Sotrastaurin (AEB071)

For research use only.

Catalog No.S2791

55 publications

Sotrastaurin (AEB071) Chemical Structure

CAS No. 425637-18-9

Sotrastaurin (AEB071) is a potent and selective pan-PKC inhibitor, mostly for PKCθ with Ki of 0.22 nM in a cell-free assay; inactive to PKCζ. Phase 2.

Selleck's Sotrastaurin (AEB071) has been cited by 55 publications

Purity & Quality Control

Choose Selective PKC Inhibitors

Biological Activity

Description Sotrastaurin (AEB071) is a potent and selective pan-PKC inhibitor, mostly for PKCθ with Ki of 0.22 nM in a cell-free assay; inactive to PKCζ. Phase 2.
Features Unlike former PKC inhibitors, Sotrastaurin does not enhance apoptosis of murine T-cell blasts in a model of activation-induced cell death.
Targets
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)
In vitro

Sotrastaurin (< 10μM) treatment effectively abrogated at low nanomolar concentration markers of early T-cell activation, such as interleukin-2 secretion and CD25 expression, in primary human and mouse T cells. Sotrastaurin (200 nM) inhibits the CD3/CD28 antibody- and alloantigen-induced T-cell proliferation responses in the absence of nonspecific antiproliferative effects. Sotrastaurin (<3 μM) markedly inhibits lymphocyte function-associated antigen-1-mediated T-cell adhesion. [1] Sotrastaurin(< 20 μM) selectively impair the proliferation of CD79 mutant ABC DLBCL cell lines, correlating with decreased NF-κB signaling avctivity. AEB071 at concentration of 5 μM induces G1 arrest and/or cell death in CD79 mutant cells. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
T cell NY\PcWFmTnWwY4Tpc44hSXO|YYm= NGfBcm8yODBibl2= MoHiN{Bp MmPVSG1UVw>? MkLnbY5pcWKrdIOgdnJPSSC|eX70bIV{cXN? MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTZ7MUG1PEc,OjV4OUGxOVg9N2F-
HUVECs  NGTITFBHfW6ldHnvckBCe3OjeR?= MVi1NFBvVQ>? MUOxJIg> MoHuVoVlfWOnczDEWHguXHKrZ3fldoVlKEWwZH;0bIVtcWGuIFT5d4Z2dmO2aX;u MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTZ|NEWzPEc,OjV4M{S1N|g9N2F-
A549 M2jZemZ2dmO2aX;uJGF{e2G7 Mm\LNE4yyqEQvF2= MlPnNlQhcA>? NFPZUGxl\WO{ZXHz[ZMhfGinIILlcIF1cX[nIGDLR{3PuSCuZY\lcEBwdiClZXzsJI1mdWK{YX7lJINwfHKnYYTl[EBCWy2LVh?= Mk\FQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{MUixOlEoRjJ3MkG4NVYyRC:jPh?=
A549 MVfGeY5kfGmxbjDBd5NigQ>? NHXTcpIxNjIEoN88US=> NHvnWXozPCCq Mn7GdoVlfWOnczD0bIUh\XiycnXzd4lwdiCuZY\lcJMhd2ZiTV3QMVItKE2PUD25JIFv\CCrboTl[5JqdiEQskG= NVHQ[W91RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyNVgyPjFpPkK1NlE5OTZzPD;hQi=>
A549 NUW3W|ZTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrlUZdSOC5zwrFOwG0> NFLIcpQzPCCq M1X5dYVvcGGwY3XzJIdzd3e2aDDpcohq[mm2aX;uJINwfHKnYYTl[EB4cXSqIFHTMWlX NVexXFF[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyNVgyPjFpPkK1NlE5OTZzPD;hQi=>
Mel202 M4SxWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHWPFBQOC53IN88US=> M{\HVVMhcA>? NFjiSnJFVVOR MXHlcohidmOnczDJVk1qdmS3Y3XkJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fS=> MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV7NUO4OUc,OjR3OUWzPFU9N2F-
92.1 NGPLW|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;INE42KM7:TR?= NULPbYFwOyCq MlywSG1UVw>? Mln5[Y5p[W6lZYOgTXIucW6mdXPl[EBz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJk> MojvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3OUWzPFUoRjJ2NUm1N|g2RC:jPh?=
