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 MVzGeY5kfGmxbjDBd5NigQ>? NYTtcXhlOTByIH7N NGXMVHQ{KGh? MoXxSG1UVw>? M3e0dolvcGmkaYTzJJJTVkFic4nueIhme2m| NUT3O4p2OjV4OUGxOVg>
HUVECs  MXPGeY5kfGmxbjDBd5NigQ>? MnO0OVAxdk1? MnnENUBp MlT6VoVlfWOnczDEWHguXHKrZ3fldoVlKEWwZH;0bIVtcWGuIFT5d4Z2dmO2aX;u MX:yOVY{PDV|OB?=
A549 M{LGUWZ2dmO2aX;uJGF{e2G7 NVS1empQOC5zwrFOwG0> NVPiPJBVOjRiaB?= NV\LcGV5\GWlcnXhd4V{KHSqZTDy[YxifGm4ZTDQT2Mu|rFibHX2[Ywhd25iY3XscEBu\W2kcnHu[UBkd3S{ZXH0[YQhSVNvSW[= M13aTFI2OjF6MU[x
A549 NWLLWZdtTnWwY4Tpc44hSXO|YYm= Mke0NE4yyqEQvF2= NIjW[IEzPCCq MVry[YR2[2W|IITo[UBmgHC{ZYPzbY9vKGyndnXsd{Bw\iCPTWCtNkwhVU2SLUmgZY5lKGmwdHXndolvKM7{MR?= MnvFNlUzOThzNkG=
A549 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3[3S|AvOcLizszN NFu5VHQzPCCq NHPlPGxmdmijbnPld{Boem:5dHigbY5pcWKrdHnvckBkd3S{ZXH0[YQhf2m2aDDBV{1KXg>? NX7KWpFbOjV{MUixOlE>
Mel202 M{PaWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYOzVXIzOC53IN88US=> MmDDN{Bp MYfEUXNQ NXO5ZXZ3\W6qYX7j[ZMhUVJvaX7keYNm\CC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHl? MofXNlQ2QTV|OEW=
92.1 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4n2d|AvPSEQvF2= Ml2zN{Bp MmLsSG1UVw>? MoPD[Y5p[W6lZYOgTXIucW6mdXPl[EBz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJk> NHHkNZozPDV7NUO4OS=>
OCM3 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fFR|AvPSEQvF2= NIPPPFE{KGh? M{PRWWROW09? MXjlcohidmOnczDJVk1qdmS3Y3XkJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fS=> M2XuOVI1PTl3M{i1
Mel202 M3[3fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW[wMlUh|ryP NWnBSJNmOyCq M{f5eGROW09? NEPlbGZqdmO{ZXHz[ZMhUVJvaX7keYNm\CClZXzsJIN6[2ynIHHydoV{fMLi MmDYNlQ2QTV|OEW=
92.1 NHLaRnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzPdHAxNjVizszN NF\3coc{KGh? NWH2cpY{TE2VTx?= NI\h[oJqdmO{ZXHz[ZMhUVJvaX7keYNm\CClZXzsJIN6[2ynIHHydoV{fMLi M{X4TFI1PTl3M{i1
OCM3 NXHx[25pT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH[yUIQxNjVizszN MmL1N{Bp MnjxSG1UVw>? M4Tke4lv[3KnYYPld{BKWi2rbnT1Z4VlKGOnbHygZ5lkdGViYYLy[ZN1yqB? NWr2eHByOjR3OUWzPFU>
Jeko-1 NWi3cW05T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVewMVQh|ryP NX72Uow6TE2VTx?= Ml3ObY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> M4C1XFI1OzZ{OUO1
Mino M372dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHL0T20xNTRizszN MUPEUXNQ NY\iTo46cW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NFL1WZozPDN4MkmzOS=>
Rec-1 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnG1NE01KM7:TR?= MmLZSG1UVw>? M{T3[4lvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> MoDRNlQ{PjJ7M{W=
SP49 NXvI[pByT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXLJUVk4OC12IN88US=> M1z6emROW09? MYTpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NV\sOIpKOjR|NkK5N|U>
Jeko-1 MmPhSpVv[3Srb36gRZN{[Xl? MWOyMlUh|ryPwrC= NXro[WN1OTJiaB?= MUTEUXNQ Mn\N[I94dnKnZ4XsZZRmeyCQRj5OvmIhfGG{Z3X0JIdmdmW| NIexOWQzPDN4MkmzOS=>
Mino NYfFUHdCTnWwY4Tpc44hSXO|YYm= NXXPRWxSOi53IN88UeKh NYXaVo9WOTJiaB?= NHqyXYRFVVOR MUTkc5dvemWpdXzheIV{KE6ILd86RkB1[XKpZYSg[4Vv\XN? M1;ZOVI1OzZ{OUO1
Rec-1 NUize|BsTnWwY4Tpc44hSXO|YYm= NFHNS2czNjVizszNxsA> M1vIOFEzKGh? MVPEUXNQ M1fib4Rwf26{ZXf1cIF1\XNiTl[t{tpDKHSjcnfleEBo\W6ncx?= NUn3e5A{OjR|NkK5N|U>
SP49 MYXGeY5kfGmxbjDBd5NigQ>? MorUNk42KM7:TdMg M2jHPFEzKGh? MVvEUXNQ NWL6SXd{\G:5boLl[5Vt[XSnczDOSk3PwkJidHHy[4V1KGenbnXz NHLxVmYzPDN4MkmzOS=>
CD3+ T  MonSSpVv[3Srb36gRZN{[Xl? NFvhUGsxNTVyMDDuUS=> M1Hu[FEhcA>? NFfNe|RqdmirYnn0d{BPTi4QulKgdIhwe3Cqb4L5cIF1cW:wIHnuJIEh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ M1PXflI{PTd|Mkiz
Mel202 NGLsUXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NELkUWoxNTVizszN M2T0OFczKGh? M{PLW2ROW09? Ml7nbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NHj2UngzOjZ3M{m2PC=>
Omm1.3 MlPJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUGwMVUh|ryP NGDPd4s4OiCq NIO1N5RFVVOR M1LGWYlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NHrKR5EzOjZ3M{m2PC=>
92.1 NV71d5ZwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX71WGliOC13IN88US=> M2D2WlczKGh? MmHwSG1UVw>? MnzybY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NVLl[o14OjJ4NUO5Olg>
Mel202 NEO3O5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXP2RYVNPSEQvF2= M4P3ZVI1KGh? NUDxZWZ3TE2VTx?= M2nmUIlv\HWlZYOgS|Eh[XK{ZYP0xsA> M3fzZVIzPjV|OU[4
Omm1.3 NIXsUpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnnsOUDPxE1? M2T0VFI1KGh? NGTZd4ZFVVOR NXK4WZRGcW6mdXPld{BIOSCjcoLld5TDqA>? NEPndowzOjZ3M{m2PC=>
92.1 NHy5ZYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHyPW02KM7:TR?= NWDzWmo5OjRiaB?= NH;3b2pFVVOR NHexS|RqdmS3Y3XzJGcyKGG{cnXzeOKh NEX1b|QzOjZ3M{m2PC=>
Mel202 MUnBdI9xfG:|aYOgRZN{[Xl? MoT0OUDPxE1? M37pflczKGh? M4DIRmROW09? MoXnbY5lfWOnczDhdI9xfG:|aYOgd4xq\2i2bIm= NYf4TXU1OjJ4NUO5Olg>
Omm1.3 NH;hPYxCeG:ydH;zbZMhSXO|YYm= M{HRcFUh|ryP MlzsO|IhcA>? NUPoVW9OTE2VTx?= MVzpcoR2[2W|IHHwc5B1d3Orcx?= M3n5W|IzPjV|OU[4
92.1 M4rOTmFxd3C2b4Ppd{BCe3OjeR?= MV21JO69VQ>? M{HUN|czKGh? NUCyO2FSTE2VTx?= NYXkV|JOcW6mdXPld{BieG:ydH;zbZMhe2mpbnnmZ4FvfGy7 NGjwWVEzOjZ3M{m2PC=>
Mel202 NGLoc2dHfW6ldHnvckBCe3OjeR?= MoHKOUDPxE1? MUSyOEBp MoLmbY5pcWKrdIOg[ZhxemW|c3nvckBidmRicHjvd5Bpd3K7bHH0bY9vKG:oIGDLR{Bqe2:ob4Ltdy=> M1nXXVIzPjV|OU[4
Omm1.3 M2jyc2Z2dmO2aX;uJGF{e2G7 MonVOUDPxE1? NXHqUlM1OjRiaB?= NGjuc2xqdmirYnn0d{BmgHC{ZYPzbY9vKGGwZDDwbI9{eGixconsZZRqd25ib3[gVGtEKGm|b3\vdo1{ MW[yNlY2Ozl4OB?=
92.1 NE\HO|lHfW6ldHnvckBCe3OjeR?= MlL0OUDPxE1? NGO3V2wzPCCq NVz2[4c{cW6qaXLpeJMh\XiycnXzd4lwdiCjbnSgdIhwe3Cqb4L5cIF1cW:wIH;mJHBMSyCrc3;mc5Juew>? M2jrcFIzPjV|OU[4
HBL1 M3HGNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWOwMlE3NTJyIN88US=> MUS1JIQ> M1q1NmlEPTB;MD61JO69VQ>? MkfGNlE{OjR7MkC=
TMD8 M{L4TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUKwMlE3NTJyIN88US=> Mm\rOUBl MlXnTWM2OD1yLkKg{txO MkG0NlE{OjR7MkC=
OCI-Ly10 NWrWdHdHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3UWmExNjF4LUKwJO69VQ>? NUfuUY5FPSCm M1rMdmlEPTB;MT6zJO69VQ>? NHzyR2wzOTN{NEmyNC=>
U2932 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWrxeGliOC5zNj2yNEDPxE1? NHHXWng2KGR? NWj4PHdVUUN3ME2xNEDPxE1? Mn;ZNlE{OjR7MkC=
OCI-Ly3 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYi4ZYUzOC5zNj2yNEDPxE1? MVS1JIQ> NUnPXmVjUUN3MP-8olIxKM7:TR?= MnXCNlE{OjR7MkC=
SuDHL2 MlLJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rUS|AvOTZvMkCg{txO NFfjS|k2KGR? MVXJR|Ux97zgMkCg{txO NGTPS5EzOTN{NEmyNC=>
SuDHL4 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojKNE4yPi1{MDFOwG0> NH7Ecpo2KGR? M1jVO2lEPTExvK6yNEDPxE1? MlzVNlE{OjR7MkC=
DB MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3fm[|AvOTZvMkCg{txO MUK1JIQ> NVnUbYxzUUN3MP-8olIxKM7:TR?= MnLSNlE{OjR7MkC=
Jurkat IL-2 MkLsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHvyPZlKSzVyPU[uO|EhyrFiMz63OkDPxE1? NV\mSJVZOTl7NECyOVk>
PBMC IL-2 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3G5NmlEPTB;ND64OEDDuSBzLkewJEDPxE1? MVixPVk1ODJ3OR?=

... 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