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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2 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.

Purity & Quality Control

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 MlmzSpVv[3Srb36gRZN{[Xl? MmHpNVAxKG6P MUSzJIg> NUPBXIFbTE2VTx?= NH;QPXdqdmirYnn0d{BzWk6DIIP5cpRp\XOrcx?= MYSyOVY6OTF3OB?=
HUVECs  MXPGeY5kfGmxbjDBd5NigQ>? NF\QOFY2ODCwTR?= MkPPNUBp NFu5WpBT\WS3Y3XzJGRVYC2Wcnnn[4Vz\WRiRX7kc5Rp\WyrYXygSJl{\nWwY4Tpc44> M4fiT|I2PjN2NUO4
A549 MlnnSpVv[3Srb36gRZN{[Xl? M2jPbFAvOcLizszN MmnINlQhcA>? M3jjV4Rm[3KnYYPld{B1cGVicnXsZZRqfmViUFvDMe6yKGyndnXsJI9vKGOnbHygcYVu[nKjbnWgZ491emWjdHXkJGFUNUmY MU[yOVIyQDF4MR?=
A549 MmHlSpVv[3Srb36gRZN{[Xl? MWmwMlHDqM7:TR?= MoX4NlQhcA>? Mnu1doVlfWOnczD0bIUh\XiycnXzd4lwdiCuZY\lcJMhd2ZiTV3QMVItKE2PUD25JIFv\CCrboTl[5JqdiEQskG= MorCNlUzOThzNkG=
A549 NYf4XIhuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXseGE5OC5zwrFOwG0> Mn[5NlQhcA>? MnXD[Y5p[W6lZYOg[5Jwf3SqIHnubIljcXSrb36gZ491emWjdHXkJJdqfGhiQWOtTXY> NYrKVFRUOjV{MUixOlE>
Mel202 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUiwV4xwOC53IN88US=> MmP5N{Bp NIfw[4VFVVOR NYHMWmxv\W6qYX7j[ZMhUVJvaX7keYNm\CC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHl? MV[yOFU6PTN6NR?=
92.1 M1;uTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnydW5xOC53IN88US=> MYizJIg> NXHafmZvTE2VTx?= MWDlcohidmOnczDJVk1qdmS3Y3XkJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fS=> MnLZNlQ2QTV|OEW=
OCM3 MlvQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXGwMlUh|ryP NF7qS5Y{KGh? MVrEUXNQ NXvuV4Fu\W6qYX7j[ZMhUVJvaX7keYNm\CC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHl? MVOyOFU6PTN6NR?=
Mel202 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUOwMlUh|ryP MXGzJIg> NVzF[IZrTE2VTx?= NFXOO|hqdmO{ZXHz[ZMhUVJvaX7keYNm\CClZXzsJIN6[2ynIHHydoV{fMLi MnHKNlQ2QTV|OEW=
92.1 NXqyd4NRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH[zUIExNjVizszN M162XVMhcA>? M2fBPGROW09? NF7WW4RqdmO{ZXHz[ZMhUVJvaX7keYNm\CClZXzsJIN6[2ynIHHydoV{fMLi MnjiNlQ2QTV|OEW=
OCM3 MnPOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILpfGkxNjVizszN NFq1N4c{KGh? NFn6blNFVVOR NULXfGJkcW6lcnXhd4V{KEmULXnu[JVk\WRiY3XscEBkgWOuZTDhdpJme3UEoB?= MnjPNlQ2QTV|OEW=
Jeko-1 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVuwMVQh|ryP NFnncm1FVVOR NIHzemRqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 M{nFblI1OzZ{OUO1
Mino M1j6W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXf0OGJXOC12IN88US=> MYjEUXNQ MlXCbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NXX2VHZvOjR|NkK5N|U>
Rec-1 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPIVmoxNTRizszN MYrEUXNQ M3XHb4lvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NXPuO5J4OjR|NkK5N|U>
SP49 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWT0UosxOC12IN88US=> MlrQSG1UVw>? MUTpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 M4Wxc|I1OzZ{OUO1
Jeko-1 Mm[xSpVv[3Srb36gRZN{[Xl? MV:yMlUh|ryPwrC= NI[xWWQyOiCq MlHCSG1UVw>? NInrelFld3ewcnXneYxifGW|IF7GMe67SiC2YYLn[ZQh\2WwZYO= NWHvdZp3OjR|NkK5N|U>
Mino M2TTUGZ2dmO2aX;uJGF{e2G7 NVvLZ2Q{Oi53IN88UeKh NYfjPJUyOTJiaB?= MXTEUXNQ M2rhR4Rwf26{ZXf1cIF1\XNiTl[t{tpDKHSjcnfleEBo\W6ncx?= M1iyPVI1OzZ{OUO1
Rec-1 NXy5TGZ2TnWwY4Tpc44hSXO|YYm= NY\WNWN7Oi53IN88UeKh MmfjNVIhcA>? NWPOd4lsTE2VTx?= NFTtUXBld3ewcnXneYxifGW|IF7GMe67SiC2YYLn[ZQh\2WwZYO= M3HCT|I1OzZ{OUO1
SP49 MkDCSpVv[3Srb36gRZN{[Xl? NFnudWYzNjVizszNxsA> Mnn1NVIhcA>? M2j3W2ROW09? M2X2dYRwf26{ZXf1cIF1\XNiTl[t{tpDKHSjcnfleEBo\W6ncx?= MkTHNlQ{PjJ7M{W=
CD3+ T  MV7GeY5kfGmxbjDBd5NigQ>? MWGwMVUxOCCwTR?= NU\VbYtNOSCq NV3q[XlKcW6qaXLpeJMhVkZvzsrCJJBpd3OyaH;yfYxifGmxbjDpckBiKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= MU[yN|U4OzJ6Mx?=
Mel202 NV7IU5NmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHpNE02KM7:TR?= NHzWfpE4OiCq M1vhNGROW09? Mm\1bY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MUeyNlY2Ozl4OB?=
Omm1.3 M3LqUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4P0NFAuPSEQvF2= NXnodlhsPzJiaB?= NFXt[5BFVVOR NX62SWJycW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NYjve2o{OjJ4NUO5Olg>
92.1 MnXQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\HV2ExNTVizszN NIrjRm44OiCq M3XmSWROW09? MonqbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NWjrdo9YOjJ4NUO5Olg>
Mel202 M3q1R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfMeJFnPSEQvF2= MmfvNlQhcA>? NULsdIgyTE2VTx?= NFHBWJpqdmS3Y3XzJGcyKGG{cnXzeOKh MnvZNlI3PTN7Nki=
Omm1.3 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPxbppvPSEQvF2= MorUNlQhcA>? MV;EUXNQ MVfpcoR2[2W|IFexJIFzemW|dNMg MmHCNlI3PTN7Nki=
92.1 NXXv[mU{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPZXoptPSEQvF2= MknkNlQhcA>? MkDkSG1UVw>? MW\pcoR2[2W|IFexJIFzemW|dNMg MWeyNlY2Ozl4OB?=
Mel202 NI\weJlCeG:ydH;zbZMhSXO|YYm= Mk\nOUDPxE1? MnXMO|IhcA>? NFX5bGVFVVOR MlTBbY5lfWOnczDhdI9xfG:|aYOgd4xq\2i2bIm= MoDnNlI3PTN7Nki=
Omm1.3 MXrBdI9xfG:|aYOgRZN{[Xl? M2XIN|Uh|ryP NWG3bYZMPzJiaB?= NYHyfFNvTE2VTx?= NV;3S5JzcW6mdXPld{BieG:ydH;zbZM> M1XLOlIzPjV|OU[4
92.1 M1ixdWFxd3C2b4Ppd{BCe3OjeR?= MYW1JO69VQ>? MVW3NkBp Mnj2SG1UVw>? M2W5Zolv\HWlZYOgZZBweHSxc3nzJJNq\26rZnPhcpRtgQ>? M4r3OVIzPjV|OU[4
Mel202 Mn:3SpVv[3Srb36gRZN{[Xl? MnrTOUDPxE1? NXXTU25FOjRiaB?= NIWyc|VqdmirYnn0d{BmgHC{ZYPzbY9vKGGwZDDwbI9{eGixconsZZRqd25ib3[gVGtEKGm|b3\vdo1{ M{LUOVIzPjV|OU[4
Omm1.3 Ml\ESpVv[3Srb36gRZN{[Xl? MknjOUDPxE1? MkGzNlQhcA>? M3LydYlvcGmkaYTzJIV5eHKnc4Ppc44h[W6mIIDoc5NxcG:{eXzheIlwdiCxZjDQT2MhcXOxZn;ycZM> MUSyNlY2Ozl4OB?=
92.1 NGq5R5FHfW6ldHnvckBCe3OjeR?= MlTDOUDPxE1? MVqyOEBp NVz0T5NNcW6qaXLpeJMh\XiycnXzd4lwdiCjbnSgdIhwe3Cqb4L5cIF1cW:wIH;mJHBMSyCrc3;mc5Juew>? NIPQc2MzOjZ3M{m2PC=>
HBL1 M1nxUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTZU2pDOC5zNj2yNEDPxE1? MnXVOUBl MoDJTWM2OD1yLkWg{txO NH32eoszOTN{NEmyNC=>
TMD8 NHm4WItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPxNE4yPi1{MDFOwG0> MXS1JIQ> NWHmeoQzUUN3ME2wMlIh|ryP M{DXWVIyOzJ2OUKw
OCI-Ly10 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;FTGFoOC5zNj2yNEDPxE1? MojROUBl NETQdIVKSzVyPUGuN{DPxE1? NYXX[HRsOjF|MkS5NlA>
U2932 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV:wMlE3NTJyIN88US=> MoPMOUBl M3nzZWlEPTB;MUCg{txO NWfBXJFPOjF|MkS5NlA>
OCI-Ly3 M1nPXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{LOTlAvOTZvMkCg{txO Mkf6OUBl NED2eHJKSzVy78{eNlAh|ryP NHTWfGwzOTN{NEmyNC=>
SuDHL2 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYCwMlE3NTJyIN88US=> NV:yUZhrPSCm MmXLTWM2OO,:nkKwJO69VQ>? MlzWNlE{OjR7MkC=
SuDHL4 M1v1PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPHNE4yPi1{MDFOwG0> MXe1JIQ> Mo\ZTWM2OO,:nkKwJO69VQ>? NHHwV3EzOTN{NEmyNC=>
DB M2XqcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVOwMlE3NTJyIN88US=> NUDhN|c2PSCm M3njUGlEPTExvK6yNEDPxE1? M3fVZVIyOzJ2OUKw
Jurkat IL-2 NYfJN4tHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXXQRopuUUN3ME22MlcyKMLzIEOuO|Yh|ryP NHf4RlMyQTl2MEK1PS=>
PBMC IL-2 MoLpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFPKV5lKSzVyPUSuPFQhyrFiMT63NEAh|ryP NHn0VYoyQTl2MEK1PS=>

... 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
+ 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 <1 mg/mL
In vivo 2% DMSO+30% PEG 300+ddH2O 10mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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
NCT02273219 Recruiting Uveal Melanoma Richard D. Carvajal|Columbia University November 2014 Phase 1
NCT01854606 Active, not recruiting CD79 Mutant or ABC-subtype Diffuse Large B-Cell Lymphoma Novartis Pharmaceuticals|Novartis December 2013 Phase 1|Phase 2
NCT01801358 Terminated Uveal Melanoma Array BioPharma August 2013 Phase 1|Phase 2
NCT01430416 Recruiting Uveal Melanoma Novartis Pharmaceuticals|Novartis December 2011 Phase 1
NCT01402440 Terminated Diffuse Large B-Cell Lymphoma Novartis Pharmaceuticals|Novartis November 2011 Phase 1
NCT00572585 Terminated 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.

PKC Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID