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50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 M3zFVGZ2dmO2aX;uJGF{e2G7 MkjLNVAxKG6P MoXNN{Bp MmPKSG1UVw>? MmjjbY5pcWKrdIOgdnJPSSC|eX70bIV{cXN? MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTZ7MUG1PEc,OjV4OUGxOVg9N2F-
HUVECs  M1jNZWZ2dmO2aX;uJGF{e2G7 MYG1NFBvVQ>? MlLrNUBp M4\VT3Jm\HWlZYOgSHRZNVS{aXfn[ZJm\CCHbnTveIhmdGmjbDDEfZNnfW6ldHnvci=> NXvjOGl[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW2N|Q2OzhpPkK1OlM1PTN6PD;hQi=>
A549 M2C0bmZ2dmO2aX;uJGF{e2G7 MXewMlHDqM7:TR?= MV[yOEBp Mnj1[IVkemWjc3XzJJRp\SC{ZXzheIl3\SCSS1Ot{tEhdGW4ZXygc44h[2WubDDt[Y1jemGwZTDjc5Rz\WG2ZXSgRXMuUVZ? MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJzOEG2NUc,OjV{MUixOlE9N2F-
A549 Mk\WSpVv[3Srb36gRZN{[Xl? MX6wMlHDqM7:TR?= M2nBOVI1KGh? MnjqdoVlfWOnczD0bIUh\XiycnXzd4lwdiCuZY\lcJMhd2ZiTV3QMVItKE2PUD25JIFv\CCrboTl[5JqdiEQskG= NXfhVWQxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyNVgyPjFpPkK1NlE5OTZzPD;hQi=>
A549 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3XRXhDOC5zwrFOwG0> NF;ObmgzPCCq NInFTWlmdmijbnPld{Boem:5dHigbY5pcWKrdHnvckBkd3S{ZXH0[YQhf2m2aDDBV{1KXg>? NUTGfmNuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyNVgyPjFpPkK1NlE5OTZzPD;hQi=>
Mel202 M{HUVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPEZ2RwOC53IN88US=> NGL0Xmo{KGh? MknCSG1UVw>? M1zOO4VvcGGwY3XzJGlTNWmwZIXj[YQhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6 MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV7NUO4OUc,OjR3OUWzPFU9N2F-
92.1 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYmwMlUh|ryP NWTVd3dYOyCq MXrEUXNQ NEPy[ZFmdmijbnPld{BKWi2rbnT1Z4VlKHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gQ>? NHjvNIg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW5OVM5PSd-MkS1PVU{QDV:L3G+
OCM3 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;aRYkxNjVizszN Ml7mN{Bp NH3W[4dFVVOR M1HBc4VvcGGwY3XzJGlTNWmwZIXj[YQhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6 NHLz[oE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW5OVM5PSd-MkS1PVU{QDV:L3G+
Mel202 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV[wMlUh|ryP MWKzJIg> M4\4[2ROW09? MUDpcoNz\WG|ZYOgTXIucW6mdXPl[EBk\WyuIHP5Z4xmKGG{cnXzeOKh NVHzXYgyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1PVU{QDVpPkK0OVk2Ozh3PD;hQi=>
92.1 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M36yZlAvPSEQvF2= MmTwN{Bp MWTEUXNQ NEfEUHVqdmO{ZXHz[ZMhUVJvaX7keYNm\CClZXzsJIN6[2ynIHHydoV{fMLi NFuyPYQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW5OVM5PSd-MkS1PVU{QDV:L3G+
OCM3 M4DCWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFy4d|kxNjVizszN MXyzJIg> M17KUGROW09? MU\pcoNz\WG|ZYOgTXIucW6mdXPl[EBk\WyuIHP5Z4xmKGG{cnXzeOKh MmDlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3OUWzPFUoRjJ2NUm1N|g2RC:jPh?=
Jeko-1 M1nleWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\aXXdWOC12IN88US=> M{\NWWROW09? NYT0ZmpKcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? M1PYfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{[yPVM2Lz5{NEO2Nlk{PTxxYU6=
Mino M37QdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnnhNE01KM7:TR?= NHv4T2VFVVOR NETIRndqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4MkmzOUc,OjR|NkK5N|U9N2F-
Rec-1 NXP3N2N5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3r4dFAuPCEQvF2= MXrEUXNQ MmHnbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4MkmzOUc,OjR|NkK5N|U9N2F-
SP49 MmrZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzMc|gxNTRizszN MXnEUXNQ NXTEVnpGcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? M{jSVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{[yPVM2Lz5{NEO2Nlk{PTxxYU6=
Jeko-1 M2rMUmZ2dmO2aX;uJGF{e2G7 MUCyMlUh|ryPwrC= M4i1SlEzKGh? MXPEUXNQ M3:5eIRwf26{ZXf1cIF1\XNiTl[t{tpDKHSjcnfleEBo\W6ncx?= M1rFZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{[yPVM2Lz5{NEO2Nlk{PTxxYU6=
Mino MnTrSpVv[3Srb36gRZN{[Xl? M2LzfVIvPSEQvF5CpC=> NFzV[o8yOiCq M2\CcmROW09? MnHY[I94dnKnZ4XsZZRmeyCQRj5OvmIhfGG{Z3X0JIdmdmW| Moj1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NkK5N|UoRjJ2M{[yPVM2RC:jPh?=
Rec-1 M4rhTWZ2dmO2aX;uJGF{e2G7 M{jIUlIvPSEQvF5CpC=> M3r3cFEzKGh? M1;QeWROW09? M1TSUYRwf26{ZXf1cIF1\XNiTl[t{tpDKHSjcnfleEBo\W6ncx?= MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4MkmzOUc,OjR|NkK5N|U9N2F-
SP49 MUDGeY5kfGmxbjDBd5NigQ>? MUeyMlUh|ryPwrC= NXT1NHU4OTJiaB?= MXXEUXNQ NXjSVZJ[\G:5boLl[5Vt[XSnczDOSk3PwkJidHHy[4V1KGenbnXz NWjjPW14RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlI6OzVpPkK0N|YzQTN3PD;hQi=>
CD3+ T  M{LDfWZ2dmO2aX;uJGF{e2G7 NIfJNWUxNTVyMDDuUS=> M4XGZ|EhcA>? M1;aOIlvcGmkaYTzJG5HNc78QjDwbI9{eGixconsZZRqd25iaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? M2LYdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUezNlg{Lz5{M{W3N|I5OzxxYU6=
Mel202 NIfDS5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3xeo1zOC13IN88US=> NED2VpU4OiCq M4nyeGROW09? M4naVIlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> M2TveFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkWzPVY5Lz5{Mk[1N|k3QDxxYU6=
Omm1.3 NIXZTZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\xb|AuPSEQvF2= M4q1flczKGh? MlLrSG1UVw>? M3u2dIlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ3M{m2PEc,OjJ4NUO5Olg9N2F-
92.1 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVywMVUh|ryP NEP5bHk4OiCq NWDIN4NITE2VTx?= M3u2folvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ3M{m2PEc,OjJ4NUO5Olg9N2F-
Mel202 M1Ty[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWGwTlc1PSEQvF2= NHLSTJkzPCCq M3XXRWROW09? MkPEbY5lfWOnczDHNUBienKnc4VCpC=> NYjIeWNKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2OVM6PjhpPkKyOlU{QTZ6PD;hQi=>
Omm1.3 M3T6cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmroOUDPxE1? MXSyOEBp MkP5SG1UVw>? NEXFblVqdmS3Y3XzJGcyKGG{cnXzeOKh MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ3M{m2PEc,OjJ4NUO5Olg9N2F-
92.1 M{\lZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjxWpQ2KM7:TR?= NGHZfGwzPCCq NEL1PJBFVVOR MmfkbY5lfWOnczDHNUBienKnc4VCpC=> M1uz[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkWzPVY5Lz5{Mk[1N|k3QDxxYU6=
Mel202 NF7vVohCeG:ydH;zbZMhSXO|YYm= Mn\LOUDPxE1? MonJO|IhcA>? MnTuSG1UVw>? M4PERolv\HWlZYOgZZBweHSxc3nzJJNtcWeqdHz5 MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ3M{m2PEc,OjJ4NUO5Olg9N2F-
Omm1.3 MVLBdI9xfG:|aYOgRZN{[Xl? MmTSOUDPxE1? M2n3R|czKGh? M3jwXmROW09? NUnES4pjcW6mdXPld{BieG:ydH;zbZM> MknnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4NUO5OlgoRjJ{NkWzPVY5RC:jPh?=
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Mel202 NEH4c3dHfW6ldHnvckBCe3OjeR?= MY[1JO69VQ>? MUSyOEBp MYPpcohq[mm2czDlfJBz\XO|aX;uJIFv\CCyaH;zdIhwenmuYYTpc44hd2ZiUFvDJIl{d2[xcn3z MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ3M{m2PEc,OjJ4NUO5Olg9N2F-
Omm1.3 NHizNnBHfW6ldHnvckBCe3OjeR?= NXrKepkxPSEQvF2= MXWyOEBp NIr4fY5qdmirYnn0d{BmgHC{ZYPzbY9vKGGwZDDwbI9{eGixconsZZRqd25ib3[gVGtEKGm|b3\vdo1{ NYLsZlZiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2OVM6PjhpPkKyOlU{QTZ6PD;hQi=>
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HBL1 Ml;ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYKwMlE3NTJyIN88US=> NED1UIQ2KGR? MlzLTWM2OD1yLkWg{txO MnToQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|MkS5NlAoRjJzM{K0PVIxRC:jPh?=
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SuDHL2 Ml7aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;ZT|AvOTZvMkCg{txO NX2wc|k5PSCm M2i5bWlEPTExvK6yNEDPxE1? NYT3enBiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzNlQ6OjBpPkKxN|I1QTJyPD;hQi=>
SuDHL4 MlPrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYGwMlE3NTJyIN88US=> MWG1JIQ> NYrOSYpYUUN3MP-8olIxKM7:TR?= MnPsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|MkS5NlAoRjJzM{K0PVIxRC:jPh?=
DB MonFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnf3NE4yPi1{MDFOwG0> MXu1JIQ> NU\pR3FrUUN3MP-8olIxKM7:TR?= MoLnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|MkS5NlAoRjJzM{K0PVIxRC:jPh?=
Jurkat IL-2 M3jLVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{m1OWlEPTB;Nj63NUDDuSB|Lke2JO69VQ>? NWK5WGY3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5OFAzPTlpPkG5PVQxOjV7PD;hQi=>
PBMC IL-2 M1jYVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jmT2lEPTB;ND64OEDDuSBzLkewJEDPxE1? MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl2MEK1PUc,OTl7NECyOVk9N2F-
Jurkat NUXvXnZNTnWwY4Tpc44h[XO|YYm= M3fiUWlvcGmkaYTpc44hd2ZiVFPSM2NFOjhvbXXkbYF1\WRiaIXtZY4hXCClZXzsJIFkfGm4YYTpc44hcW5iSoXyb4F1KGOnbHzzJIV5eHKnc4PpcochcHWvYX6gTWwzKHC{b33veIVzKGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfUwhUUN3MDC9JFAvODV2IN88UU4> M{fidFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OEK3PFMyLz5zOUiyO|g{OTxxYU6=
Jurkat T NX3HNolsTnWwY4Tpc44h[XO|YYm= MX61JIhzew>? M4nOS2lvcGmkaYTpc44hd2ZiUFvDeIhmfGFiaX6gbJVu[W5iSoXyb4F1KFRiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJIFvfGlvQ1SzM2NFOjhiYX70bYJw\HlvaX7keYNm\CCWLXPlcIwh[WO2aY\heIlwdiCkeTDt[YF{fXKrbneg[IVkemWjc3WgbY4hUUxvMjDz[YNz\XSrb36gZYZ1\XJiNTDodpMh[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5MEBKSzVyIE2gNE4xQDFizszNMi=> NYjaZoxGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixN|E4OTRpPkK4NVMyPzF2PD;hQi=>
B-cells M4\HZmZ2dmO2aX;uJIF{e2G7 NVjh[Y9uUW6qaXLpeIlwdiCxZjDQT2Nj\XSjIHnuJI1wfXOnIFKgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKEmpTT3zeIlufWyjdHXkJINmdGxicILvcIln\XKjdHnvckwhUUN3MDC9JFAvOjN2IN88UU4> M33kNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MUOxO|E1Lz5{OEGzNVcyPDxxYU6=
bone marrow cells NXvNfWJVSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M3XWelQh\GG7cx?= Mo[zRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDDRmEhdW:3c3WgZo9v\SCvYYLyc5ch[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDbN2hefGi7bXnkbY5mKGmwY3;ydI9z[XSrb36gZYZ1\XJiNDDkZZl{NCCLQ{WwJF0hOy55IN88UU4> MlfjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl6Mke4N|EoRjF7OEK3PFMyRC:jPh?=

... 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
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.

PKC Signaling Pathway Map

PKC Inhibitors with Unique Features

相关PKC产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID