Sotrastaurin (AEB071)

Catalog No.S2791

For research use only.

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.

Sotrastaurin (AEB071) Chemical Structure

CAS No. 425637-18-9

Selleck's Sotrastaurin (AEB071) has been cited by 60 publications

Purity & Quality Control

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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)
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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 NVXp[HJLTnWwY4Tpc44hSXO|YYm= MYixNFAhdk1? Mk\DN{Bp Mn;sSG1UVw>? MkjDbY5pcWKrdIOgdnJPSSC|eX70bIV{cXN? MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTZ7MUG1PEc,OjV4OUGxOVg9N2F-
HUVECs  MUnGeY5kfGmxbjDBd5NigQ>? NYn4NHhGPTBybl2= MkH0NUBp NVjkWnBuWmWmdXPld{BFXFhvVILp[4dmemWmIFXu[I91cGWuaXHsJGR6e2[3bnP0bY9v Mn7DQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV4M{S1N|goRjJ3NkO0OVM5RC:jPh?=
A549 MkjSSpVv[3Srb36gRZN{[Xl? M1i0flAvOcLizszN NWPQfYJvOjRiaB?= NYDweVR5\GWlcnXhd4V{KHSqZTDy[YxifGm4ZTDQT2Mu|rFibHX2[Ywhd25iY3XscEBu\W2kcnHu[UBkd3S{ZXH0[YQhSVNvSW[= Ml[yQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{MUixOlEoRjJ3MkG4NVYyRC:jPh?=
A549 MUnGeY5kfGmxbjDBd5NigQ>? NIrXVHAxNjIEoN88US=> MWKyOEBp Mom5doVlfWOnczD0bIUh\XiycnXzd4lwdiCuZY\lcJMhd2ZiTV3QMVItKE2PUD25JIFv\CCrboTl[5JqdiEQskG= NHL5ToM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKxPFE3OSd-MkWyNVgyPjF:L3G+
A549 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXuwMlHDqM7:TR?= NHfwdGYzPCCq NXLYTpVo\W6qYX7j[ZMh\3Kxd4ToJIlvcGmkaYTpc44h[2:2cnXheIVlKHerdHigRXMuUVZ? M1nwXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkG4NVYyLz5{NUKxPFE3OTxxYU6=
Mel202 NEnOe5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;pNE42KM7:TR?= NVfRWGhsOyCq MYXEUXNQ MnnG[Y5p[W6lZYOgTXIucW6mdXPl[EBz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJk> NHu3PZQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW5OVM5PSd-MkS1PVU{QDV:L3G+
92.1 NUPmWmFtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH72Om0xNjVizszN M37lVFMhcA>? MnvpSG1UVw>? NXrLOI1J\W6qYX7j[ZMhUVJvaX7keYNm\CC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHl? MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV7NUO4OUc,OjR3OUWzPFU9N2F-
OCM3 M4j3Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojBNE42KM7:TR?= MXmzJIg> NWnh[WVITE2VTx?= M{PwNIVvcGGwY3XzJGlTNWmwZIXj[YQhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6 MmPLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3OUWzPFUoRjJ2NUm1N|g2RC:jPh?=
Mel202 NGjzSY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVuwMlUh|ryP MYCzJIg> MnrhSG1UVw>? NGDGdY9qdmO{ZXHz[ZMhUVJvaX7keYNm\CClZXzsJIN6[2ynIHHydoV{fMLi M3\rV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NUm1N|g2Lz5{NEW5OVM5PTxxYU6=
92.1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEftcXYxNjVizszN NV;4S2R3OyCq NGnsOHVFVVOR M4nLXolv[3KnYYPld{BKWi2rbnT1Z4VlKGOnbHygZ5lkdGViYYLy[ZN1yqB? NXX1b5hFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1PVU{QDVpPkK0OVk2Ozh3PD;hQi=>
