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 NGLWRZhHfW6ldHnvckBCe3OjeR?= M{fJU|ExOCCwTR?= MWSzJIg> MUfEUXNQ NUHwdXhmcW6qaXLpeJMhelKQQTDzfY51cGW|aYO= NI\5dmgzPTZ7MUG1PC=>
HUVECs  NEjtXXdHfW6ldHnvckBCe3OjeR?= MVe1NFBvVQ>? MlHyNUBp NEfOXW9T\WS3Y3XzJGRVYC2Wcnnn[4Vz\WRiRX7kc5Rp\WyrYXygSJl{\nWwY4Tpc44> NYXXTHU4OjV4M{S1N|g>
A549 NUnLb25TTnWwY4Tpc44hSXO|YYm= M1;M[|AvOcLizszN MlfHNlQhcA>? NEnI[3Zl\WO{ZXHz[ZMhfGinIILlcIF1cX[nIGDLR{3PuSCuZY\lcEBwdiClZXzsJI1mdWK{YX7lJINwfHKnYYTl[EBCWy2LVh?= MWGyOVIyQDF4MR?=
A549 M4rQTmZ2dmO2aX;uJGF{e2G7 M3\hflAvOcLizszN NYPY[Y9EOjRiaB?= MVzy[YR2[2W|IITo[UBmgHC{ZYPzbY9vKGyndnXsd{Bw\iCPTWCtNkwhVU2SLUmgZY5lKGmwdHXndolvKM7{MR?= NHvoe2EzPTJzOEG2NS=>
A549 M1fN[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH2xbYExNjIEoN88US=> NH;m[JIzPCCq MULlcohidmOnczDndo94fGhiaX7obYJqfGmxbjDjc5Rz\WG2ZXSge4l1cCCDUz3JWi=> NIDCcnQzPTJzOEG2NS=>
Mel202 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\xNE42KM7:TR?= MWGzJIg> NVnQfJBwTE2VTx?= MUXlcohidmOnczDJVk1qdmS3Y3XkJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fS=> M2rCbVI1PTl3M{i1
92.1 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DaNVAvPSEQvF2= NHr6TVc{KGh? Mme2SG1UVw>? MlrP[Y5p[W6lZYOgTXIucW6mdXPl[EBz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJk> MoTQNlQ2QTV|OEW=
OCM3 M3zlfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MonsNE42KM7:TR?= NYfz[3BDOyCq NYrwO|llTE2VTx?= MVflcohidmOnczDJVk1qdmS3Y3XkJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fS=> MW[yOFU6PTN6NR?=
Mel202 NIHxPFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DQWVAvPSEQvF2= NVzPR5F{OyCq NVPtXo5xTE2VTx?= NHK3SopqdmO{ZXHz[ZMhUVJvaX7keYNm\CClZXzsJIN6[2ynIHHydoV{fMLi MVKyOFU6PTN6NR?=
92.1 NIG1RY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjPUYoxNjVizszN MlfIN{Bp MlTxSG1UVw>? MUDpcoNz\WG|ZYOgTXIucW6mdXPl[EBk\WyuIHP5Z4xmKGG{cnXzeOKh NV7QbFFlOjR3OUWzPFU>
OCM3 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLIW4V6OC53IN88US=> NYfnSox1OyCq MkLMSG1UVw>? Mn;kbY5kemWjc3XzJGlTNWmwZIXj[YQh[2WubDDjfYNt\SCjcoLld5TDqA>? MnLpNlQ2QTV|OEW=
Jeko-1 M{\u[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXPdo01OC12IN88US=> MX3EUXNQ M1vPPYlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> MonLNlQ{PjJ7M{W=
Mino Mn2wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTsNE01KM7:TR?= M3W5W2ROW09? MWXpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MY[yOFM3Ojl|NR?=
Rec-1 M1;yUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml65NE01KM7:TR?= MVLEUXNQ M2fHVolvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> MYWyOFM3Ojl|NR?=
SP49 MnfwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1G1OlAuPCEQvF2= NYToT5huTE2VTx?= MVjpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NG\NSm4zPDN4MkmzOS=>
Jeko-1 NY\JNnBqTnWwY4Tpc44hSXO|YYm= M4TL[VIvPSEQvF5CpC=> NF;O[VcyOiCq MVHEUXNQ NWLxRoVZ\G:5boLl[5Vt[XSnczDOSk3PwkJidHHy[4V1KGenbnXz MofYNlQ{PjJ7M{W=
Mino M2G3d2Z2dmO2aX;uJGF{e2G7 NGDE[IYzNjVizszNxsA> NVW0fpR[OTJiaB?= MorjSG1UVw>? MlLB[I94dnKnZ4XsZZRmeyCQRj5OvmIhfGG{Z3X0JIdmdmW| NWThRYdVOjR|NkK5N|U>
Rec-1 MVHGeY5kfGmxbjDBd5NigQ>? NXrvN41vOi53IN88UeKh NUHiUWd4OTJiaB?= NF;jXoNFVVOR Ml7M[I94dnKnZ4XsZZRmeyCQRj5OvmIhfGG{Z3X0JIdmdmW| M4S3XVI1OzZ{OUO1
SP49 NE\USHVHfW6ldHnvckBCe3OjeR?= MmnrNk42KM7:TdMg M3PZWFEzKGh? M2nUfGROW09? MYnkc5dvemWpdXzheIV{KE6ILd86RkB1[XKpZYSg[4Vv\XN? NYDaSY9{OjR|NkK5N|U>
CD3+ T  NGCwdI5HfW6ldHnvckBCe3OjeR?= MWGwMVUxOCCwTR?= NUPrVW1YOSCq NEf5ZlFqdmirYnn0d{BPTi4QulKgdIhwe3Cqb4L5cIF1cW:wIHnuJIEh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ MlrCNlM2PzN{OEO=
Mel202 NHHSWm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjsSFRVOC13IN88US=> NUfJb|lJPzJiaB?= NULtdWtuTE2VTx?= NUG3XnhKcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? MVqyNlY2Ozl4OB?=
Omm1.3 MnrXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXOwMVUh|ryP M3fafFczKGh? MlXSSG1UVw>? NFT1WWlqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 NVLvWpFZOjJ4NUO5Olg>
92.1 NX\ofZhLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWD2ZW9mOC13IN88US=> MWS3NkBp MnvUSG1UVw>? NV7ob5dIcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? MYGyNlY2Ozl4OB?=
Mel202 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHzR5g2KM7:TR?= M164ZVI1KGh? MVLEUXNQ Mn;ObY5lfWOnczDHNUBienKnc4VCpC=> NV7MNo9[OjJ4NUO5Olg>
Omm1.3 MnrNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HJclUh|ryP Mny2NlQhcA>? Ml72SG1UVw>? MlvmbY5lfWOnczDHNUBienKnc4VCpC=> MlG2NlI3PTN7Nki=
92.1 MmCwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfGOUDPxE1? M2P4fFI1KGh? Mn6ySG1UVw>? MlTrbY5lfWOnczDHNUBienKnc4VCpC=> M1y4TVIzPjV|OU[4
Mel202 MoTURZBweHSxc3nzJGF{e2G7 NGLWVJQ2KM7:TR?= MV[3NkBp NFriWm9FVVOR MkjJbY5lfWOnczDhdI9xfG:|aYOgd4xq\2i2bIm= NHO4PJEzOjZ3M{m2PC=>
Omm1.3 MY\BdI9xfG:|aYOgRZN{[Xl? NGXBTmw2KM7:TR?= MorlO|IhcA>? Mn\pSG1UVw>? NEW2eXBqdmS3Y3XzJIFxd3C2b4Ppdy=> NFjDUnMzOjZ3M{m2PC=>
92.1 NYf0bVloSXCxcITvd4l{KEG|c3H5 M2\vW|Uh|ryP NVT2SFVIPzJiaB?= NFfpSG9FVVOR MmXBbY5lfWOnczDhdI9xfG:|aYOgd4lodmmoY3HueIx6 MmjzNlI3PTN7Nki=
Mel202 NVrn[2huTnWwY4Tpc44hSXO|YYm= MYG1JO69VQ>? M2XHSFI1KGh? NVzIZotzcW6qaXLpeJMh\XiycnXzd4lwdiCjbnSgdIhwe3Cqb4L5cIF1cW:wIH;mJHBMSyCrc3;mc5Juew>? MXOyNlY2Ozl4OB?=
Omm1.3 NEnFcolHfW6ldHnvckBCe3OjeR?= Mk[2OUDPxE1? M4\I[VI1KGh? M{PRVIlvcGmkaYTzJIV5eHKnc4Ppc44h[W6mIIDoc5NxcG:{eXzheIlwdiCxZjDQT2MhcXOxZn;ycZM> MX[yNlY2Ozl4OB?=
92.1 NIP5Tm9HfW6ldHnvckBCe3OjeR?= MUC1JO69VQ>? MlHiNlQhcA>? MYXpcohq[mm2czDlfJBz\XO|aX;uJIFv\CCyaH;zdIhwenmuYYTpc44hd2ZiUFvDJIl{d2[xcn3z NHTtd5MzOjZ3M{m2PC=>
HBL1 NX7qNIdWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLmSZQxNjF4LUKwJO69VQ>? MV21JIQ> NXSzUXBnUUN3ME2wMlUh|ryP NHn0fXMzOTN{NEmyNC=>
TMD8 NV;NR2toT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPwbXUxNjF4LUKwJO69VQ>? MVe1JIQ> NUOw[GwyUUN3ME2wMlIh|ryP MXmyNVMzPDl{MB?=
OCI-Ly10 Mn6yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HlfFAvOTZvMkCg{txO MUm1JIQ> NEHOcGNKSzVyPUGuN{DPxE1? MVWyNVMzPDl{MB?=
U2932 M2TRS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M16w[VAvOTZvMkCg{txO MonmOUBl Mn3HTWM2OD1zMDFOwG0> MnL0NlE{OjR7MkC=
OCI-Ly3 NWfKZot1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUntRYptOC5zNj2yNEDPxE1? NGfJR3E2KGR? NYGxTmNJUUN3MP-8olIxKM7:TR?= M4LDWVIyOzJ2OUKw
SuDHL2 NIPzbFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWewMlE3NTJyIN88US=> MmGzOUBl Mmj6TWM2OO,:nkKwJO69VQ>? M1XnNFIyOzJ2OUKw
SuDHL4 NIDoU2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLRbnIxNjF4LUKwJO69VQ>? Mn;tOUBl MmnMTWM2OO,:nkKwJO69VQ>? MkfGNlE{OjR7MkC=
DB MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEezWFExNjF4LUKwJO69VQ>? NWHSO3FmPSCm M33zN2lEPTExvK6yNEDPxE1? MnHLNlE{OjR7MkC=
Jurkat IL-2 NHu4Z|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTZwN{GgxtEhOy55NjFOwG0> Ml\YNVk6PDB{NUm=
PBMC IL-2 MljsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3fERmlEPTB;ND64OEDDuSBzLkewJEDPxE1? NIW2SVYyQTl2MEK1PS=>

... 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