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 MWPGeY5kfGmxbjDBd5NigQ>? MmXnNVAxKG6P NVTVUpV3OyCq MmX5SG1UVw>? MlXsbY5pcWKrdIOgdnJPSSC|eX70bIV{cXN? M2jIcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NkmxNVU5Lz5{NU[5NVE2QDxxYU6=
HUVECs  MXrGeY5kfGmxbjDBd5NigQ>? NF\wS5o2ODCwTR?= MkW0NUBp MVjS[YR2[2W|IFTUXE1VemmpZ3Xy[YQhTW6mb4To[Yxq[WxiRInz[pVv[3Srb36= MmfMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV4M{S1N|goRjJ3NkO0OVM5RC:jPh?=
A549 NYDFe4o5TnWwY4Tpc44hSXO|YYm= MYGwMlHDqM7:TR?= MoD5NlQhcA>? NXzIeINP\GWlcnXhd4V{KHSqZTDy[YxifGm4ZTDQT2Mu|rFibHX2[Ywhd25iY3XscEBu\W2kcnHu[UBkd3S{ZXH0[YQhSVNvSW[= NUL5PZluRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyNVgyPjFpPkK1NlE5OTZzPD;hQi=>
A549 MWDGeY5kfGmxbjDBd5NigQ>? NE\CdIcxNjIEoN88US=> M4jSe|I1KGh? NILuXlhz\WS3Y3XzJJRp\SCneIDy[ZN{cW:wIHzleoVteyCxZjDNUXAuOixiTV3QMVkh[W6mIHnueIVoemmwIN8yNS=> NXTRZ4N7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyNVgyPjFpPkK1NlE5OTZzPD;hQi=>
A549 MoPiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYjnb3RpOC5zwrFOwG0> M13SSVI1KGh? NFzJOmdmdmijbnPld{Boem:5dHigbY5pcWKrdHnvckBkd3S{ZXH0[YQhf2m2aDDBV{1KXg>? M4XhVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkG4NVYyLz5{NUKxPFE3OTxxYU6=
Mel202 NX22bHoxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojXNE42KM7:TR?= M37zNVMhcA>? MlfrSG1UVw>? NETDXFRmdmijbnPld{BKWi2rbnT1Z4VlKHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gQ>? MoDJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3OUWzPFUoRjJ2NUm1N|g2RC:jPh?=
92.1 NWjwWJVLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnoT4U5OC53IN88US=> NHr3ZVU{KGh? MkGwSG1UVw>? MYHlcohidmOnczDJVk1qdmS3Y3XkJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fS=> M3nYeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NUm1N|g2Lz5{NEW5OVM5PTxxYU6=
OCM3 NX\VVJh4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPaXHVpOC53IN88US=> NHvMOpo{KGh? NEfsWo5FVVOR NG\nTGFmdmijbnPld{BKWi2rbnT1Z4VlKHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gQ>? MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV7NUO4OUc,OjR3OUWzPFU9N2F-
Mel202 NYLqbIFPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFy1NmsxNjVizszN MnnlN{Bp MYjEUXNQ NF\wVY1qdmO{ZXHz[ZMhUVJvaX7keYNm\CClZXzsJIN6[2ynIHHydoV{fMLi MlfHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3OUWzPFUoRjJ2NUm1N|g2RC:jPh?=
92.1 NEfuOFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17pUlAvPSEQvF2= NVrSRnd7OyCq NHPEeYZFVVOR Mk\6bY5kemWjc3XzJGlTNWmwZIXj[YQh[2WubDDjfYNt\SCjcoLld5TDqA>? M1\W[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NUm1N|g2Lz5{NEW5OVM5PTxxYU6=
OCM3 NY\UcZdIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jUTlAvPSEQvF2= NEnHWGk{KGh? NH:zbmFFVVOR M1Tv[olv[3KnYYPld{BKWi2rbnT1Z4VlKGOnbHygZ5lkdGViYYLy[ZN1yqB? MoLhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3OUWzPFUoRjJ2NUm1N|g2RC:jPh?=
Jeko-1 M{LMSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnL[GJLOC12IN88US=> MVPEUXNQ MXnpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MmHCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NkK5N|UoRjJ2M{[yPVM2RC:jPh?=
Mino NX:yRmdYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWmwMVQh|ryP NVPN[o9mTE2VTx?= NVH1UmtycW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? M{\GXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{[yPVM2Lz5{NEO2Nlk{PTxxYU6=
Rec-1 M2rSdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYGwMVQh|ryP Mo[1SG1UVw>? MnH5bY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> M4Xkc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{[yPVM2Lz5{NEO2Nlk{PTxxYU6=
SP49 MomyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXmxXmVTOC12IN88US=> M2nkcWROW09? NUfWPGNrcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4MkmzOUc,OjR|NkK5N|U9N2F-
Jeko-1 Ml\kSpVv[3Srb36gRZN{[Xl? NHjzSHYzNjVizszNxsA> NUPjeWx4OTJiaB?= MYLEUXNQ NFnVUJRld3ewcnXneYxifGW|IF7GMe67SiC2YYLn[ZQh\2WwZYO= MoXZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NkK5N|UoRjJ2M{[yPVM2RC:jPh?=
Mino MnvGSpVv[3Srb36gRZN{[Xl? MWSyMlUh|ryPwrC= NFLWdmgyOiCq NILjUnlFVVOR MWLkc5dvemWpdXzheIV{KE6ILd86RkB1[XKpZYSg[4Vv\XN? MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4MkmzOUc,OjR|NkK5N|U9N2F-
Rec-1 M4e2dWZ2dmO2aX;uJGF{e2G7 NWjTXZRwOi53IN88UeKh MnfnNVIhcA>? NUHsbZM2TE2VTx?= NWnkNVZj\G:5boLl[5Vt[XSnczDOSk3PwkJidHHy[4V1KGenbnXz MoPHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NkK5N|UoRjJ2M{[yPVM2RC:jPh?=
SP49 MkjMSpVv[3Srb36gRZN{[Xl? NYTkVGdGOi53IN88UeKh MnrwNVIhcA>? MXXEUXNQ MVPkc5dvemWpdXzheIV{KE6ILd86RkB1[XKpZYSg[4Vv\XN? M{K5O|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{[yPVM2Lz5{NEO2Nlk{PTxxYU6=
CD3+ T  NX3xUIxsTnWwY4Tpc44hSXO|YYm= M4[xOVAuPTByIH7N M1zXdFEhcA>? NXe4RogycW6qaXLpeJMhVkZvzsrCJJBpd3OyaH;yfYxifGmxbjDpckBiKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzV5M{K4N{c,OjN3N{OyPFM9N2F-
Mel202 MnXiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPVbXBNOC13IN88US=> M3;Bc|czKGh? MnLDSG1UVw>? NYexU4RGcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NGDkXGw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[1N|k3QCd-MkK2OVM6Pjh:L3G+
Omm1.3 Mn\MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\INE02KM7:TR?= MkXSO|IhcA>? NUCwXoZkTE2VTx?= NXXySnhwcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NH[3UZU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[1N|k3QCd-MkK2OVM6Pjh:L3G+
92.1 MmnpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTiNE02KM7:TR?= M2LRW|czKGh? NFq1OHFFVVOR NFTLRmpqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ3M{m2PEc,OjJ4NUO5Olg9N2F-
Mel202 M13Ucmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLibGw2KM7:TR?= M2q2OVI1KGh? M{nYe2ROW09? M{LQe4lv\HWlZYOgS|Eh[XK{ZYP0xsA> NVOwfnRVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2OVM6PjhpPkKyOlU{QTZ6PD;hQi=>
Omm1.3 NUS5[2R3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDFOUDPxE1? NYPXTWU3OjRiaB?= NYXqdWVqTE2VTx?= NFfIT5ZqdmS3Y3XzJGcyKGG{cnXzeOKh NEnk[nc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[1N|k3QCd-MkK2OVM6Pjh:L3G+
92.1 MkLJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvJOUDPxE1? MY[yOEBp MmjkSG1UVw>? M1SxVolv\HWlZYOgS|Eh[XK{ZYP0xsA> M3fPWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkWzPVY5Lz5{Mk[1N|k3QDxxYU6=
Mel202 MYTBdI9xfG:|aYOgRZN{[Xl? MnPKOUDPxE1? NHrHZVk4OiCq MUXEUXNQ NGnTNGFqdmS3Y3XzJIFxd3C2b4Ppd{B{dGmpaITsfS=> M1iwelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkWzPVY5Lz5{Mk[1N|k3QDxxYU6=
Omm1.3 Mn\hRZBweHSxc3nzJGF{e2G7 MXy1JO69VQ>? NHO0N3k4OiCq MYHEUXNQ NIDHXHJqdmS3Y3XzJIFxd3C2b4Ppdy=> NFv3SXM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[1N|k3QCd-MkK2OVM6Pjh:L3G+
92.1 MYDBdI9xfG:|aYOgRZN{[Xl? NEfUXHM2KM7:TR?= Ml7rO|IhcA>? M4\6XmROW09? NW\DXoxKcW6mdXPld{BieG:ydH;zbZMhe2mpbnnmZ4FvfGy7 NHzMSoo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[1N|k3QCd-MkK2OVM6Pjh:L3G+
Mel202 NFLuRm5HfW6ldHnvckBCe3OjeR?= M17DPFUh|ryP M3zxSFI1KGh? M1TQZYlvcGmkaYTzJIV5eHKnc4Ppc44h[W6mIIDoc5NxcG:{eXzheIlwdiCxZjDQT2MhcXOxZn;ycZM> NWD1VHJMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2OVM6PjhpPkKyOlU{QTZ6PD;hQi=>
Omm1.3 MlTWSpVv[3Srb36gRZN{[Xl? M1XDcVUh|ryP NHnyc2kzPCCq Ml;xbY5pcWKrdIOg[ZhxemW|c3nvckBidmRicHjvd5Bpd3K7bHH0bY9vKG:oIGDLR{Bqe2:ob4Ltdy=> NV2yfYFERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2OVM6PjhpPkKyOlU{QTZ6PD;hQi=>
92.1 M3z6RWZ2dmO2aX;uJGF{e2G7 MWO1JO69VQ>? M4TwZ|I1KGh? M4raS4lvcGmkaYTzJIV5eHKnc4Ppc44h[W6mIIDoc5NxcG:{eXzheIlwdiCxZjDQT2MhcXOxZn;ycZM> MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ3M{m2PEc,OjJ4NUO5Olg9N2F-
HBL1 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXqwMlE3NTJyIN88US=> M{nHdlUh\A>? NF33[HZKSzVyPUCuOUDPxE1? MmrZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|MkS5NlAoRjJzM{K0PVIxRC:jPh?=
TMD8 NVrQWnJVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\TNE4yPi1{MDFOwG0> M322VVUh\A>? Mn;YTWM2OD1yLkKg{txO M3nOfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{K0PVIxLz5{MUOyOFkzODxxYU6=
OCI-Ly10 NWDINZhCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWewMlE3NTJyIN88US=> MlPSOUBl MXHJR|UxRTFwMzFOwG0> MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN{NEmyNEc,OjF|MkS5NlA9N2F-
U2932 NFf6dWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV2wMlE3NTJyIN88US=> NVizOmpZPSCm MXzJR|UxRTFyIN88US=> MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN{NEmyNEc,OjF|MkS5NlA9N2F-
OCI-Ly3 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2XKV|AvOTZvMkCg{txO NX\yVWUzPSCm MWDJR|Ux97zgMkCg{txO NYTZVoJyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzNlQ6OjBpPkKxN|I1QTJyPD;hQi=>
SuDHL2 NWC2PFRzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLKNE4yPi1{MDFOwG0> M4jlNFUh\A>? M1K4Z2lEPTExvK6yNEDPxE1? MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN{NEmyNEc,OjF|MkS5NlA9N2F-
SuDHL4 NHzXVIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXm2S4hJOC5zNj2yNEDPxE1? NHTmcpE2KGR? MnP2TWM2OO,:nkKwJO69VQ>? MnvlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|MkS5NlAoRjJzM{K0PVIxRC:jPh?=
DB MonJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIX6R4gxNjF4LUKwJO69VQ>? MmPSOUBl MkHwTWM2OO,:nkKwJO69VQ>? MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN{NEmyNEc,OjF|MkS5NlA9N2F-
Jurkat IL-2 M4ntfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn3XTWM2OD14LkexJOKyKDNwN{[g{txO MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl2MEK1PUc,OTl7NECyOVk9N2F-
PBMC IL-2 MnzHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInOWYdKSzVyPUSuPFQhyrFiMT63NEAh|ryP M1rZUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUSwNlU6Lz5zOUm0NFI2QTxxYU6=
Jurkat MYPGeY5kfGmxbjDhd5NigQ>? NWXnZnB1UW6qaXLpeIlwdiCxZjDUR3IwS0R{OD3t[YRq[XSnZDDoeY1idiCWIHPlcIwh[WO2aY\heIlwdiCrbjDKeZJs[XRiY3XscJMh\XiycnXzd4lv\yCqdX3hckBKVDJicILvcY91\XJiYomgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6NCCLQ{WwJF0hOC5yNUSg{txONg>? NWHpWnJQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm4Nlc5OzFpPkG5PFI4QDNzPD;hQi=>
Jurkat T M2HDW2Z2dmO2aX;uJIF{e2G7 NULvXGhHPSCqcoO= NF3lWWtKdmirYnn0bY9vKG:oIGDLR5Rp\XSjIHnuJIh2dWGwIFr1dotifCCWIHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBidnSrLVPEN{9ETDJ6IHHueIljd2S7LXnu[JVk\WRiVD3j[YxtKGGldHn2ZZRqd25iYomgcYVie3W{aX7nJIRm[3KnYYPlJIlvKEmOLUKgd4VkemW2aX;uJIFnfGW{IEWgbJJ{KGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfUwhUUN3MDC9JFAvODhzIN88UU4> MkLlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhzM{G3NVQoRjJ6MUOxO|E1RC:jPh?=
B-cells NH\UWWFHfW6ldHnvckBie3OjeR?= NIDPTpNKdmirYnn0bY9vKG:oIGDLR4JmfGFiaX6gcY92e2ViQjDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4hUWePLYP0bY12dGG2ZXSgZ4VtdCCycn;sbYZmemG2aX;uMEBKSzVyIE2gNE4zOzRizszNMi=> NXnE[3BlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixN|E4OTRpPkK4NVMyPzF2PD;hQi=>
bone marrow cells MW\BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? M{[4WlQh\GG7cx?= NI\xRlJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JGNDSSCvb4Xz[UBjd26nIH3hdpJwfyClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJHs{UF22aIntbYRqdmViaX7jc5Jxd3KjdHnvckBi\nSncjC0JIRigXNuIFnDOVAhRSB|Lkeg{txONg>? NG\OUpY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUiyO|g{OSd-MUm4Nlc5OzF:L3G+
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 2022-01-17)

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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