OCM3 NF\h[FJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYmwMlUh|ryP M4L2PFMhcA>? M2D2fWROW09? NECwZ3hmdmijbnPld{BKWi2rbnT1Z4VlKHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gQ>? MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV7NUO4OUc,OjR3OUWzPFU9N2F-
Mel202 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVz3TWJSOC53IN88US=> NFGyUGY{KGh? NHOzVGJFVVOR Mo\tbY5kemWjc3XzJGlTNWmwZIXj[YQh[2WubDDjfYNt\SCjcoLld5TDqA>? Mm\IQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3OUWzPFUoRjJ2NUm1N|g2RC:jPh?=
92.1 Mo\xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXn[nN2OC53IN88US=> NXzKNXlQOyCq MkW0SG1UVw>? NYLvTo5LcW6lcnXhd4V{KEmULXnu[JVk\WRiY3XscEBkgWOuZTDhdpJme3UEoB?= NHjteoo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW5OVM5PSd-MkS1PVU{QDV:L3G+
OCM3 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzCbIFuOC53IN88US=> MWSzJIg> M1z0OWROW09? NXrTeYtucW6lcnXhd4V{KEmULXnu[JVk\WRiY3XscEBkgWOuZTDhdpJme3UEoB?= MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV7NUO4OUc,OjR3OUWzPFU9N2F-
Jeko-1 MkPOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1nYW|AuPCEQvF2= M4\XfGROW09? MXTpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NFS2PVM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2Nlk{PSd-MkSzOlI6OzV:L3G+
Mino NIDzPJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHu0fogxNTRizszN M1i2dWROW09? NVjXfVF6cW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NXrlU4piRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlI6OzVpPkK0N|YzQTN3PD;hQi=>
Rec-1 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV6wMVQh|ryP MXjEUXNQ M17ZNYlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NW\hVXJ4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlI6OzVpPkK0N|YzQTN3PD;hQi=>
SP49 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFS0[JExNTRizszN MkHLSG1UVw>? MmDZbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> Ml3JQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NkK5N|UoRjJ2M{[yPVM2RC:jPh?=
Jeko-1 MoG5SpVv[3Srb36gRZN{[Xl? NUi1eVJbOi53IN88UeKh NIji[GoyOiCq MUDEUXNQ M3jCUoRwf26{ZXf1cIF1\XNiTl[t{tpDKHSjcnfleEBo\W6ncx?= MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4MkmzOUc,OjR|NkK5N|U9N2F-
Mino Mnf2SpVv[3Srb36gRZN{[Xl? M3K0ZVIvPSEQvF5CpC=> NE\sTIoyOiCq NFrjRlRFVVOR NXfzSpYx\G:5boLl[5Vt[XSnczDOSk3PwkJidHHy[4V1KGenbnXz NHfnRmc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2Nlk{PSd-MkSzOlI6OzV:L3G+
Rec-1 MUDGeY5kfGmxbjDBd5NigQ>? NIO4dnUzNjVizszNxsA> NIXKSHIyOiCq MUXEUXNQ Mljq[I94dnKnZ4XsZZRmeyCQRj5OvmIhfGG{Z3X0JIdmdmW| NVHrOlJURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlI6OzVpPkK0N|YzQTN3PD;hQi=>
SP49 NHf2VWFHfW6ldHnvckBCe3OjeR?= M2npRlIvPSEQvF5CpC=> NIXrdYUyOiCq M1zlTGROW09? M3nEXYRwf26{ZXf1cIF1\XNiTl[t{tpDKHSjcnfleEBo\W6ncx?= M3;JflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{[yPVM2Lz5{NEO2Nlk{PTxxYU6=
CD3+ T  M1TzfGZ2dmO2aX;uJGF{e2G7 MYewMVUxOCCwTR?= NUHuXo5[OSCq MnnUbY5pcWKrdIOgUmYu|rqEIIDoc5NxcG:{eXzheIlwdiCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MkjyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3N{OyPFMoRjJ|NUezNlg{RC:jPh?=
Mel202 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHnEW4kxNTVizszN M3ryUVczKGh? MlO0SG1UVw>? M2HXOolvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NH7L[Zc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[1N|k3QCd-MkK2OVM6Pjh:L3G+
Omm1.3 M37GdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUWwMVUh|ryP M3Tmc|czKGh? Mk\USG1UVw>? MYjpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NUH3R25FRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2OVM6PjhpPkKyOlU{QTZ6PD;hQi=>
92.1 M2DGSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LHZ|AuPSEQvF2= M3f6cFczKGh? MVXEUXNQ M13LS4lvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ3M{m2PEc,OjJ4NUO5Olg9N2F-
Mel202 NYX4UFIzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXW1JO69VQ>? MXqyOEBp MYjEUXNQ M1XRR4lv\HWlZYOgS|Eh[XK{ZYP0xsA> M{fZSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkWzPVY5Lz5{Mk[1N|k3QDxxYU6=
Omm1.3 NYXJU5JST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLQOUDPxE1? MmKwNlQhcA>? NFPMS2VFVVOR MVvpcoR2[2W|IFexJIFzemW|dNMg NXvFSHJiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2OVM6PjhpPkKyOlU{QTZ6PD;hQi=>
92.1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVnXUnhnPSEQvF2= NV;DZo01OjRiaB?= M1fHTGROW09? NVj2W4lDcW6mdXPld{BIOSCjcoLld5TDqA>? NELHNHQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[1N|k3QCd-MkK2OVM6Pjh:L3G+
Mel202 NEe3[lhCeG:ydH;zbZMhSXO|YYm= Ml7QOUDPxE1? MWq3NkBp M2DXfmROW09? M{ThTolv\HWlZYOgZZBweHSxc3nzJJNtcWeqdHz5 MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ3M{m2PEc,OjJ4NUO5Olg9N2F-
Omm1.3 NU\oRWZESXCxcITvd4l{KEG|c3H5 MXW1JO69VQ>? NUDKSGJbPzJiaB?= M2XHPWROW09? NHXvdnpqdmS3Y3XzJIFxd3C2b4Ppdy=> NVvpbnV5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2OVM6PjhpPkKyOlU{QTZ6PD;hQi=>
92.1 MX;BdI9xfG:|aYOgRZN{[Xl? NG\HZnk2KM7:TR?= MVe3NkBp MUjEUXNQ NHjpSZFqdmS3Y3XzJIFxd3C2b4Ppd{B{cWewaX\jZY51dHl? MkiyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4NUO5OlgoRjJ{NkWzPVY5RC:jPh?=
Mel202 NW\y[YZ5TnWwY4Tpc44hSXO|YYm= MmjFOUDPxE1? NYXTO|dvOjRiaB?= M2PaeIlvcGmkaYTzJIV5eHKnc4Ppc44h[W6mIIDoc5NxcG:{eXzheIlwdiCxZjDQT2MhcXOxZn;ycZM> MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ3M{m2PEc,OjJ4NUO5Olg9N2F-
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HBL1 NWDzV3hyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXSwMlE3NTJyIN88US=> NX;VNpBoPSCm NInGOnFKSzVyPUCuOUDPxE1? M3LTZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{K0PVIxLz5{MUOyOFkzODxxYU6=
TMD8 M165cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrDcWpQOC5zNj2yNEDPxE1? M{mwUFUh\A>? NWXXcYNlUUN3ME2wMlIh|ryP M335[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{K0PVIxLz5{MUOyOFkzODxxYU6=
OCI-Ly10 NF:1Z3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkDqNE4yPi1{MDFOwG0> M1rKd|Uh\A>? NU[w[2psUUN3ME2xMlMh|ryP NUizSplnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzNlQ6OjBpPkKxN|I1QTJyPD;hQi=>
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SuDHL2 MlvnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjydWQxNjF4LUKwJO69VQ>? NHv3ZXo2KGR? MV7JR|Ux97zgMkCg{txO M3XvSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{K0PVIxLz5{MUOyOFkzODxxYU6=
SuDHL4 NEHNO5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIW3cmYxNjF4LUKwJO69VQ>? M4PVUlUh\A>? MYHJR|Ux97zgMkCg{txO MnzrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|MkS5NlAoRjJzM{K0PVIxRC:jPh?=
DB MlLZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGf1[IsxNjF4LUKwJO69VQ>? M1q0WVUh\A>? NEHnZZZKSzVy78{eNlAh|ryP M3nNOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{K0PVIxLz5{MUOyOFkzODxxYU6=
Jurkat IL-2 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTZwN{GgxtEhOy55NjFOwG0> NXvDVpVNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5OFAzPTlpPkG5PVQxOjV7PD;hQi=>
PBMC IL-2 NFzHSVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTRwOESgxtEhOS55MDCg{txO MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl2MEK1PUc,OTl7NECyOVk9N2F-
Jurkat MkfnSpVv[3Srb36gZZN{[Xl? MXnJcohq[mm2aX;uJI9nKFSFUj;DSFI5NW2nZHnheIVlKGi3bXHuJHQh[2WubDDhZ5RqfmG2aX;uJIlvKEq3cnvheEBk\WyuczDlfJBz\XO|aX7nJIh2dWGwIFnMNkBxem:vb4TldkBjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYmsJGlEPTBiPTCwMlA2PCEQvF2u NVLaR4l[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm4Nlc5OzFpPkG5PFI4QDNzPD;hQi=>
Jurkat T MXTGeY5kfGmxbjDhd5NigQ>? MXu1JIhzew>? NVj1OYs3UW6qaXLpeIlwdiCxZjDQT2N1cGW2YTDpckBpfW2jbjDKeZJs[XRiVDDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4h[W62aT3DSFMwS0R{ODDhcpRq[m:meT3pcoR2[2WmIGStZ4VtdCCjY4TpeoF1cW:wIHL5JI1m[XO3cnnu[{Bl\WO{ZXHz[UBqdiCLTD2yJJNm[3KndHnvckBi\nSncjC1JIhzeyCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZktKEmFNUCgQUAxNjB6MTFOwG0v MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDF|MUexOEc,OjhzM{G3NVQ9N2F-
B-cells M2XKeWZ2dmO2aX;uJIF{e2G7 NYTUcmR7UW6qaXLpeIlwdiCxZjDQT2Nj\XSjIHnuJI1wfXOnIFKgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKEmpTT3zeIlufWyjdHXkJINmdGxicILvcIln\XKjdHnvckwhUUN3MDC9JFAvOjN2IN88UU4> NIjQeWc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEGzNVcyPCd-MkixN|E4OTR:L3G+
bone marrow cells MmrQRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M364NFQh\GG7cx?= M4\WemFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgR2JCKG2xdYPlJIJwdmVibXHydo94KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gX|NJZXSqeX3p[Ilv\SCrbnPvdpBwemG2aX;uJIFnfGW{IESg[IF6eyxiSVO1NEA:KDNwNzFOwG0v NEXERYY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUiyO|g{OSd-MUm4Nlc5OzF:L3G+

... 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
In vivo Sotrastaurin (80 mg/kg) results in significant inhibition of in vivo tumor growth in a subcutaneous TMD8 xenograft model in SCID. [2] Sotrastaurin orally administrated at 10 mg/kg and 30 mg/kg b.i.d. show a dose-dependent immunosuppressive effect leading to pronounced prolongation of heart allograft survival in rats. [3]

Protocol

Animal Research:[3]
- Collapse
  • Animal Models: male Wistar/F rats
  • Dosages: 10 mg/kg and 30 mg/kg
  • Administration: Orally administrated
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 87 mg/mL (198.41 mM)
Water Insoluble
Ethanol '2 mg/mL
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing.
10mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 438.48
Formula

C25H22N6O2

CAS No. 425637-18-9
Storage powder
in solvent
Synonyms N/A
Smiles CN1CCN(CC1)C2=NC3=CC=CC=C3C(=N2)C4=C(C(=O)NC4=O)C5=CNC6=CC=CC=C65

In vivo Formulation Calculator (Clear solution)

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Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

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Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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Molecular Weight Calculator

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

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

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

  • Question 1:

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

  • Answer:

    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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID