Sotrastaurin

Catalog No.S2791 Synonyms: AEB071

Sotrastaurin Chemical Structure

Molecular Weight(MW): 438.48

Sotrastaurin 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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In DMSO USD 190 In stock
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3 Customer Reviews

  • Lysates from H3122 and MGH006 cells treated with 1 µM PMA in the presence or absence of 0.3 µM sotrastaurin (SOT) were fractionated. Immunoblotting was performed with the indicated antibodies.

    Cancer Cell, 2015, 27(3): 397-408 . Sotrastaurin purchased from Selleck.

    J-Lat A2 cells were stimulated by TPA (10 nM) for 24 h in the presence of the indicated concentrations of AUY922 and sotrastaurin, alone or in combination. Samples were analyzed by FACS and data plotted using MacSynergy II software. (A) Representative McSynergy II plot: areas of the graph above zero indicate an additive or synergistic effect. (B) Representative checkerboard grid used to calculate the plot shown in A.

    Proc Natl Acad Sci USA, 2014, 111(15): E1528-37. Sotrastaurin purchased from Selleck.

  • Primary mantle cell lymphoma (MCL) cells respond differentially to sotrastaurin and ibrutinib. Primary MCL cells (MCL01-MCL04) were treated with 3 μmol/l sotrastaurin or 400 nmol/l ibrutinib for 2 h (A) or 22 h (B) followed by a stimulation with 3 μg/ml anti-human IgM antibody for 10 min. Subsequently whole cell lysates were analysed by Western blotting. DMSO, dimethyl sulphoxide.

    Br J Haematol, 2016, 173(3):394-403. Sotrastaurin purchased from Selleck.

Purity & Quality Control

Choose Selective PKC Inhibitors

Biological Activity

Description Sotrastaurin 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 MmjTSpVv[3Srb36gRZN{[Xl? NFT2fFAyODBibl2= NGLjUXc{KGh? NGK0[pRFVVOR MYrpcohq[mm2czDyVm5CKHO7boTo[ZNqew>? M1\nflI2PjlzMUW4
HUVECs  MV7GeY5kfGmxbjDBd5NigQ>? MXO1NFBvVQ>? NF65Xo4yKGh? NUnM[VhTWmWmdXPld{BFXFhvVILp[4dmemWmIFXu[I91cGWuaXHsJGR6e2[3bnP0bY9v NH\qd5czPTZ|NEWzPC=>
A549 M3PnZ2Z2dmO2aX;uJGF{e2G7 NV;YR3JlOC5zwrFOwG0> M4DlOFI1KGh? MULk[YNz\WG|ZYOgeIhmKHKnbHH0bZZmKFCNQz5OtUBt\X[nbDDvckBk\WyuIH3lcYJz[W6nIHPveJJm[XSnZDDBV{1KXg>? MXKyOVIyQDF4MR?=
A549 MXzGeY5kfGmxbjDBd5NigQ>? M2jQ[VAvOcLizszN MnW3NlQhcA>? MYPy[YR2[2W|IITo[UBmgHC{ZYPzbY9vKGyndnXsd{Bw\iCPTWCtNkwhVU2SLUmgZY5lKGmwdHXndolvKM7{MR?= M4q0T|I2OjF6MU[x
A549 M1zCfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYqwMlHDqM7:TR?= MnTqNlQhcA>? MXHlcohidmOnczDndo94fGhiaX7obYJqfGmxbjDjc5Rz\WG2ZXSge4l1cCCDUz3JWi=> MWWyOVIyQDF4MR?=
Mel202 M3LzNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnnJNE42KM7:TR?= MXGzJIg> MkfySG1UVw>? NYHlTnlN\W6qYX7j[ZMhUVJvaX7keYNm\CC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHl? NWTncXhPOjR3OUWzPFU>
92.1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLP[JExNjVizszN M3\r[FMhcA>? MYfEUXNQ MmPt[Y5p[W6lZYOgTXIucW6mdXPl[EBz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJk> M2m1R|I1PTl3M{i1
OCM3 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml7ENE42KM7:TR?= MmOzN{Bp M4TuemROW09? NHnyPHdmdmijbnPld{BKWi2rbnT1Z4VlKHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gQ>? NWrYSGYyOjR3OUWzPFU>
Mel202 M3zqVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnZWWZYOC53IN88US=> NWnPUHZTOyCq NEfYUmZFVVOR M{T1Wolv[3KnYYPld{BKWi2rbnT1Z4VlKGOnbHygZ5lkdGViYYLy[ZN1yqB? NUDqT5dnOjR3OUWzPFU>
92.1 NHPIT4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPvPXYxNjVizszN NXT4W3YzOyCq NWLZWZdpTE2VTx?= MX3pcoNz\WG|ZYOgTXIucW6mdXPl[EBk\WyuIHP5Z4xmKGG{cnXzeOKh NUfkeVR{OjR3OUWzPFU>
OCM3 NE[4TIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGfaV5oxNjVizszN MUGzJIg> MmTPSG1UVw>? M2rKUYlv[3KnYYPld{BKWi2rbnT1Z4VlKGOnbHygZ5lkdGViYYLy[ZN1yqB? NX;kdJJrOjR3OUWzPFU>
Jeko-1 NIHDTYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUHJbZFtOC12IN88US=> MYnEUXNQ NFPTVJZqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 M3fjWVI1OzZ{OUO1
Mino NWXoT2dvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVjlSZRUOC12IN88US=> M{LR[GROW09? NXvFd2hHcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NFuzNWkzPDN4MkmzOS=>
Rec-1 NIHER3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLCbIwxNTRizszN NWHENohuTE2VTx?= NHTa[ZhqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 MWOyOFM3Ojl|NR?=
SP49 NYLvd3NiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13NUFAuPCEQvF2= MXXEUXNQ M{TmTYlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NWS1W5ZbOjR|NkK5N|U>
Jeko-1 NHj3T2pHfW6ldHnvckBCe3OjeR?= NHTJeHYzNjVizszNxsA> MmL1NVIhcA>? MmnISG1UVw>? M2LaU4Rwf26{ZXf1cIF1\XNiTl[t{tpDKHSjcnfleEBo\W6ncx?= MljiNlQ{PjJ7M{W=
Mino MX\GeY5kfGmxbjDBd5NigQ>? Ml\wNk42KM7:TdMg MoLyNVIhcA>? MXXEUXNQ Mkez[I94dnKnZ4XsZZRmeyCQRj5OvmIhfGG{Z3X0JIdmdmW| M3;JNVI1OzZ{OUO1
Rec-1 NXHicHBoTnWwY4Tpc44hSXO|YYm= M1Pw[|IvPSEQvF5CpC=> MkHNNVIhcA>? MUTEUXNQ MXfkc5dvemWpdXzheIV{KE6ILd86RkB1[XKpZYSg[4Vv\XN? MmjvNlQ{PjJ7M{W=
SP49 NHPLZWZHfW6ldHnvckBCe3OjeR?= NITKXJIzNjVizszNxsA> NXn6TJFGOTJiaB?= MorwSG1UVw>? MnjG[I94dnKnZ4XsZZRmeyCQRj5OvmIhfGG{Z3X0JIdmdmW| NXLzS|NIOjR|NkK5N|U>
CD3+ T  MXjGeY5kfGmxbjDBd5NigQ>? M1XOclAuPTByIH7N M3fCXlEhcA>? M{DaNolvcGmkaYTzJG5HNc78QjDwbI9{eGixconsZZRqd25iaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? M4i4PFI{PTd|Mkiz
Mel202 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWewMVUh|ryP NVPhd29NPzJiaB?= MYLEUXNQ MWHpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MoPJNlI3PTN7Nki=
Omm1.3 NHj5W3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHHHTY8xNTVizszN NYLQXnVNPzJiaB?= NF7PU3ZFVVOR NYX1[G14cW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NVT5SXZxOjJ4NUO5Olg>
92.1 NILkXWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfqNE02KM7:TR?= MVS3NkBp M33wSGROW09? MV\pcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NWfWfGw3OjJ4NUO5Olg>
Mel202 M4LMS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFn2S|E2KM7:TR?= NUjN[2lNOjRiaB?= MonYSG1UVw>? NHntRpdqdmS3Y3XzJGcyKGG{cnXzeOKh MlLkNlI3PTN7Nki=
Omm1.3 MoHOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXO1JO69VQ>? M1nvSlI1KGh? M3PmOGROW09? MofUbY5lfWOnczDHNUBienKnc4VCpC=> M1foUVIzPjV|OU[4
92.1 NGfjOXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTldpZMPSEQvF2= MWWyOEBp NG[5TJdFVVOR MYrpcoR2[2W|IFexJIFzemW|dNMg MUKyNlY2Ozl4OB?=
Mel202 MVHBdI9xfG:|aYOgRZN{[Xl? M4q1NlUh|ryP MUe3NkBp NXTxemw{TE2VTx?= Mnr3bY5lfWOnczDhdI9xfG:|aYOgd4xq\2i2bIm= NVnrOFBoOjJ4NUO5Olg>
Omm1.3 M3G1d2Fxd3C2b4Ppd{BCe3OjeR?= MYW1JO69VQ>? NFLXd2Q4OiCq MV7EUXNQ MorTbY5lfWOnczDhdI9xfG:|aYO= MVyyNlY2Ozl4OB?=
92.1 MlvURZBweHSxc3nzJGF{e2G7 MWS1JO69VQ>? MofqO|IhcA>? MWPEUXNQ MX3pcoR2[2W|IHHwc5B1d3OrczDzbYdvcW[lYX70cJk> M3:1VVIzPjV|OU[4
Mel202 M2PVXmZ2dmO2aX;uJGF{e2G7 MX[1JO69VQ>? MV6yOEBp MkfSbY5pcWKrdIOg[ZhxemW|c3nvckBidmRicHjvd5Bpd3K7bHH0bY9vKG:oIGDLR{Bqe2:ob4Ltdy=> MVOyNlY2Ozl4OB?=
Omm1.3 MnTySpVv[3Srb36gRZN{[Xl? NIT3eYk2KM7:TR?= NEH2XoIzPCCq MVzpcohq[mm2czDlfJBz\XO|aX;uJIFv\CCyaH;zdIhwenmuYYTpc44hd2ZiUFvDJIl{d2[xcn3z MVeyNlY2Ozl4OB?=
92.1 NYmzXJR7TnWwY4Tpc44hSXO|YYm= Ml[4OUDPxE1? M3zrTlI1KGh? MnW5bY5pcWKrdIOg[ZhxemW|c3nvckBidmRicHjvd5Bpd3K7bHH0bY9vKG:oIGDLR{Bqe2:ob4Ltdy=> M3X0WFIzPjV|OU[4
HBL1 Mnm0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\2OlAvOTZvMkCg{txO MV[1JIQ> MULJR|UxRTBwNTFOwG0> NUPDco5ZOjF|MkS5NlA>
TMD8 NInzTplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fUdlAvOTZvMkCg{txO M4D6TlUh\A>? MkDVTWM2OD1yLkKg{txO MlfyNlE{OjR7MkC=
OCI-Ly10 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\kO|AvOTZvMkCg{txO NF\4T|M2KGR? MXvJR|UxRTFwMzFOwG0> NYfTblNIOjF|MkS5NlA>
U2932 M1:ySWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYmyemhPOC5zNj2yNEDPxE1? M4rlVVUh\A>? MVvJR|UxRTFyIN88US=> M{OyclIyOzJ2OUKw
OCI-Ly3 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHYNE4yPi1{MDFOwG0> MUO1JIQ> MlfZTWM2OO,:nkKwJO69VQ>? M1TWSlIyOzJ2OUKw
SuDHL2 Ml\OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vHR|AvOTZvMkCg{txO NFzlOXE2KGR? M1PwfmlEPTExvK6yNEDPxE1? NWn5VZMxOjF|MkS5NlA>
SuDHL4 Ml\pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYjKZWpxOC5zNj2yNEDPxE1? MWS1JIQ> NYXGO|NLUUN3MP-8olIxKM7:TR?= NW\R[YRYOjF|MkS5NlA>
DB NUjySVZQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIGyT40xNjF4LUKwJO69VQ>? M4DMUlUh\A>? NX2yXZhlUUN3MP-8olIxKM7:TR?= NHPiR5YzOTN{NEmyNC=>
Jurkat IL-2 M4i2[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWLJR|UxRTZwN{GgxtEhOy55NjFOwG0> MoXwNVk6PDB{NUm=
PBMC IL-2 NYi3eWw4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmHDTWM2OD12Lki0JOKyKDFwN{CgJO69VQ>? MXqxPVk1ODJ3OR?=

... Click to View More Cell Line Experimental Data

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]
+ Expand
  • Animal Models: male Wistar/F rats
  • Formulation: Saline
  • 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 individually and in order:
2% DMSO+30% PEG 300+ddH2O
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
Synonyms AEB071

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01854606 Completed CD79 Mutant or ABC-subtype Diffuse Large B-Cell Lymphoma Novartis Pharmaceuticals|Novartis December 5, 2013 Phase 1|Phase 2
NCT02273219 Recruiting Uveal Melanoma Richard D. Carvajal|Columbia University November 2014 Phase 1
NCT01801358 Terminated Uveal Melanoma Array BioPharma August 2013 Phase 1|Phase 2
NCT01402440 Terminated Diffuse Large B-Cell Lymphoma Novartis Pharmaceuticals|Novartis November 2011 Phase 1
NCT00572585 Completed Ulcerative Colitis Novartis Pharmaceuticals|Novartis April 2010 Phase 2
NCT01128335 Completed Liver Transplantation Novartis Pharmaceuticals|Novartis April 2010 Phase 2

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID