Sotrastaurin

For research use only.

Catalog No.S2791 Synonyms: AEB071

49 publications

Sotrastaurin 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.

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Selleck's Sotrastaurin has been cited by 49 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 NWnWdFJPTnWwY4Tpc44hSXO|YYm= M1fCdlExOCCwTR?= MWWzJIg> MlzhSG1UVw>? MWLpcohq[mm2czDyVm5CKHO7boTo[ZNqew>? M3jhS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NkmxNVU5Lz5{NU[5NVE2QDxxYU6=
HUVECs  Mlu2SpVv[3Srb36gRZN{[Xl? MkHLOVAxdk1? NFHXZpAyKGh? NEW1PI9T\WS3Y3XzJGRVYC2Wcnnn[4Vz\WRiRX7kc5Rp\WyrYXygSJl{\nWwY4Tpc44> M4nvRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NkO0OVM5Lz5{NU[zOFU{QDxxYU6=
A549 MoX1SpVv[3Srb36gRZN{[Xl? NEnSN|ExNjIEoN88US=> M4G2clI1KGh? M4fI[IRm[3KnYYPld{B1cGVicnXsZZRqfmViUFvDMe6yKGyndnXsJI9vKGOnbHygcYVu[nKjbnWgZ491emWjdHXkJGFUNUmY NHnzN5Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKxPFE3OSd-MkWyNVgyPjF:L3G+
A549 MWfGeY5kfGmxbjDBd5NigQ>? M4jqZlAvOcLizszN NGDRW4szPCCq Mm\UdoVlfWOnczD0bIUh\XiycnXzd4lwdiCuZY\lcJMhd2ZiTV3QMVItKE2PUD25JIFv\CCrboTl[5JqdiEQskG= MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJzOEG2NUc,OjV{MUixOlE9N2F-
A549 MoW1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4PyXFAvOcLizszN M4C1cFI1KGh? NFy3R49mdmijbnPld{Boem:5dHigbY5pcWKrdHnvckBkd3S{ZXH0[YQhf2m2aDDBV{1KXg>? MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJzOEG2NUc,OjV{MUixOlE9N2F-
Mel202 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYmwMlUh|ryP MYWzJIg> NH3Le3BFVVOR MV3lcohidmOnczDJVk1qdmS3Y3XkJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fS=> MmrkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3OUWzPFUoRjJ2NUm1N|g2RC:jPh?=
92.1 MlH2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY[wMlUh|ryP NI\xXlI{KGh? MkW0SG1UVw>? NUjLUFFp\W6qYX7j[ZMhUVJvaX7keYNm\CC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHl? MoHmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3OUWzPFUoRjJ2NUm1N|g2RC:jPh?=
OCM3 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfpNE42KM7:TR?= MkDqN{Bp MV;EUXNQ M1LLXoVvcGGwY3XzJGlTNWmwZIXj[YQhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6 MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV7NUO4OUc,OjR3OUWzPFU9N2F-
Mel202 NF;Sd2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\HNE42KM7:TR?= MmDKN{Bp NYPodWRITE2VTx?= MVrpcoNz\WG|ZYOgTXIucW6mdXPl[EBk\WyuIHP5Z4xmKGG{cnXzeOKh NHmzSnU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW5OVM5PSd-MkS1PVU{QDV:L3G+
92.1 M4LUdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LvW|AvPSEQvF2= NYT0R|FjOyCq NFvMfXlFVVOR M3jRb4lv[3KnYYPld{BKWi2rbnT1Z4VlKGOnbHygZ5lkdGViYYLy[ZN1yqB? MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV7NUO4OUc,OjR3OUWzPFU9N2F-
OCM3 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnfoNE42KM7:TR?= NFvIOpg{KGh? NVPrc|N2TE2VTx?= NGOzdIdqdmO{ZXHz[ZMhUVJvaX7keYNm\CClZXzsJIN6[2ynIHHydoV{fMLi NI\aZXM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW5OVM5PSd-MkS1PVU{QDV:L3G+
