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 NVPjW4ZvTnWwY4Tpc44hSXO|YYm= NXXwRlJFOTByIH7N NFjiWJI{KGh? M{HCZ2ROW09? MYHpcohq[mm2czDyVm5CKHO7boTo[ZNqew>? M4r3ZlI2PjlzMUW4
HUVECs  NIX3cIdHfW6ldHnvckBCe3OjeR?= MYK1NFBvVQ>? MV:xJIg> NWHtfYVXWmWmdXPld{BFXFhvVILp[4dmemWmIFXu[I91cGWuaXHsJGR6e2[3bnP0bY9v M{DhRVI2PjN2NUO4
A549 NHO1SphHfW6ldHnvckBCe3OjeR?= MX:wMlHDqM7:TR?= Mkn1NlQhcA>? NYrBWIlZ\GWlcnXhd4V{KHSqZTDy[YxifGm4ZTDQT2Mu|rFibHX2[Ywhd25iY3XscEBu\W2kcnHu[UBkd3S{ZXH0[YQhSVNvSW[= MWGyOVIyQDF4MR?=
A549 Mni5SpVv[3Srb36gRZN{[Xl? NH7OSWkxNjIEoN88US=> NWrIdotJOjRiaB?= MXTy[YR2[2W|IITo[UBmgHC{ZYPzbY9vKGyndnXsd{Bw\iCPTWCtNkwhVU2SLUmgZY5lKGmwdHXndolvKM7{MR?= M{i5dlI2OjF6MU[x
A549 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXWwMlHDqM7:TR?= Mn7uNlQhcA>? NFyyU3hmdmijbnPld{Boem:5dHigbY5pcWKrdHnvckBkd3S{ZXH0[YQhf2m2aDDBV{1KXg>? NGHufGszPTJzOEG2NS=>
Mel202 NIjJPI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWD0RmxjOC53IN88US=> M4rSNFMhcA>? NYDIUZRvTE2VTx?= NXfKN21s\W6qYX7j[ZMhUVJvaX7keYNm\CC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHl? MWqyOFU6PTN6NR?=
92.1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHWweYwxNjVizszN MXGzJIg> NHLCT5pFVVOR NX;iWFF2\W6qYX7j[ZMhUVJvaX7keYNm\CC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHl? M1v5TlI1PTl3M{i1
OCM3 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHn3dJIxNjVizszN NVvKSYxlOyCq NE\ndIdFVVOR NHTmcI9mdmijbnPld{BKWi2rbnT1Z4VlKHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gQ>? NG\lS2UzPDV7NUO4OS=>
Mel202 MkLPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;qdWIxNjVizszN NVTlZ4t1OyCq MY\EUXNQ NFv2OGFqdmO{ZXHz[ZMhUVJvaX7keYNm\CClZXzsJIN6[2ynIHHydoV{fMLi MmmzNlQ2QTV|OEW=
92.1 NV7XblV[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFTidG8xNjVizszN M1\J[lMhcA>? MYXEUXNQ NX\OW5VbcW6lcnXhd4V{KEmULXnu[JVk\WRiY3XscEBkgWOuZTDhdpJme3UEoB?= M2TUelI1PTl3M{i1
OCM3 MlLVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUmwMlUh|ryP M2\GRlMhcA>? MnrGSG1UVw>? MYTpcoNz\WG|ZYOgTXIucW6mdXPl[EBk\WyuIHP5Z4xmKGG{cnXzeOKh NFzSO5kzPDV7NUO4OS=>
Jeko-1 NVW3ZnVlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\N[FAuPCEQvF2= NYfKeHd3TE2VTx?= NVfXdWh7cW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? MmfaNlQ{PjJ7M{W=
Mino MlW1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PCbVAuPCEQvF2= NGK0NIhFVVOR M1HySIlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NGH0WWIzPDN4MkmzOS=>
Rec-1 NHHBcXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHGyR2gxNTRizszN NWfaVHdGTE2VTx?= M4rNPYlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NELFeGgzPDN4MkmzOS=>
SP49 NE\VbWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TXPVAuPCEQvF2= MonxSG1UVw>? NWLTNlF6cW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? MnvCNlQ{PjJ7M{W=
Jeko-1 NVzpV3k1TnWwY4Tpc44hSXO|YYm= NH7iVGwzNjVizszNxsA> NIDhTVYyOiCq M4e0UmROW09? Mmrz[I94dnKnZ4XsZZRmeyCQRj5OvmIhfGG{Z3X0JIdmdmW| NGSxTpAzPDN4MkmzOS=>
Mino NEjhWJBHfW6ldHnvckBCe3OjeR?= MVWyMlUh|ryPwrC= M1LvelEzKGh? M{\YXWROW09? MnHE[I94dnKnZ4XsZZRmeyCQRj5OvmIhfGG{Z3X0JIdmdmW| NUn5UYs{OjR|NkK5N|U>
Rec-1 NWe4VG1ZTnWwY4Tpc44hSXO|YYm= MkjLNk42KM7:TdMg MXGxNkBp NVfES|h1TE2VTx?= Mn7U[I94dnKnZ4XsZZRmeyCQRj5OvmIhfGG{Z3X0JIdmdmW| MViyOFM3Ojl|NR?=
SP49 NWrFenJmTnWwY4Tpc44hSXO|YYm= NIHsVW8zNjVizszNxsA> M3;jPFEzKGh? MnXOSG1UVw>? NVTBWohS\G:5boLl[5Vt[XSnczDOSk3PwkJidHHy[4V1KGenbnXz NULnOpZOOjR|NkK5N|U>
CD3+ T  NGT4fYRHfW6ldHnvckBCe3OjeR?= NIjQdYExNTVyMDDuUS=> M1roe|EhcA>? MkfUbY5pcWKrdIOgUmYu|rqEIIDoc5NxcG:{eXzheIlwdiCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MWGyN|U4OzJ6Mx?=
Mel202 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rVcFAuPSEQvF2= M2rJRVczKGh? MoXMSG1UVw>? NFjVcpRqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 MWCyNlY2Ozl4OB?=
Omm1.3 NUi3WFJuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnOe4hoOC13IN88US=> M1HaZlczKGh? NV[xdIN3TE2VTx?= MnXDbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MV2yNlY2Ozl4OB?=
92.1 M1P5Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWewMVUh|ryP NYK1OoNVPzJiaB?= MnzKSG1UVw>? M4XJ[YlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> MVWyNlY2Ozl4OB?=
Mel202 MnznS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTyOUDPxE1? NXO5[nBEOjRiaB?= MXXEUXNQ MUDpcoR2[2W|IFexJIFzemW|dNMg MnnuNlI3PTN7Nki=
Omm1.3 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3PSIp{PSEQvF2= NWPiUGpIOjRiaB?= MXTEUXNQ NWHlblM{cW6mdXPld{BIOSCjcoLld5TDqA>? MXeyNlY2Ozl4OB?=
92.1 NVjQbpZOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknDOUDPxE1? MUSyOEBp MWXEUXNQ NI\HNWNqdmS3Y3XzJGcyKGG{cnXzeOKh NEK2O4czOjZ3M{m2PC=>
Mel202 MUfBdI9xfG:|aYOgRZN{[Xl? M3r3WFUh|ryP NX\KVJptPzJiaB?= NV\3UVFjTE2VTx?= NHPpb2RqdmS3Y3XzJIFxd3C2b4Ppd{B{dGmpaITsfS=> M1PCWFIzPjV|OU[4
Omm1.3 MlTmRZBweHSxc3nzJGF{e2G7 M124UVUh|ryP MXW3NkBp M3zjOmROW09? MUfpcoR2[2W|IHHwc5B1d3Orcx?= M4jpN|IzPjV|OU[4
92.1 MVvBdI9xfG:|aYOgRZN{[Xl? M33DZlUh|ryP NHHyeWc4OiCq MVfEUXNQ M1;5[Ylv\HWlZYOgZZBweHSxc3nzJJNq\26rZnPhcpRtgQ>? NXfOZpdnOjJ4NUO5Olg>
Mel202 NH31R4VHfW6ldHnvckBCe3OjeR?= NUTZW|FtPSEQvF2= NFHOTGQzPCCq NYnubJVzcW6qaXLpeJMh\XiycnXzd4lwdiCjbnSgdIhwe3Cqb4L5cIF1cW:wIH;mJHBMSyCrc3;mc5Juew>? NIrQOXUzOjZ3M{m2PC=>
Omm1.3 NW\pTVViTnWwY4Tpc44hSXO|YYm= M1roTlUh|ryP MlTBNlQhcA>? MUHpcohq[mm2czDlfJBz\XO|aX;uJIFv\CCyaH;zdIhwenmuYYTpc44hd2ZiUFvDJIl{d2[xcn3z MmXuNlI3PTN7Nki=
92.1 NYDzSHc3TnWwY4Tpc44hSXO|YYm= MWW1JO69VQ>? M{PsS|I1KGh? NHSwTppqdmirYnn0d{BmgHC{ZYPzbY9vKGGwZDDwbI9{eGixconsZZRqd25ib3[gVGtEKGm|b3\vdo1{ NXz6c5F5OjJ4NUO5Olg>
HBL1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HJVlAvOTZvMkCg{txO MX61JIQ> MWnJR|UxRTBwNTFOwG0> NInnUnozOTN{NEmyNC=>
TMD8 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrjNE4yPi1{MDFOwG0> NYK1PYc2PSCm NVTOUlBrUUN3ME2wMlIh|ryP NUPzd3RLOjF|MkS5NlA>
OCI-Ly10 MlHFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXGwMlE3NTJyIN88US=> MnzROUBl NHPNXIZKSzVyPUGuN{DPxE1? NHu1UpQzOTN{NEmyNC=>
U2932 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIT3SlExNjF4LUKwJO69VQ>? M4DHSVUh\A>? M1Ty[mlEPTB;MUCg{txO MY[yNVMzPDl{MB?=
OCI-Ly3 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\IeIQxNjF4LUKwJO69VQ>? MWe1JIQ> MmTETWM2OO,:nkKwJO69VQ>? MYKyNVMzPDl{MB?=
SuDHL2 NV3ZWmozT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUHDWnNZOC5zNj2yNEDPxE1? M2C2ZlUh\A>? M2j4TWlEPTExvK6yNEDPxE1? Mn;WNlE{OjR7MkC=
SuDHL4 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2XVRVAvOTZvMkCg{txO Mkm0OUBl NFPHNJdKSzVy78{eNlAh|ryP MoO4NlE{OjR7MkC=
DB NEjYO5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\tNE4yPi1{MDFOwG0> MUe1JIQ> NGDD[G9KSzVy78{eNlAh|ryP MYOyNVMzPDl{MB?=
Jurkat IL-2 M37NOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXNc3ZPUUN3ME22MlcyKMLzIEOuO|Yh|ryP MUixPVk1ODJ3OR?=
PBMC IL-2 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLsZZVKSzVyPUSuPFQhyrFiMT63NEAh|ryP MofWNVk6PDB{NUm=

... 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
NCT01854606 Completed CD79 Mutant or ABC-subtype Diffuse Large B-Cell Lymphoma Novartis Pharmaceuticals|Novartis December 5 2013 Phase 1
NCT02273219 Active not 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
NCT01128335 Completed Liver Transplantation Novartis Pharmaceuticals|Novartis April 2010 Phase 2
NCT00572585 Completed Ulcerative Colitis 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