVrIR|ZiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzNlQ6OjBpPkKxN|I1QTJyPD;hQi=>
OCI-Ly10 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjZVlJTOC5zNj2yNEDPxE1? M2fOTFUh\A>? NIf6PIVKSzVyPUGuN{DPxE1? NVS5SXl2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzNlQ6OjBpPkKxN|I1QTJyPD;hQi=>
U2932 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1vOWVAvOTZvMkCg{txO NUT2XYdkPSCm M1LnTWlEPTB;MUCg{txO MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN{NEmyNEc,OjF|MkS5NlA9N2F-
OCI-Ly3 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXSwMlE3NTJyIN88US=> Mn22OUBl M{TUV2lEPTExvK6yNEDPxE1? NWrYWIdPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzNlQ6OjBpPkKxN|I1QTJyPD;hQi=>
SuDHL2 M{PaW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoOzNE4yPi1{MDFOwG0> M1PZUlUh\A>? MmTGTWM2OO,:nkKwJO69VQ>? MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN{NEmyNEc,OjF|MkS5NlA9N2F-
SuDHL4 NFfwfI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVmwMlE3NTJyIN88US=> NVexe4ZYPSCm MV\JR|Ux97zgMkCg{txO NIP0NWk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUOyOFkzOCd-MkGzNlQ6OjB:L3G+
DB M4\aT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1O1NFAvOTZvMkCg{txO NF7qO|E2KGR? NXzQco9OUUN3MP-8olIxKM7:TR?= MlrXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|MkS5NlAoRjJzM{K0PVIxRC:jPh?=
Jurkat IL-2 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILlOWtKSzVyPU[uO|EhyrFiMz63OkDPxE1? NVmxdohFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5OFAzPTlpPkG5PVQxOjV7PD;hQi=>
PBMC IL-2 MnXlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvTTWM2OD12Lki0JOKyKDFwN{CgJO69VQ>? NIP1[mU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm0NFI2QSd-MUm5OFAzPTl:L3G+
Jurkat NYjmO2FiTnWwY4Tpc44h[XO|YYm= NUKxNIh[UW6qaXLpeIlwdiCxZjDUR3IwS0R{OD3t[YRq[XSnZDDoeY1idiCWIHPlcIwh[WO2aY\heIlwdiCrbjDKeZJs[XRiY3XscJMh\XiycnXzd4lv\yCqdX3hckBKVDJicILvcY91\XJiYomgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6NCCLQ{WwJF0hOC5yNUSg{txONg>? MknQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl6Mke4N|EoRjF7OEK3PFMyRC:jPh?=
Jurkat T M3KzfWZ2dmO2aX;uJIF{e2G7 M{mzUlUhcHK| NHXUeY9KdmirYnn0bY9vKG:oIGDLR5Rp\XSjIHnuJIh2dWGwIFr1dotifCCWIHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBidnSrLVPEN{9ETDJ6IHHueIljd2S7LXnu[JVk\WRiVD3j[YxtKGGldHn2ZZRqd25iYomgcYVie3W{aX7nJIRm[3KnYYPlJIlvKEmOLUKgd4VkemW2aX;uJIFnfGW{IEWgbJJ{KGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfUwhUUN3MDC9JFAvODhzIN88UU4> MnixQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhzM{G3NVQoRjJ6MUOxO|E1RC:jPh?=
B-cells M2TxdmZ2dmO2aX;uJIF{e2G7 MXfJcohq[mm2aX;uJI9nKFCNQ3LleIEhcW5ibX;1d4UhSiClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gTYdONXO2aX31cIF1\WRiY3XscEBxem:uaX\ldoF1cW:wLDDJR|UxKD1iMD6yN|Qh|ryPLh?= MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDF|MUexOEc,OjhzM{G3NVQ9N2F-
bone marrow cells NECyc2JCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NXrIelFzPCCmYYnz M174dWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgR2JCKG2xdYPlJIJwdmVibXHydo94KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gX|NJZXSqeX3p[Ilv\SCrbnPvdpBwemG2aX;uJIFnfGW{IESg[IF6eyxiSVO1NEA:KDNwNzFOwG0v NUHJOJkyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm4Nlc5OzFpPkG5PFI4QDNzPD;hQi=>

... 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)
Ethanol 2 mg/mL (4.56 mM)
Water 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)：
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 AEB071

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、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
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.

  • 最新的PKC抑制剂

    Ro 31-8220 Mesylate New : Pan-PKC inhibitor with IC50 of 5 nM, 24 nM, 14 nM, 27 nM, and 24 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, and PKC-ε, respectively, and also shows potent inhibition against MAPKAP-K1b, MSK1, GSK3β and S6K1.

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。

  • LDN-214117 New

    LDN-214117是一种有效的选择性 BMP I型受体激酶 ALK2 抑制剂，IC50为 24 nM。

  • Staurosporine

    Staurosporine (CGP 41251) 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)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。

  • Bisindolylmaleimide IX (Ro 31-8220 Mesylate)

    Bisindolylmaleimide IX (Ro 31-8220 Mesylate)是一种pan-PKC抑制剂，作用于PKC-α， PKC-βI， PKC-βII， PKC-γ和PKC-ε，IC50分别为5 nM， 24 nM， 14 nM， 27 nM和24 nM，也有效抑制MAPKAP-K1b， MSK1， GSK3β和S6K1。

  • 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