OCM3 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWWwMlUh|ryP M170U|MhcA>? NGXBXHpFVVOR MWnpcoNz\WG|ZYOgTXIucW6mdXPl[EBk\WyuIHP5Z4xmKGG{cnXzeOKh NGrOfHQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW5OVM5PSd-MkS1PVU{QDV:L3G+
Jeko-1 M3jhdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI\WVlkxNTRizszN NY[5XnJvTE2VTx?= NYjOXJBScW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4MkmzOUc,OjR|NkK5N|U9N2F-
Mino M{jVU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVS4VFJ1OC12IN88US=> NGP3[|VFVVOR MnnmbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NUDablFqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlI6OzVpPkK0N|YzQTN3PD;hQi=>
Rec-1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV6ye3FlOC12IN88US=> MnO1SG1UVw>? MnK5bY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4MkmzOUc,OjR|NkK5N|U9N2F-
SP49 NUDUW5Y4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXn0VnZXOC12IN88US=> M{WzNmROW09? M{HPRYlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NHqzXVg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2Nlk{PSd-MkSzOlI6OzV:L3G+
Jeko-1 MV;GeY5kfGmxbjDBd5NigQ>? MWGyMlUh|ryPwrC= NHfvSFcyOiCq MXjEUXNQ MUHkc5dvemWpdXzheIV{KE6ILd86RkB1[XKpZYSg[4Vv\XN? MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4MkmzOUc,OjR|NkK5N|U9N2F-
Mino MWDGeY5kfGmxbjDBd5NigQ>? Moe1Nk42KM7:TdMg Ml6yNVIhcA>? Ml3vSG1UVw>? MmLC[I94dnKnZ4XsZZRmeyCQRj5OvmIhfGG{Z3X0JIdmdmW| NH7pTJY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2Nlk{PSd-MkSzOlI6OzV:L3G+
Rec-1 NEnPW2VHfW6ldHnvckBCe3OjeR?= M1fBblIvPSEQvF5CpC=> NXfBSVZFOTJiaB?= NFHVd4tFVVOR NFL5Xo9ld3ewcnXneYxifGW|IF7GMe67SiC2YYLn[ZQh\2WwZYO= MnrqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NkK5N|UoRjJ2M{[yPVM2RC:jPh?=
SP49 M4W4TWZ2dmO2aX;uJGF{e2G7 NYjOVYxHOi53IN88UeKh NInWN|EyOiCq NGT6c4JFVVOR Ml2x[I94dnKnZ4XsZZRmeyCQRj5OvmIhfGG{Z3X0JIdmdmW| MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4MkmzOUc,OjR|NkK5N|U9N2F-
CD3+ T  NUnGe|d2TnWwY4Tpc44hSXO|YYm= NVzEXGRTOC13MECgcm0> M37pOlEhcA>? MWnpcohq[mm2czDOSk3PwkJicHjvd5Bpd3K7bHH0bY9vKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz NIDYZ5M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{W3N|I5Oyd-MkO1O|MzQDN:L3G+
Mel202 NVG0V|NxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLzRnJmOC13IN88US=> NX7pOFNDPzJiaB?= NVLHN2dCTE2VTx?= MnHzbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MkfyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4NUO5OlgoRjJ{NkWzPVY5RC:jPh?=
Omm1.3 MonBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HZRVAuPSEQvF2= MVW3NkBp M3X6V2ROW09? NH22S|RqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ3M{m2PEc,OjJ4NUO5Olg9N2F-
92.1 MoX4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\Od5VmOC13IN88US=> MVW3NkBp MWrEUXNQ NE\QR3JqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 NVT3XI5jRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2OVM6PjhpPkKyOlU{QTZ6PD;hQi=>
Mel202 M4DWXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlzsOUDPxE1? MX2yOEBp NX7FVXljTE2VTx?= MmrYbY5lfWOnczDHNUBienKnc4VCpC=> M4DscFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkWzPVY5Lz5{Mk[1N|k3QDxxYU6=
Omm1.3 MojkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILnUFE2KM7:TR?= MUGyOEBp NFf6O5NFVVOR NFyxUotqdmS3Y3XzJGcyKGG{cnXzeOKh NEHPUIg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[1N|k3QCd-MkK2OVM6Pjh:L3G+
92.1 NYWyV2w5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzWSJRRPSEQvF2= MnfVNlQhcA>? NFzTZYVFVVOR NV3yNIlScW6mdXPld{BIOSCjcoLld5TDqA>? NH33Opg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[1N|k3QCd-MkK2OVM6Pjh:L3G+
Mel202 NHnBUnZCeG:ydH;zbZMhSXO|YYm= NWWyZpc4PSEQvF2= MkfFO|IhcA>? M1nQS2ROW09? Mkn5bY5lfWOnczDhdI9xfG:|aYOgd4xq\2i2bIm= NYLVR5hqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2OVM6PjhpPkKyOlU{QTZ6PD;hQi=>
Omm1.3 M2nZfWFxd3C2b4Ppd{BCe3OjeR?= NVPufZNqPSEQvF2= M1ruO|czKGh? NITnT3dFVVOR MmS0bY5lfWOnczDhdI9xfG:|aYO= MnTVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4NUO5OlgoRjJ{NkWzPVY5RC:jPh?=
92.1 MWTBdI9xfG:|aYOgRZN{[Xl? NVy5VWhHPSEQvF2= NWPJXIVHPzJiaB?= M3HtTmROW09? MlHIbY5lfWOnczDhdI9xfG:|aYOgd4lodmmoY3HueIx6 MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ3M{m2PEc,OjJ4NUO5Olg9N2F-
Mel202 MWPGeY5kfGmxbjDBd5NigQ>? NHvNdmk2KM7:TR?= MnHBNlQhcA>? Mn7XbY5pcWKrdIOg[ZhxemW|c3nvckBidmRicHjvd5Bpd3K7bHH0bY9vKG:oIGDLR{Bqe2:ob4Ltdy=> MmrLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4NUO5OlgoRjJ{NkWzPVY5RC:jPh?=
Omm1.3 MnS3SpVv[3Srb36gRZN{[Xl? NWfZNI1oPSEQvF2= NFrl[VYzPCCq NEHaT49qdmirYnn0d{BmgHC{ZYPzbY9vKGGwZDDwbI9{eGixconsZZRqd25ib3[gVGtEKGm|b3\vdo1{ MoqyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4NUO5OlgoRjJ{NkWzPVY5RC:jPh?=
92.1 MWDGeY5kfGmxbjDBd5NigQ>? NEfFcWc2KM7:TR?= NGrtPFEzPCCq MXXpcohq[mm2czDlfJBz\XO|aX;uJIFv\CCyaH;zdIhwenmuYYTpc44hd2ZiUFvDJIl{d2[xcn3z M4DVSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkWzPVY5Lz5{Mk[1N|k3QDxxYU6=
HBL1 NIjUfWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\vPVAvOTZvMkCg{txO M{LaNVUh\A>? MYDJR|UxRTBwNTFOwG0> MkfRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|MkS5NlAoRjJzM{K0PVIxRC:jPh?=
TMD8 MmDNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHt[JVCOC5zNj2yNEDPxE1? NITsem02KGR? NGrUT2lKSzVyPUCuNkDPxE1? MlLFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|MkS5NlAoRjJzM{K0PVIxRC:jPh?=
OCI-Ly10 MlXpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmr4NE4yPi1{MDFOwG0> NFjC[XQ2KGR? MUnJR|UxRTFwMzFOwG0> MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN{NEmyNEc,OjF|MkS5NlA9N2F-
U2932 M2jWWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zrZlAvOTZvMkCg{txO MkXCOUBl NYjJVpQzUUN3ME2xNEDPxE1? NY\5d5Z1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzNlQ6OjBpPkKxN|I1QTJyPD;hQi=>
OCI-Ly3 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXrhVllWOC5zNj2yNEDPxE1? NHjSW3Q2KGR? Mmq0TWM2OO,:nkKwJO69VQ>? M{\YPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{K0PVIxLz5{MUOyOFkzODxxYU6=
SuDHL2 M2SwPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\BcVYyOC5zNj2yNEDPxE1? MkX5OUBl M37SPGlEPTExvK6yNEDPxE1? NGLwTm49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUOyOFkzOCd-MkGzNlQ6OjB:L3G+
SuDHL4 MnrtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTONE4yPi1{MDFOwG0> NGjO[nM2KGR? M1K0cGlEPTExvK6yNEDPxE1? M4WyPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{K0PVIxLz5{MUOyOFkzODxxYU6=
DB MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV72SFJPOC5zNj2yNEDPxE1? MXm1JIQ> MoSwTWM2OO,:nkKwJO69VQ>? NXPmd|BGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzNlQ6OjBpPkKxN|I1QTJyPD;hQi=>
Jurkat IL-2 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTZwN{GgxtEhOy55NjFOwG0> NYDTXZNLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5OFAzPTlpPkG5PVQxOjV7PD;hQi=>
PBMC IL-2 NH3uTJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPWe3BKSzVyPUSuPFQhyrFiMT63NEAh|ryP M1zZSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUSwNlU6Lz5zOUm0NFI2QTxxYU6=
Jurkat M3jnbWZ2dmO2aX;uJIF{e2G7 MXPJcohq[mm2aX;uJI9nKFSFUj;DSFI5NW2nZHnheIVlKGi3bXHuJHQh[2WubDDhZ5RqfmG2aX;uJIlvKEq3cnvheEBk\WyuczDlfJBz\XO|aX7nJIh2dWGwIFnMNkBxem:vb4TldkBjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYmsJGlEPTBiPTCwMlA2PCEQvF2u MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTh{N{izNUc,OTl6Mke4N|E9N2F-
Jurkat T MYHGeY5kfGmxbjDhd5NigQ>? NV:5U3dtPSCqcoO= NVPke3BmUW6qaXLpeIlwdiCxZjDQT2N1cGW2YTDpckBpfW2jbjDKeZJs[XRiVDDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4h[W62aT3DSFMwS0R{ODDhcpRq[m:meT3pcoR2[2WmIGStZ4VtdCCjY4TpeoF1cW:wIHL5JI1m[XO3cnnu[{Bl\WO{ZXHz[UBqdiCLTD2yJJNm[3KndHnvckBi\nSncjC1JIhzeyCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZktKEmFNUCgQUAxNjB6MTFOwG0v MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDF|MUexOEc,OjhzM{G3NVQ9N2F-
B-cells NFL1UnBHfW6ldHnvckBie3OjeR?= MXrJcohq[mm2aX;uJI9nKFCNQ3LleIEhcW5ibX;1d4UhSiClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gTYdONXO2aX31cIF1\WRiY3XscEBxem:uaX\ldoF1cW:wLDDJR|UxKD1iMD6yN|Qh|ryPLh?= MnPCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhzM{G3NVQoRjJ6MUOxO|E1RC:jPh?=
bone marrow cells M2HDS2FvfGmycn;sbYZmemG2aY\lJIF{e2G7 MkCyOEBl[Xm| MYnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IFPCRUBud3W|ZTDic45mKG2jcoLve{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIGuzTH11cHmvaXTpcoUhcW6lb4Lwc5JifGmxbjDh[pRmeiB2IHThfZMtKEmFNUCgQUA{NjdizszNMi=> M{jWPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OEK3PFMyLz5zOUiyO|g{OTxxYU6=
Assay
Methods Test Index PMID
Western blot pPKCδ/θ / phosphorylated MARCKS / p53 / MDM2 / PUMA / p21 ; Cyclin D1 / p27(Kip1) ; Bcl-xl / XIAP / Survivin ; PKCα / PKCδ / PKCβ / PKCε / PKCθ ; p-Marcks / p-ERK / p-AKT / p-S6 / Marcks / ERK / AKT / S6 29593251 22653968
Growth inhibition assay Cell viability 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 (from reference)

Animal Research:[3]
  • 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 3 years -20°C powder
2 years -80°C in solvent
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)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

(data from https://clinicaltrials.gov, updated on 2021-09-06)

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

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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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