Jeko-1 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjaNE01KM7:TR?= NXH0T5BMTE2VTx?= NXLDTIl{cW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NE\qWJo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2Nlk{PSd-MkSzOlI6OzV:L3G+
Mino M1;GOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3tVIoxNTRizszN NFHMTHhFVVOR NVLBRWxvcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? Mm\UQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NkK5N|UoRjJ2M{[yPVM2RC:jPh?=
Rec-1 MmH3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7ITFAxNTRizszN M2ToWWROW09? NIHGUWRqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4MkmzOUc,OjR|NkK5N|U9N2F-
SP49 MmPPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUiwMVQh|ryP MoHlSG1UVw>? M2\NXolvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> MkPLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NkK5N|UoRjJ2M{[yPVM2RC:jPh?=
Jeko-1 NXG1NIJjTnWwY4Tpc44hSXO|YYm= MnXRNk42KM7:TdMg NHu5Z3oyOiCq NIT4UG9FVVOR MVXkc5dvemWpdXzheIV{KE6ILd86RkB1[XKpZYSg[4Vv\XN? NILkdVk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2Nlk{PSd-MkSzOlI6OzV:L3G+
Mino M2DSTGZ2dmO2aX;uJGF{e2G7 NGq2XZAzNjVizszNxsA> NX7sVm9NOTJiaB?= MYLEUXNQ MXfkc5dvemWpdXzheIV{KE6ILd86RkB1[XKpZYSg[4Vv\XN? NHLsbpc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2Nlk{PSd-MkSzOlI6OzV:L3G+
Rec-1 NWrQNYpuTnWwY4Tpc44hSXO|YYm= M2fBRlIvPSEQvF5CpC=> MojTNVIhcA>? NHjvU5VFVVOR MkHZ[I94dnKnZ4XsZZRmeyCQRj5OvmIhfGG{Z3X0JIdmdmW| NYPaOmlwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlI6OzVpPkK0N|YzQTN3PD;hQi=>
SP49 M1jRNmZ2dmO2aX;uJGF{e2G7 NIDFdFMzNjVizszNxsA> NFXoTnkyOiCq M{jKS2ROW09? MYHkc5dvemWpdXzheIV{KE6ILd86RkB1[XKpZYSg[4Vv\XN? NIHJUGE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2Nlk{PSd-MkSzOlI6OzV:L3G+
CD3+ T  M2jKUWZ2dmO2aX;uJGF{e2G7 M{TLfVAuPTByIH7N MXSxJIg> NEPUNXBqdmirYnn0d{BPTi4QulKgdIhwe3Cqb4L5cIF1cW:wIHnuJIEh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzV5M{K4N{c,OjN3N{OyPFM9N2F-
Mel202 NWrIPFdET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVWwMVUh|ryP Ml;KO|IhcA>? NU[zeIYxTE2VTx?= MlfsbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NWXvdmRZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2OVM6PjhpPkKyOlU{QTZ6PD;hQi=>
Omm1.3 NGXoWIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fSUlAuPSEQvF2= M3fJ[|czKGh? NWjEVXRETE2VTx?= NVTTcGR4cW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ3M{m2PEc,OjJ4NUO5Olg9N2F-
92.1 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXewMVUh|ryP NHywO4g4OiCq NUPwd5pyTE2VTx?= MlfGbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MmC3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4NUO5OlgoRjJ{NkWzPVY5RC:jPh?=
Mel202 NInqbZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4frfFUh|ryP NY\kb|F7OjRiaB?= NGfE[GtFVVOR M1nEXYlv\HWlZYOgS|Eh[XK{ZYP0xsA> MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ3M{m2PEc,OjJ4NUO5Olg9N2F-
Omm1.3 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUi1JO69VQ>? M3PzV|I1KGh? NVT1[m5DTE2VTx?= NFSxUI5qdmS3Y3XzJGcyKGG{cnXzeOKh M{XORVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkWzPVY5Lz5{Mk[1N|k3QDxxYU6=
