Sotrastaurin (AEB071)

For research use only.

Catalog No.S2791

51 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.

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Selleck's Sotrastaurin (AEB071) has been cited by 51 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 NHfXW3JHfW6ldHnvckBCe3OjeR?= M{XOfVExOCCwTR?= NYW4[GduOyCq Ml\nSG1UVw>? M3zBSIlvcGmkaYTzJJJTVkFic4nueIhme2m| MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTZ7MUG1PEc,OjV4OUGxOVg9N2F-
HUVECs  MVPGeY5kfGmxbjDBd5NigQ>? NFrGNpA2ODCwTR?= NWS0PVh{OSCq MX;S[YR2[2W|IFTUXE1VemmpZ3Xy[YQhTW6mb4To[Yxq[WxiRInz[pVv[3Srb36= M1LBRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NkO0OVM5Lz5{NU[zOFU{QDxxYU6=
A549 M1rpcmZ2dmO2aX;uJGF{e2G7 MXOwMlHDqM7:TR?= NWrTepdyOjRiaB?= MkXs[IVkemWjc3XzJJRp\SC{ZXzheIl3\SCSS1Ot{tEhdGW4ZXygc44h[2WubDDt[Y1jemGwZTDjc5Rz\WG2ZXSgRXMuUVZ? NG[1T|c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKxPFE3OSd-MkWyNVgyPjF:L3G+
A549 MnHaSpVv[3Srb36gRZN{[Xl? MkTYNE4yyqEQvF2= M2X2[lI1KGh? M130fJJm\HWlZYOgeIhmKGW6cILld5Nqd25ibHX2[Yx{KG:oIF3NVE0zNCCPTWCtPUBidmRiaX70[YdzcW5izsKx MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJzOEG2NUc,OjV{MUixOlE9N2F-
A549 NW[5[HZPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4XHSVAvOcLizszN MlG4NlQhcA>? M4LEbIVvcGGwY3XzJIdzd3e2aDDpcohq[mm2aX;uJINwfHKnYYTl[EB4cXSqIFHTMWlX MlTUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{MUixOlEoRjJ3MkG4NVYyRC:jPh?=
Mel202 MlLnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXtNE42KM7:TR?= M4XwbVMhcA>? NHjtWXJFVVOR MY\lcohidmOnczDJVk1qdmS3Y3XkJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fS=> NXHEOJl7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1PVU{QDVpPkK0OVk2Ozh3PD;hQi=>
92.1 Mo\zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zHSlAvPSEQvF2= M1LOT|MhcA>? M1LDS2ROW09? NUPid3Jm\W6qYX7j[ZMhUVJvaX7keYNm\CC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHl? M{THbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NUm1N|g2Lz5{NEW5OVM5PTxxYU6=
OCM3 M3nw[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkG0NE42KM7:TR?= MonpN{Bp Mn[wSG1UVw>? MXTlcohidmOnczDJVk1qdmS3Y3XkJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fS=> NHXmdGQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW5OVM5PSd-MkS1PVU{QDV:L3G+
Mel202 NVGycWJtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEnJem8xNjVizszN MVSzJIg> MX7EUXNQ NW\NXYFGcW6lcnXhd4V{KEmULXnu[JVk\WRiY3XscEBkgWOuZTDhdpJme3UEoB?= NELjdFA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW5OVM5PSd-MkS1PVU{QDV:L3G+
92.1 M2rM[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4C4VlAvPSEQvF2= NF7OTFE{KGh? NXL5[phmTE2VTx?= NYfHbo9ScW6lcnXhd4V{KEmULXnu[JVk\WRiY3XscEBkgWOuZTDhdpJme3UEoB?= NX7UNlUxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1PVU{QDVpPkK0OVk2Ozh3PD;hQi=>
OCM3 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4nKUlAvPSEQvF2= MmrDN{Bp MXfEUXNQ MYDpcoNz\WG|ZYOgTXIucW6mdXPl[EBk\WyuIHP5Z4xmKGG{cnXzeOKh NXv2SoFIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1PVU{QDVpPkK0OVk2Ozh3PD;hQi=>
Jeko-1 M1\semdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTNW|ZYOC12IN88US=> NYX4WGVuTE2VTx?= NVPHZnN1cW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? M3zy[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{[yPVM2Lz5{NEO2Nlk{PTxxYU6=
Mino MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVGwMVQh|ryP MlzqSG1UVw>? NY\xbHJncW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? Mo\WQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NkK5N|UoRjJ2M{[yPVM2RC:jPh?=
Rec-1 M2rBPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nRR|AuPCEQvF2= Mke3SG1UVw>? MWTpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NYjUcolvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlI6OzVpPkK0N|YzQTN3PD;hQi=>
SP49 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTodYFOOC12IN88US=> MUXEUXNQ NYDKUXk{cW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4MkmzOUc,OjR|NkK5N|U9N2F-
Jeko-1 MWnGeY5kfGmxbjDBd5NigQ>? M3exWFIvPSEQvF5CpC=> MnjzNVIhcA>? MWjEUXNQ MnrQ[I94dnKnZ4XsZZRmeyCQRj5OvmIhfGG{Z3X0JIdmdmW| M{\xTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{[yPVM2Lz5{NEO2Nlk{PTxxYU6=
Mino MYTGeY5kfGmxbjDBd5NigQ>? Mnv4Nk42KM7:TdMg NWPMcZp2OTJiaB?= NUWxOWgxTE2VTx?= NGjaZnhld3ewcnXneYxifGW|IF7GMe67SiC2YYLn[ZQh\2WwZYO= M3;Vb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{[yPVM2Lz5{NEO2Nlk{PTxxYU6=
Rec-1 NGjPZYlHfW6ldHnvckBCe3OjeR?= MWKyMlUh|ryPwrC= MmrrNVIhcA>? NYjIZpl[TE2VTx?= NGP4WWNld3ewcnXneYxifGW|IF7GMe67SiC2YYLn[ZQh\2WwZYO= MlLyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NkK5N|UoRjJ2M{[yPVM2RC:jPh?=
SP49 MYDGeY5kfGmxbjDBd5NigQ>? NIPqPJYzNjVizszNxsA> M2L6PVEzKGh? M3zVbWROW09? MnXV[I94dnKnZ4XsZZRmeyCQRj5OvmIhfGG{Z3X0JIdmdmW| MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4MkmzOUc,OjR|NkK5N|U9N2F-
CD3+ T  Mkf6SpVv[3Srb36gRZN{[Xl? MWmwMVUxOCCwTR?= M3TyWVEhcA>? NEXMSVZqdmirYnn0d{BPTi4QulKgdIhwe3Cqb4L5cIF1cW:wIHnuJIEh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ NF6z[mc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{W3N|I5Oyd-MkO1O|MzQDN:L3G+
Mel202 NYLhc3ZCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfRcGsxNTVizszN NX\hUJlVPzJiaB?= NHz1fXFFVVOR NUPadGNmcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ3M{m2PEc,OjJ4NUO5Olg9N2F-
Omm1.3 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfSVXczOC13IN88US=> MY[3NkBp NEixb4pFVVOR MlrubY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ3M{m2PEc,OjJ4NUO5Olg9N2F-
92.1 MmrpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGrmSHoxNTVizszN M1PONFczKGh? NVLsbJh5TE2VTx?= MkHQbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NFLNSY89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[1N|k3QCd-MkK2OVM6Pjh:L3G+
Mel202 M3\RSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEH5O4E2KM7:TR?= M1TUWlI1KGh? M1XpVGROW09? NWLuSpJ7cW6mdXPld{BIOSCjcoLld5TDqA>? NHPHR3k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[1N|k3QCd-MkK2OVM6Pjh:L3G+
Omm1.3 NV[2VHNVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TOelUh|ryP NX:wO|Z[OjRiaB?= NXHNO205TE2VTx?= MUXpcoR2[2W|IFexJIFzemW|dNMg MoXDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4NUO5OlgoRjJ{NkWzPVY5RC:jPh?=
92.1 MnfPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlm4OUDPxE1? NVXGendKOjRiaB?= NYjC[o96TE2VTx?= NYD1V5FWcW6mdXPld{BIOSCjcoLld5TDqA>? NV7M[WVxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2OVM6PjhpPkKyOlU{QTZ6PD;hQi=>
Mel202 M336OGFxd3C2b4Ppd{BCe3OjeR?= Ml3IOUDPxE1? NUf4W4JyPzJiaB?= MYHEUXNQ NUHoUWNucW6mdXPld{BieG:ydH;zbZMhe2yrZ3j0cJk> M2fV[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkWzPVY5Lz5{Mk[1N|k3QDxxYU6=
Omm1.3 Mm\iRZBweHSxc3nzJGF{e2G7 NXnGOnVCPSEQvF2= MXu3NkBp NEH0ZYNFVVOR Ml7qbY5lfWOnczDhdI9xfG:|aYO= NVSzTXI3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2OVM6PjhpPkKyOlU{QTZ6PD;hQi=>
92.1 MoL4RZBweHSxc3nzJGF{e2G7 MX61JO69VQ>? NV:zXYo2PzJiaB?= NXTaVYtbTE2VTx?= MnfRbY5lfWOnczDhdI9xfG:|aYOgd4lodmmoY3HueIx6 M1L2TVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkWzPVY5Lz5{Mk[1N|k3QDxxYU6=
Mel202 NYq3bnVuTnWwY4Tpc44hSXO|YYm= NITnXow2KM7:TR?= MW[yOEBp NWPac2prcW6qaXLpeJMh\XiycnXzd4lwdiCjbnSgdIhwe3Cqb4L5cIF1cW:wIH;mJHBMSyCrc3;mc5Juew>? NXvYZ3g4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2OVM6PjhpPkKyOlU{QTZ6PD;hQi=>
Omm1.3 M1Sw[2Z2dmO2aX;uJGF{e2G7 MnLsOUDPxE1? MUeyOEBp MYTpcohq[mm2czDlfJBz\XO|aX;uJIFv\CCyaH;zdIhwenmuYYTpc44hd2ZiUFvDJIl{d2[xcn3z NGGyR2U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[1N|k3QCd-MkK2OVM6Pjh:L3G+
92.1 NFLYZYlHfW6ldHnvckBCe3OjeR?= M4jPW|Uh|ryP NEKzXY8zPCCq MkHobY5pcWKrdIOg[ZhxemW|c3nvckBidmRicHjvd5Bpd3K7bHH0bY9vKG:oIGDLR{Bqe2:ob4Ltdy=> M1n1RVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkWzPVY5Lz5{Mk[1N|k3QDxxYU6=
HBL1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUSwMlE3NTJyIN88US=> M2fWR|Uh\A>? MoLVTWM2OD1yLkWg{txO MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN{NEmyNEc,OjF|MkS5NlA9N2F-
TMD8 M4POdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLzbJpSOC5zNj2yNEDPxE1? MkXHOUBl MVXJR|UxRTBwMjFOwG0> MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN{NEmyNEc,OjF|MkS5NlA9N2F-
OCI-Ly10 NFjmR5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVewMlE3NTJyIN88US=> NGHDd|Y2KGR? MUnJR|UxRTFwMzFOwG0> M1zpbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{K0PVIxLz5{MUOyOFkzODxxYU6=
U2932 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{Pab|AvOTZvMkCg{txO MoG2OUBl M{C3UmlEPTB;MUCg{txO MmTSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|MkS5NlAoRjJzM{K0PVIxRC:jPh?=
OCI-Ly3 NIHaT5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXywMlE3NTJyIN88US=> NH3We|E2KGR? NIfmXlNKSzVy78{eNlAh|ryP MknkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|MkS5NlAoRjJzM{K0PVIxRC:jPh?=
SuDHL2 NH\tOHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TyW|AvOTZvMkCg{txO NFPWfXI2KGR? MX3JR|Ux97zgMkCg{txO MmnxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|MkS5NlAoRjJzM{K0PVIxRC:jPh?=
SuDHL4 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUOwWZhxOC5zNj2yNEDPxE1? MonjOUBl NEHBZ3FKSzVy78{eNlAh|ryP NV\aZpJkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzNlQ6OjBpPkKxN|I1QTJyPD;hQi=>
DB NIfJbVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mon6NE4yPi1{MDFOwG0> NWHGc5JiPSCm NUG2XZg1UUN3MP-8olIxKM7:TR?= NEjBZok9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUOyOFkzOCd-MkGzNlQ6OjB:L3G+
Jurkat IL-2 NGLzephIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\EWFhSUUN3ME22MlcyKMLzIEOuO|Yh|ryP NIiwVlI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm0NFI2QSd-MUm5OFAzPTl:L3G+
PBMC IL-2 M2jKNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jReWlEPTB;ND64OEDDuSBzLkewJEDPxE1? MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl2MEK1PUc,OTl7NECyOVk9N2F-
Jurkat NUnHXop4TnWwY4Tpc44h[XO|YYm= NGLzb4dKdmirYnn0bY9vKG:oIGTDVk9ETDJ6LX3l[IlifGWmIHj1cYFvKFRiY3XscEBi[3SrdnH0bY9vKGmwIFr1dotifCClZXzsd{BmgHC{ZYPzbY5oKGi3bXHuJGlNOiCycn;tc5RmeiCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZktKEmFNUCgQUAxNjB3NDFOwG0v MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTh{N{izNUc,OTl6Mke4N|E9N2F-
Jurkat T MmXSSpVv[3Srb36gZZN{[Xl? MoHqOUBpenN? NWXUWndkUW6qaXLpeIlwdiCxZjDQT2N1cGW2YTDpckBpfW2jbjDKeZJs[XRiVDDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4h[W62aT3DSFMwS0R{ODDhcpRq[m:meT3pcoR2[2WmIGStZ4VtdCCjY4TpeoF1cW:wIHL5JI1m[XO3cnnu[{Bl\WO{ZXHz[UBqdiCLTD2yJJNm[3KndHnvckBi\nSncjC1JIhzeyCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZktKEmFNUCgQUAxNjB6MTFOwG0v NInIZmo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEGzNVcyPCd-MkixN|E4OTR:L3G+
B-cells MX7GeY5kfGmxbjDhd5NigQ>? MljQTY5pcWKrdHnvckBw\iCSS1Pi[ZRiKGmwIH3veZNmKEJiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJGloVS2|dHnteYxifGWmIHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OCB;IECuNlM1KM7:TT6= M4TRV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MUOxO|E1Lz5{OEGzNVcyPDxxYU6=
bone marrow cells NE\a[VZCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MXi0JIRigXN? MV3BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IFPCRUBud3W|ZTDic45mKG2jcoLve{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIGuzTH11cHmvaXTpcoUhcW6lb4Lwc5JifGmxbjDh[pRmeiB2IHThfZMtKEmFNUCgQUA{NjdizszNMi=> NE\vbZg9[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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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 SDS / 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:

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Molecular Weight Calculator

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

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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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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