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 62 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 MYDGeY5kfGmxbjDBd5NigQ>? Mo\hNVAxKG6P MYmzJIg> NWe4ZVRGTE2VTx?= M4C4N4lvcGmkaYTzJJJTVkFic4nueIhme2m| MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTZ7MUG1PEc,OjV4OUGxOVg9N2F-
HUVECs  M2fLWGZ2dmO2aX;uJGF{e2G7 MmfOOVAxdk1? MmLKNUBp MX3S[YR2[2W|IFTUXE1VemmpZ3Xy[YQhTW6mb4To[Yxq[WxiRInz[pVv[3Srb36= NFHP[5I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NU[zOFU{QCd-MkW2N|Q2Ozh:L3G+
A549 MXrGeY5kfGmxbjDBd5NigQ>? MkjKNE4yyqEQvF2= NWrEWnd[OjRiaB?= M4rGe4Rm[3KnYYPld{B1cGVicnXsZZRqfmViUFvDMe6yKGyndnXsJI9vKGOnbHygcYVu[nKjbnWgZ491emWjdHXkJGFUNUmY MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJzOEG2NUc,OjV{MUixOlE9N2F-
A549 MkP6SpVv[3Srb36gRZN{[Xl? MnHWNE4yyqEQvF2= M4rES|I1KGh? NHfseI1z\WS3Y3XzJJRp\SCneIDy[ZN{cW:wIHzleoVteyCxZjDNUXAuOixiTV3QMVkh[W6mIHnueIVoemmwIN8yNS=> NX7IUnhPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyNVgyPjFpPkK1NlE5OTZzPD;hQi=>
A549 M{XiXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDiZo1KOC5zwrFOwG0> M2TvVlI1KGh? M1nvboVvcGGwY3XzJIdzd3e2aDDpcohq[mm2aX;uJINwfHKnYYTl[EB4cXSqIFHTMWlX NXeweo83RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyNVgyPjFpPkK1NlE5OTZzPD;hQi=>
Mel202 MnT3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PNN|AvPSEQvF2= M2LDXFMhcA>? MY\EUXNQ NXvUbJFP\W6qYX7j[ZMhUVJvaX7keYNm\CC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHl? M{jnfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NUm1N|g2Lz5{NEW5OVM5PTxxYU6=
92.1 NGqxXFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnjTNE42KM7:TR?= Mk\5N{Bp MXLEUXNQ Mkfq[Y5p[W6lZYOgTXIucW6mdXPl[EBz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJk> NVPVR|NCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1PVU{QDVpPkK0OVk2Ozh3PD;hQi=>
OCM3 NIn1RW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLVNE42KM7:TR?= MmXBN{Bp MmDOSG1UVw>? MXHlcohidmOnczDJVk1qdmS3Y3XkJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fS=> MnPkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3OUWzPFUoRjJ2NUm1N|g2RC:jPh?=
Mel202 NYnWVIRoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\GZ40xNjVizszN Mmj5N{Bp MUHEUXNQ MnXKbY5kemWjc3XzJGlTNWmwZIXj[YQh[2WubDDjfYNt\SCjcoLld5TDqA>? NVXaS|ZkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1PVU{QDVpPkK0OVk2Ozh3PD;hQi=>
92.1 NXHCXWpwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIrZSHkxNjVizszN MVezJIg> M3vVRmROW09? MoG4bY5kemWjc3XzJGlTNWmwZIXj[YQh[2WubDDjfYNt\SCjcoLld5TDqA>? NFLZeWQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW5OVM5PSd-MkS1PVU{QDV:L3G+
OCM3 NXzEeXh4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHONE42KM7:TR?= MkHBN{Bp NGTQWIxFVVOR NGDoSopqdmO{ZXHz[ZMhUVJvaX7keYNm\CClZXzsJIN6[2ynIHHydoV{fMLi NYDLXlVpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1PVU{QDVpPkK0OVk2Ozh3PD;hQi=>
Jeko-1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlrENE01KM7:TR?= MlHtSG1UVw>? NFPlUYdqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 NFrR[Fk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2Nlk{PSd-MkSzOlI6OzV:L3G+
Mino Mn;5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYCwMVQh|ryP MnK2SG1UVw>? NGTaRZpqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 M3ewblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{[yPVM2Lz5{NEO2Nlk{PTxxYU6=
Rec-1 Mn3DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF:wZlYxNTRizszN NILUdWVFVVOR MXPpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NXe5d|hQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlI6OzVpPkK0N|YzQTN3PD;hQi=>
SP49 NHfVe5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7BNE01KM7:TR?= NUnjOXhbTE2VTx?= NH7JfpFqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 NUD1RWlURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlI6OzVpPkK0N|YzQTN3PD;hQi=>
Jeko-1 NFTkb3FHfW6ldHnvckBCe3OjeR?= NX2yb5RFOi53IN88UeKh NFXaWGUyOiCq NW[4ZmhSTE2VTx?= MoH1[I94dnKnZ4XsZZRmeyCQRj5OvmIhfGG{Z3X0JIdmdmW| NWfNcodmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlI6OzVpPkK0N|YzQTN3PD;hQi=>
Mino NX;Melg3TnWwY4Tpc44hSXO|YYm= NX\xOIk5Oi53IN88UeKh NHLnUZMyOiCq MlntSG1UVw>? NXzxNIxI\G:5boLl[5Vt[XSnczDOSk3PwkJidHHy[4V1KGenbnXz Mmq0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NkK5N|UoRjJ2M{[yPVM2RC:jPh?=
Rec-1 NH2zb2dHfW6ldHnvckBCe3OjeR?= MkHoNk42KM7:TdMg NGrtNWUyOiCq MWfEUXNQ MnPR[I94dnKnZ4XsZZRmeyCQRj5OvmIhfGG{Z3X0JIdmdmW| NUDTVZY3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlI6OzVpPkK0N|YzQTN3PD;hQi=>
SP49 M1nyemZ2dmO2aX;uJGF{e2G7 MnvFNk42KM7:TdMg NFTD[3QyOiCq MXHEUXNQ NIDoN4Nld3ewcnXneYxifGW|IF7GMe67SiC2YYLn[ZQh\2WwZYO= M4KyNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{[yPVM2Lz5{NEO2Nlk{PTxxYU6=
CD3+ T  NHPnOWZHfW6ldHnvckBCe3OjeR?= NYTwU|RDOC13MECgcm0> MnnBNUBp MnrIbY5pcWKrdIOgUmYu|rqEIIDoc5NxcG:{eXzheIlwdiCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzV5M{K4N{c,OjN3N{OyPFM9N2F-
Mel202 M2nHN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYGwMVUh|ryP MXy3NkBp MVXEUXNQ M1PrSYlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NYjhRpBYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2OVM6PjhpPkKyOlU{QTZ6PD;hQi=>
Omm1.3 MoTmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\tNE02KM7:TR?= NUXqWoVbPzJiaB?= NV\B[XVETE2VTx?= MmLlbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NHnJXVE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[1N|k3QCd-MkK2OVM6Pjh:L3G+
92.1 NVG3RWZjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;LeVAuPSEQvF2= M1ezNlczKGh? NHnXWW5FVVOR NI\KNWJqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 NXu4TZJ3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2OVM6PjhpPkKyOlU{QTZ6PD;hQi=>
Mel202 NVftOYVJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHhSnk{PSEQvF2= NF;md2EzPCCq NVzSUVh6TE2VTx?= MmDybY5lfWOnczDHNUBienKnc4VCpC=> M3i4PVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkWzPVY5Lz5{Mk[1N|k3QDxxYU6=
Omm1.3 NGjG[nZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nxdVUh|ryP NYHL[WVIOjRiaB?= Moe1SG1UVw>? M1jRdIlv\HWlZYOgS|Eh[XK{ZYP0xsA> M2X2RVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkWzPVY5Lz5{Mk[1N|k3QDxxYU6=
92.1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDUVXA3PSEQvF2= MU[yOEBp NHfMb5RFVVOR NEfCPXdqdmS3Y3XzJGcyKGG{cnXzeOKh MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ3M{m2PEc,OjJ4NUO5Olg9N2F-
Mel202 M3LVcWFxd3C2b4Ppd{BCe3OjeR?= M4rr[|Uh|ryP MUO3NkBp M4L5S2ROW09? NETDWFBqdmS3Y3XzJIFxd3C2b4Ppd{B{dGmpaITsfS=> MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ3M{m2PEc,OjJ4NUO5Olg9N2F-
Omm1.3 MXvBdI9xfG:|aYOgRZN{[Xl? MmHGOUDPxE1? M3zWTFczKGh? MX;EUXNQ M2D2[4lv\HWlZYOgZZBweHSxc3nz MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ3M{m2PEc,OjJ4NUO5Olg9N2F-
92.1 M3TDemFxd3C2b4Ppd{BCe3OjeR?= NVTPc2l[PSEQvF2= Mo\KO|IhcA>? NGDyWllFVVOR NW\3S5JicW6mdXPld{BieG:ydH;zbZMhe2mpbnnmZ4FvfGy7 NXHUWYhXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2OVM6PjhpPkKyOlU{QTZ6PD;hQi=>
Mel202 M37NfmZ2dmO2aX;uJGF{e2G7 NInWUFg2KM7:TR?= MVeyOEBp NEPJS|BqdmirYnn0d{BmgHC{ZYPzbY9vKGGwZDDwbI9{eGixconsZZRqd25ib3[gVGtEKGm|b3\vdo1{ MkDEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4NUO5OlgoRjJ{NkWzPVY5RC:jPh?=
Omm1.3 NGfoW5NHfW6ldHnvckBCe3OjeR?= NH\1Rnc2KM7:TR?= NYfIOVZmOjRiaB?= MVLpcohq[mm2czDlfJBz\XO|aX;uJIFv\CCyaH;zdIhwenmuYYTpc44hd2ZiUFvDJIl{d2[xcn3z MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ3M{m2PEc,OjJ4NUO5Olg9N2F-
92.1 MWXGeY5kfGmxbjDBd5NigQ>? NUDGVJhTPSEQvF2= M2G3OlI1KGh? NI\nfpNqdmirYnn0d{BmgHC{ZYPzbY9vKGGwZDDwbI9{eGixconsZZRqd25ib3[gVGtEKGm|b3\vdo1{ MnWxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4NUO5OlgoRjJ{NkWzPVY5RC:jPh?=
HBL1 NWiyN5pIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jIVlAvOTZvMkCg{txO NYfDcHJSPSCm MWnJR|UxRTBwNTFOwG0> NIP0e|M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUOyOFkzOCd-MkGzNlQ6OjB:L3G+
TMD8 MmjIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPCfYZOOC5zNj2yNEDPxE1? MnjMOUBl NUnudFRFUUN3ME2wMlIh|ryP Moi4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|MkS5NlAoRjJzM{K0PVIxRC:jPh?=
OCI-Ly10 NGrRVJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFnsZ2sxNjF4LUKwJO69VQ>? MlzUOUBl NEDMVWxKSzVyPUGuN{DPxE1? M2\LblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{K0PVIxLz5{MUOyOFkzODxxYU6=
U2932 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfI[mJXOC5zNj2yNEDPxE1? MVq1JIQ> NIrPbllKSzVyPUGwJO69VQ>? M1GzfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{K0PVIxLz5{MUOyOFkzODxxYU6=
OCI-Ly3 NWj2[VlkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXeyeIN7OC5zNj2yNEDPxE1? Moe2OUBl M3\kUWlEPTExvK6yNEDPxE1? M{fZUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{K0PVIxLz5{MUOyOFkzODxxYU6=
SuDHL2 M4PzWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jrPFAvOTZvMkCg{txO NVP2eWZXPSCm M2fQ[WlEPTExvK6yNEDPxE1? M32xVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{K0PVIxLz5{MUOyOFkzODxxYU6=
SuDHL4 NF7MWIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGCxT|cxNjF4LUKwJO69VQ>? NHnPSXY2KGR? Mln6TWM2OO,:nkKwJO69VQ>? MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN{NEmyNEc,OjF|MkS5NlA9N2F-
DB MnW3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV:wMlE3NTJyIN88US=> NUTicWFXPSCm NHf6[WZKSzVy78{eNlAh|ryP M3\TPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{K0PVIxLz5{MUOyOFkzODxxYU6=
Jurkat IL-2 NYXrTpRtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmSzTWM2OD14LkexJOKyKDNwN{[g{txO MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl2MEK1PUc,OTl7NECyOVk9N2F-
PBMC IL-2 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTRwOESgxtEhOS55MDCg{txO MlGwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7NECyOVkoRjF7OUSwNlU6RC:jPh?=
Jurkat M1TPV2Z2dmO2aX;uJIF{e2G7 MVzJcohq[mm2aX;uJI9nKFSFUj;DSFI5NW2nZHnheIVlKGi3bXHuJHQh[2WubDDhZ5RqfmG2aX;uJIlvKEq3cnvheEBk\WyuczDlfJBz\XO|aX7nJIh2dWGwIFnMNkBxem:vb4TldkBjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYmsJGlEPTBiPTCwMlA2PCEQvF2u MoroQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl6Mke4N|EoRjF7OEK3PFMyRC:jPh?=
Jurkat T MYTGeY5kfGmxbjDhd5NigQ>? NIfjcpk2KGi{cx?= NWXqbII5UW6qaXLpeIlwdiCxZjDQT2N1cGW2YTDpckBpfW2jbjDKeZJs[XRiVDDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4h[W62aT3DSFMwS0R{ODDhcpRq[m:meT3pcoR2[2WmIGStZ4VtdCCjY4TpeoF1cW:wIHL5JI1m[XO3cnnu[{Bl\WO{ZXHz[UBqdiCLTD2yJJNm[3KndHnvckBi\nSncjC1JIhzeyCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZktKEmFNUCgQUAxNjB6MTFOwG0v NWOwZ5R2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixN|E4OTRpPkK4NVMyPzF2PD;hQi=>
B-cells NFqzblFHfW6ldHnvckBie3OjeR?= NEj5UoxKdmirYnn0bY9vKG:oIGDLR4JmfGFiaX6gcY92e2ViQjDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4hUWePLYP0bY12dGG2ZXSgZ4VtdCCycn;sbYZmemG2aX;uMEBKSzVyIE2gNE4zOzRizszNMi=> MnHmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhzM{G3NVQoRjJ6MUOxO|E1RC:jPh?=
bone marrow cells MV3BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MXK0JIRigXN? NGPX[4RCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JGNDSSCvb4Xz[UBjd26nIH3hdpJwfyClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJHs{UF22aIntbYRqdmViaX7jc5Jxd3KjdHnvckBi\nSncjC0JIRigXNuIFnDOVAhRSB|Lkeg{txONg>? M2LINlxiKHSjcnfleF0oZ2KuYX7rK{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

Solubility (25°C)

In vitro

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

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 2022-08-01)

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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