92.1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\yUlUh|ryP NFLtNGczPCCq NVyxVXNyTE2VTx?= NFGzVo5qdmS3Y3XzJGcyKGG{cnXzeOKh MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ3M{m2PEc,OjJ4NUO5Olg9N2F-
Mel202 NFnFRppCeG:ydH;zbZMhSXO|YYm= NHnQXpM2KM7:TR?= NUPzNnBIPzJiaB?= MUfEUXNQ NU\uWYxmcW6mdXPld{BieG:ydH;zbZMhe2yrZ3j0cJk> MkO5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4NUO5OlgoRjJ{NkWzPVY5RC:jPh?=
Omm1.3 NYr6ZYV3SXCxcITvd4l{KEG|c3H5 Mo\jOUDPxE1? NEjQO2Q4OiCq M37sOWROW09? Mn;5bY5lfWOnczDhdI9xfG:|aYO= NYLpPGZrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2OVM6PjhpPkKyOlU{QTZ6PD;hQi=>
92.1 MWXBdI9xfG:|aYOgRZN{[Xl? NXrWbpFsPSEQvF2= MmjFO|IhcA>? MYjEUXNQ MVPpcoR2[2W|IHHwc5B1d3OrczDzbYdvcW[lYX70cJk> MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ3M{m2PEc,OjJ4NUO5Olg9N2F-
Mel202 NEHkRVBHfW6ldHnvckBCe3OjeR?= MVm1JO69VQ>? NV7IeXpEOjRiaB?= NGXi[lVqdmirYnn0d{BmgHC{ZYPzbY9vKGGwZDDwbI9{eGixconsZZRqd25ib3[gVGtEKGm|b3\vdo1{ M2Xsd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkWzPVY5Lz5{Mk[1N|k3QDxxYU6=
Omm1.3 NFTLTY1HfW6ldHnvckBCe3OjeR?= NVnyWY1iPSEQvF2= NHTzdm8zPCCq NXPsVVlLcW6qaXLpeJMh\XiycnXzd4lwdiCjbnSgdIhwe3Cqb4L5cIF1cW:wIH;mJHBMSyCrc3;mc5Juew>? MlntQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4NUO5OlgoRjJ{NkWzPVY5RC:jPh?=
92.1 NULGOpNSTnWwY4Tpc44hSXO|YYm= MonoOUDPxE1? NIi1WHIzPCCq M2HSUIlvcGmkaYTzJIV5eHKnc4Ppc44h[W6mIIDoc5NxcG:{eXzheIlwdiCxZjDQT2MhcXOxZn;ycZM> Mle2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4NUO5OlgoRjJ{NkWzPVY5RC:jPh?=
HBL1 NVXLW|FiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYewMlE3NTJyIN88US=> NIXQcIw2KGR? M4npVmlEPTB;MD61JO69VQ>? M3rlS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{K0PVIxLz5{MUOyOFkzODxxYU6=
TMD8 NUPZUpJuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXe3NndnOC5zNj2yNEDPxE1? MkThOUBl NFHBe2lKSzVyPUCuNkDPxE1? MnPsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|MkS5NlAoRjJzM{K0PVIxRC:jPh?=
OCI-Ly10 MkHYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF72WGkxNjF4LUKwJO69VQ>? M1naZlUh\A>? NIjOSoJKSzVyPUGuN{DPxE1? NUTaUIttRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzNlQ6OjBpPkKxN|I1QTJyPD;hQi=>
U2932 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWKwMlE3NTJyIN88US=> MWi1JIQ> MXvJR|UxRTFyIN88US=> MkHPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|MkS5NlAoRjJzM{K0PVIxRC:jPh?=
OCI-Ly3 NIHBVJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4jZN|AvOTZvMkCg{txO NVe4XFl4PSCm NIDKeY9KSzVy78{eNlAh|ryP MkHzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|MkS5NlAoRjJzM{K0PVIxRC:jPh?=
SuDHL2 NFPHcpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfoflU4OC5zNj2yNEDPxE1? MmTkOUBl NX3SNWhCUUN3MP-8olIxKM7:TR?= MlHMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|MkS5NlAoRjJzM{K0PVIxRC:jPh?=
SuDHL4 MnLzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLPNE4yPi1{MDFOwG0> Ml:4OUBl NIfRZ2RKSzVy78{eNlAh|ryP NGLmUIE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUOyOFkzOCd-MkGzNlQ6OjB:L3G+
DB MoXYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;ZelAvOTZvMkCg{txO MXq1JIQ> M3jhUGlEPTExvK6yNEDPxE1? M{LveFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{K0PVIxLz5{MUOyOFkzODxxYU6=
Jurkat IL-2 NUnmbWM6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NETRc21KSzVyPU[uO|EhyrFiMz63OkDPxE1? Mmi0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7NECyOVkoRjF7OUSwNlU6RC:jPh?=
PBMC IL-2 M3vuUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjxTWM2OD12Lki0JOKyKDFwN{CgJO69VQ>? MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl2MEK1PUc,OTl7NECyOVk9N2F-
Jurkat MX3GeY5kfGmxbjDhd5NigQ>? MUjJcohq[mm2aX;uJI9nKFSFUj;DSFI5NW2nZHnheIVlKGi3bXHuJHQh[2WubDDhZ5RqfmG2aX;uJIlvKEq3cnvheEBk\WyuczDlfJBz\XO|aX7nJIh2dWGwIFnMNkBxem:vb4TldkBjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYmsJGlEPTBiPTCwMlA2PCEQvF2u M1L3elxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OEK3PFMyLz5zOUiyO|g{OTxxYU6=
Jurkat T NFfmTVZHfW6ldHnvckBie3OjeR?= MojtOUBpenN? NIG1cYlKdmirYnn0bY9vKG:oIGDLR5Rp\XSjIHnuJIh2dWGwIFr1dotifCCWIHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBidnSrLVPEN{9ETDJ6IHHueIljd2S7LXnu[JVk\WRiVD3j[YxtKGGldHn2ZZRqd25iYomgcYVie3W{aX7nJIRm[3KnYYPlJIlvKEmOLUKgd4VkemW2aX;uJIFnfGW{IEWgbJJ{KGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfUwhUUN3MDC9JFAvODhzIN88UU4> NF3nVHQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEGzNVcyPCd-MkixN|E4OTR:L3G+
B-cells MVvGeY5kfGmxbjDhd5NigQ>? M13RZWlvcGmkaYTpc44hd2ZiUFvDZoV1[SCrbjDtc5V{\SCEIHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBK\01vc4TpcZVt[XSnZDDj[YxtKHC{b3zp[oVz[XSrb36sJGlEPTBiPTCwMlI{PCEQvF2u NGKxT|A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEGzNVcyPCd-MkixN|E4OTR:L3G+
bone marrow cells NGHqcVhCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M2mwTVQh\GG7cx?= MkXZRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDDRmEhdW:3c3WgZo9v\SCvYYLyc5ch[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDbN2hefGi7bXnkbY5mKGmwY3;ydI9z[XSrb36gZYZ1\XJiNDDkZZl{NCCLQ{WwJF0hOy55IN88UU4> M132NlxiKHSjcnfleF0oZ2KuYX7rK{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
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)
Ethanol 2 mg/mL (4.56 mM)
Water Insoluble
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 AEB071
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)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Step 2: Enter the in vivo formulation ()
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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 MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

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

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

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  • Computed Result

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    C2=C1/X C2: LOG(C2):
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Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

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)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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

If you have any other enquiries, please leave a message.

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID