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
USD 170 In stock
USD 670 In stock
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4 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.

    Western blotting analysis of FLT3ePIM-1 signaling in MV4-11 cells treated with increasing concentrations of SGI-1776, quizartinib, or sotrastaurin for 24 h.

    Biochem Biophys Res Commun, 2018, 10.1016/j.bbrc.2018.07.049. 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 M2rZTWZ2dmO2aX;uJGF{e2G7 MUKxNFAhdk1? NEfjWlM{KGh? MlG3SG1UVw>? M{PWRolvcGmkaYTzJJJTVkFic4nueIhme2m| NXH0[ZEzOjV4OUGxOVg>
HUVECs  NIHyXZFHfW6ldHnvckBCe3OjeR?= MnfROVAxdk1? MleyNUBp NV\RN45TWmWmdXPld{BFXFhvVILp[4dmemWmIFXu[I91cGWuaXHsJGR6e2[3bnP0bY9v NYHpfWNXOjV4M{S1N|g>
A549 Mo\zSpVv[3Srb36gRZN{[Xl? MkT5NE4yyqEQvF2= NUjNW255OjRiaB?= M4XjfIRm[3KnYYPld{B1cGVicnXsZZRqfmViUFvDMe6yKGyndnXsJI9vKGOnbHygcYVu[nKjbnWgZ491emWjdHXkJGFUNUmY M4m2cVI2OjF6MU[x
A549 MX;GeY5kfGmxbjDBd5NigQ>? MXGwMlHDqM7:TR?= NVjPdGZVOjRiaB?= MYDy[YR2[2W|IITo[UBmgHC{ZYPzbY9vKGyndnXsd{Bw\iCPTWCtNkwhVU2SLUmgZY5lKGmwdHXndolvKM7{MR?= NX3McY56OjV{MUixOlE>
A549 M2ezSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjzTIVSOC5zwrFOwG0> MVKyOEBp Mlrn[Y5p[W6lZYOg[5Jwf3SqIHnubIljcXSrb36gZ491emWjdHXkJJdqfGhiQWOtTXY> MnfmNlUzOThzNkG=
Mel202 MljzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2Xzc|AvPSEQvF2= NEHG[Zo{KGh? MnH4SG1UVw>? Mn3J[Y5p[W6lZYOgTXIucW6mdXPl[EBz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJk> MkT0NlQ2QTV|OEW=
92.1 NHnNPXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVywMlUh|ryP NFrCWpg{KGh? Mn7DSG1UVw>? NUK1UFZS\W6qYX7j[ZMhUVJvaX7keYNm\CC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHl? NHKwVYczPDV7NUO4OS=>
OCM3 NFjK[G9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkHHNE42KM7:TR?= NYTyO414OyCq MXHEUXNQ MknS[Y5p[W6lZYOgTXIucW6mdXPl[EBz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJk> NGG5dIEzPDV7NUO4OS=>
Mel202 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\odFAvPSEQvF2= NFjGPYI{KGh? M2q4emROW09? M{\uSYlv[3KnYYPld{BKWi2rbnT1Z4VlKGOnbHygZ5lkdGViYYLy[ZN1yqB? MoTkNlQ2QTV|OEW=
92.1 MlLQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\IcHIxNjVizszN MoH0N{Bp M1uzNmROW09? M13CN4lv[3KnYYPld{BKWi2rbnT1Z4VlKGOnbHygZ5lkdGViYYLy[ZN1yqB? NHLOS5EzPDV7NUO4OS=>
OCM3 NFns[FVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHyNE42KM7:TR?= NHjvXZk{KGh? MX3EUXNQ NETQO|dqdmO{ZXHz[ZMhUVJvaX7keYNm\CClZXzsJIN6[2ynIHHydoV{fMLi NGri[IIzPDV7NUO4OS=>
Jeko-1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWiwMVQh|ryP M1zJfWROW09? NFzsUVBqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 M2GzRVI1OzZ{OUO1
Mino MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvyN|Y6OC12IN88US=> M2rqVGROW09? MYXpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 Ml[1NlQ{PjJ7M{W=
Rec-1 M3G1dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYWwMVQh|ryP NFG4bVVFVVOR MXnpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MVuyOFM3Ojl|NR?=
SP49 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\nTVAuPCEQvF2= MnjySG1UVw>? MmDGbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> M1PqSFI1OzZ{OUO1
Jeko-1 M3jNVmZ2dmO2aX;uJGF{e2G7 MYGyMlUh|ryPwrC= NULZN|hVOTJiaB?= MXrEUXNQ MlzS[I94dnKnZ4XsZZRmeyCQRj5OvmIhfGG{Z3X0JIdmdmW| M{jWflI1OzZ{OUO1
Mino NW\oRXU3TnWwY4Tpc44hSXO|YYm= NEXFcpAzNjVizszNxsA> NUnyWY14OTJiaB?= MlPsSG1UVw>? MUnkc5dvemWpdXzheIV{KE6ILd86RkB1[XKpZYSg[4Vv\XN? NGjnW|MzPDN4MkmzOS=>
Rec-1 MmTtSpVv[3Srb36gRZN{[Xl? M17QfVIvPSEQvF5CpC=> NIXvUJUyOiCq NVrnRVhITE2VTx?= MULkc5dvemWpdXzheIV{KE6ILd86RkB1[XKpZYSg[4Vv\XN? MmDrNlQ{PjJ7M{W=
SP49 M4HoUGZ2dmO2aX;uJGF{e2G7 NWf4clhZOi53IN88UeKh NEDaVWoyOiCq NWrOc5gyTE2VTx?= M2rR[YRwf26{ZXf1cIF1\XNiTl[t{tpDKHSjcnfleEBo\W6ncx?= MlqzNlQ{PjJ7M{W=
CD3+ T  M4XWdmZ2dmO2aX;uJGF{e2G7 M2iwR|AuPTByIH7N NHnsRooyKGh? M3noSolvcGmkaYTzJG5HNc78QjDwbI9{eGixconsZZRqd25iaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MkK1NlM2PzN{OEO=
Mel202 NXW1UY5FT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjCNE02KM7:TR?= MVu3NkBp MnXhSG1UVw>? MlmzbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NIjQO5MzOjZ3M{m2PC=>
Omm1.3 NYSzNZVbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml71NE02KM7:TR?= M{XB[VczKGh? MXnEUXNQ NU\TO2pscW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NYW3dIRXOjJ4NUO5Olg>
92.1 MonxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXuwMVUh|ryP NI\mR3I4OiCq MmKzSG1UVw>? NEHk[GNqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 MW[yNlY2Ozl4OB?=
Mel202 MlrtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUS1JO69VQ>? MlPtNlQhcA>? MkjGSG1UVw>? Mmr2bY5lfWOnczDHNUBienKnc4VCpC=> MXqyNlY2Ozl4OB?=
Omm1.3 NYXmdGdYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPYXlEyPSEQvF2= NVHHelM1OjRiaB?= MVfEUXNQ M3jqWolv\HWlZYOgS|Eh[XK{ZYP0xsA> MnzmNlI3PTN7Nki=
92.1 NGq5b4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWq1JO69VQ>? NHnIVWkzPCCq MWnEUXNQ M{\NdIlv\HWlZYOgS|Eh[XK{ZYP0xsA> NYXsfXdDOjJ4NUO5Olg>
Mel202 NYPiXnd2SXCxcITvd4l{KEG|c3H5 MXy1JO69VQ>? NGrJT2U4OiCq MlXrSG1UVw>? MULpcoR2[2W|IHHwc5B1d3OrczDzcIlocHSueR?= NY\VeVd[OjJ4NUO5Olg>
Omm1.3 MkXGRZBweHSxc3nzJGF{e2G7 M3\3N|Uh|ryP NHnufm44OiCq Mmf1SG1UVw>? MULpcoR2[2W|IHHwc5B1d3Orcx?= MYmyNlY2Ozl4OB?=
92.1 NYro[WZUSXCxcITvd4l{KEG|c3H5 NECzdZo2KM7:TR?= NHzEOI84OiCq NFe2e21FVVOR M1;XTIlv\HWlZYOgZZBweHSxc3nzJJNq\26rZnPhcpRtgQ>? NFXINIEzOjZ3M{m2PC=>
Mel202 M3i4cGZ2dmO2aX;uJGF{e2G7 M3vvVFUh|ryP MlfMNlQhcA>? NWP0ZlA3cW6qaXLpeJMh\XiycnXzd4lwdiCjbnSgdIhwe3Cqb4L5cIF1cW:wIH;mJHBMSyCrc3;mc5Juew>? NV\O[mV3OjJ4NUO5Olg>
Omm1.3 NXzvUnJ{TnWwY4Tpc44hSXO|YYm= Mmm4OUDPxE1? MWeyOEBp NX7EcI8{cW6qaXLpeJMh\XiycnXzd4lwdiCjbnSgdIhwe3Cqb4L5cIF1cW:wIH;mJHBMSyCrc3;mc5Juew>? NI[5U3UzOjZ3M{m2PC=>
92.1 M2n6eWZ2dmO2aX;uJGF{e2G7 NE\DZ5Y2KM7:TR?= MU[yOEBp NWDYVZpqcW6qaXLpeJMh\XiycnXzd4lwdiCjbnSgdIhwe3Cqb4L5cIF1cW:wIH;mJHBMSyCrc3;mc5Juew>? M2j0R|IzPjV|OU[4
HBL1 MnrYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXFNE4yPi1{MDFOwG0> MknkOUBl NWXvb5VrUUN3ME2wMlUh|ryP NY[5dlFQOjF|MkS5NlA>
TMD8 M4DEZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFvyRYUxNjF4LUKwJO69VQ>? MmDKOUBl NEXFSG1KSzVyPUCuNkDPxE1? M1\3flIyOzJ2OUKw
OCI-Ly10 NEHGPJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\NWVAvOTZvMkCg{txO NYW5T|ZmPSCm NYXQSWpPUUN3ME2xMlMh|ryP M4H1flIyOzJ2OUKw
U2932 NHjmUW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjTWnhJOC5zNj2yNEDPxE1? MmnZOUBl M4jJcmlEPTB;MUCg{txO MkDrNlE{OjR7MkC=
OCI-Ly3 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLRdoJYOC5zNj2yNEDPxE1? NHz2THc2KGR? M{CwXmlEPTExvK6yNEDPxE1? MWCyNVMzPDl{MB?=
SuDHL2 NFjJN5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jQNFAvOTZvMkCg{txO NGHEUFE2KGR? MVnJR|Ux97zgMkCg{txO MUGyNVMzPDl{MB?=
SuDHL4 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\QVI4xNjF4LUKwJO69VQ>? MnLuOUBl M1\YRmlEPTExvK6yNEDPxE1? M1jDUlIyOzJ2OUKw
DB MljoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3fOblAvOTZvMkCg{txO M3jUcVUh\A>? M3e3emlEPTExvK6yNEDPxE1? M{jJSlIyOzJ2OUKw
Jurkat IL-2 NYXubZBiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnzuTWM2OD14LkexJOKyKDNwN{[g{txO Ml7KNVk6PDB{NUm=
PBMC IL-2 NUTZV29CT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTRwOESgxtEhOS55MDCg{txO NWLFOYlLOTl7NECyOVk>

... 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 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 AEB071

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02285244 Withdrawn Prolymphocytic Leukemia|Recurrent Mantle Cell Lymphoma|Recurrent Small Lymphocytic Lymphoma|Refractory Chronic Lymphocytic Leukemia|Richter Syndrome James Blachly|Novartis|Ohio State University Comprehensive Cancer Center March 12 2015 Phase 2
NCT02273219 Active not recruiting Uveal Melanoma Richard D. Carvajal|Columbia University November 2014 Phase 1
NCT01854606 Completed CD79 Mutant or ABC-subtype Diffuse Large B-Cell Lymphoma Novartis Pharmaceuticals|Novartis December 5 2013 Phase 1
NCT01801358 Terminated Uveal Melanoma Array BioPharma August 2013 Phase 1|Phase 2
NCT01430416 Active not recruiting Uveal Melanoma Novartis Pharmaceuticals|Novartis December 20 2011 Phase 1
NCT01402440 Terminated 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

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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