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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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

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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 NXXWOmIyTnWwY4Tpc44hSXO|YYm= MorENVAxKG6P NHjCVWM{KGh? NEjxbmlFVVOR M3L4SolvcGmkaYTzJJJTVkFic4nueIhme2m| M32yc|I2PjlzMUW4
HUVECs  NX\KWYI5TnWwY4Tpc44hSXO|YYm= MnHZOVAxdk1? NUXabJpDOSCq M3fzVHJm\HWlZYOgSHRZNVS{aXfn[ZJm\CCHbnTveIhmdGmjbDDEfZNnfW6ldHnvci=> NEez[WgzPTZ|NEWzPC=>
A549 MnX4SpVv[3Srb36gRZN{[Xl? NUXKSmZmOC5zwrFOwG0> M1TvVVI1KGh? NV6ybWUy\GWlcnXhd4V{KHSqZTDy[YxifGm4ZTDQT2Mu|rFibHX2[Ywhd25iY3XscEBu\W2kcnHu[UBkd3S{ZXH0[YQhSVNvSW[= M3WxfVI2OjF6MU[x
A549 M1nYcWZ2dmO2aX;uJGF{e2G7 NVfjPGpkOC5zwrFOwG0> NH35[3MzPCCq M2TST5Jm\HWlZYOgeIhmKGW6cILld5Nqd25ibHX2[Yx{KG:oIF3NVE0zNCCPTWCtPUBidmRiaX70[YdzcW5izsKx NX7ifG5xOjV{MUixOlE>
A549 MkLSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHvyeWcxNjIEoN88US=> MYWyOEBp Mm\4[Y5p[W6lZYOg[5Jwf3SqIHnubIljcXSrb36gZ491emWjdHXkJJdqfGhiQWOtTXY> NWjDbGRFOjV{MUixOlE>
Mel202 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHIVpUxNjVizszN NX7lPYdUOyCq MVzEUXNQ NYPl[lM3\W6qYX7j[ZMhUVJvaX7keYNm\CC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHl? MX[yOFU6PTN6NR?=
92.1 NHzKVZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DERVAvPSEQvF2= Mm\wN{Bp M4rW[2ROW09? M4DhXoVvcGGwY3XzJGlTNWmwZIXj[YQhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6 MWmyOFU6PTN6NR?=
OCM3 MnHYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVywMlUh|ryP MoPUN{Bp M133TGROW09? MVjlcohidmOnczDJVk1qdmS3Y3XkJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fS=> MmfkNlQ2QTV|OEW=
Mel202 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUKwMlUh|ryP NFf5TWs{KGh? MkjnSG1UVw>? MXnpcoNz\WG|ZYOgTXIucW6mdXPl[EBk\WyuIHP5Z4xmKGG{cnXzeOKh NXm2OWtXOjR3OUWzPFU>
92.1 NIfmN4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;ze5RxOC53IN88US=> NGq4[2E{KGh? MXvEUXNQ M4nQc4lv[3KnYYPld{BKWi2rbnT1Z4VlKGOnbHygZ5lkdGViYYLy[ZN1yqB? MUKyOFU6PTN6NR?=
OCM3 M3HlXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17hc|AvPSEQvF2= NHLj[Yo{KGh? NVXvOoVwTE2VTx?= MnTJbY5kemWjc3XzJGlTNWmwZIXj[YQh[2WubDDjfYNt\SCjcoLld5TDqA>? MV2yOFU6PTN6NR?=
Jeko-1 NFzhNIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nMOFAuPCEQvF2= NWPmVJd7TE2VTx?= MlT4bY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> M4DzZlI1OzZ{OUO1
Mino MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXiwMVQh|ryP M37td2ROW09? MVnpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MXOyOFM3Ojl|NR?=
Rec-1 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFz6PGIxNTRizszN NULC[21iTE2VTx?= M3zOW4lvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> MoXQNlQ{PjJ7M{W=
SP49 M3:wPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\MNE01KM7:TR?= MVfEUXNQ MluzbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NEDLSnQzPDN4MkmzOS=>
Jeko-1 MXXGeY5kfGmxbjDBd5NigQ>? NYfSNHFJOi53IN88UeKh NGLO[YoyOiCq M4raW2ROW09? M4e2SoRwf26{ZXf1cIF1\XNiTl[t{tpDKHSjcnfleEBo\W6ncx?= NFnrdoozPDN4MkmzOS=>
Mino MnjUSpVv[3Srb36gRZN{[Xl? NF3Lb2gzNjVizszNxsA> NUTZSpM6OTJiaB?= NGTOcodFVVOR M3zhbYRwf26{ZXf1cIF1\XNiTl[t{tpDKHSjcnfleEBo\W6ncx?= NVWzcXpNOjR|NkK5N|U>
Rec-1 MlHGSpVv[3Srb36gRZN{[Xl? MVyyMlUh|ryPwrC= Ml7INVIhcA>? M3vuR2ROW09? M4nLUIRwf26{ZXf1cIF1\XNiTl[t{tpDKHSjcnfleEBo\W6ncx?= M1XiO|I1OzZ{OUO1
SP49 M3LDcmZ2dmO2aX;uJGF{e2G7 MXSyMlUh|ryPwrC= M1:2O|EzKGh? MoDmSG1UVw>? M{jrVoRwf26{ZXf1cIF1\XNiTl[t{tpDKHSjcnfleEBo\W6ncx?= MXWyOFM3Ojl|NR?=
CD3+ T  NWnKZ3lyTnWwY4Tpc44hSXO|YYm= NYjoepR[OC13MECgcm0> NVjsNllDOSCq Mm\ZbY5pcWKrdIOgUmYu|rqEIIDoc5NxcG:{eXzheIlwdiCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? M1q5TFI{PTd|Mkiz
Mel202 NFvlZ2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPtNE02KM7:TR?= MYm3NkBp M1TmV2ROW09? MWPpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MonCNlI3PTN7Nki=
Omm1.3 MlTHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYq4SlJjOC13IN88US=> NYCwXY82PzJiaB?= NHnN[2lFVVOR NGfOSmFqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 MlvWNlI3PTN7Nki=
92.1 NIS3e49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXGwMVUh|ryP Mmf3O|IhcA>? MVnEUXNQ NVXuSIdNcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NWfpbIk6OjJ4NUO5Olg>
Mel202 NUXpcFVUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHSemE2KM7:TR?= M360ZlI1KGh? NYLrOYJQTE2VTx?= MXXpcoR2[2W|IFexJIFzemW|dNMg NFf4UnozOjZ3M{m2PC=>
Omm1.3 M1nZT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\BVmdIPSEQvF2= Ml;4NlQhcA>? NIn2eFFFVVOR NHr1[oZqdmS3Y3XzJGcyKGG{cnXzeOKh MmTCNlI3PTN7Nki=
92.1 NIrPT3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPUS4xnPSEQvF2= MVqyOEBp NY\jXWo6TE2VTx?= M3[5Solv\HWlZYOgS|Eh[XK{ZYP0xsA> MkfNNlI3PTN7Nki=
Mel202 MlHoRZBweHSxc3nzJGF{e2G7 M4nyS|Uh|ryP NECzbJk4OiCq NV\n[ok2TE2VTx?= M{jCSolv\HWlZYOgZZBweHSxc3nzJJNtcWeqdHz5 NGi0TVYzOjZ3M{m2PC=>
Omm1.3 MnvMRZBweHSxc3nzJGF{e2G7 NVHv[JpVPSEQvF2= Ml3FO|IhcA>? M1PuW2ROW09? NFvtfWlqdmS3Y3XzJIFxd3C2b4Ppdy=> NFW4VpozOjZ3M{m2PC=>
92.1 NXzKbW1FSXCxcITvd4l{KEG|c3H5 NX\jTJZZPSEQvF2= NUjseXFUPzJiaB?= NGDFSJBFVVOR Mn7MbY5lfWOnczDhdI9xfG:|aYOgd4lodmmoY3HueIx6 MnfuNlI3PTN7Nki=
Mel202 M4fUfmZ2dmO2aX;uJGF{e2G7 NVfvOXo4PSEQvF2= MVqyOEBp MYjpcohq[mm2czDlfJBz\XO|aX;uJIFv\CCyaH;zdIhwenmuYYTpc44hd2ZiUFvDJIl{d2[xcn3z NYjKUHFLOjJ4NUO5Olg>
Omm1.3 MmnYSpVv[3Srb36gRZN{[Xl? NFTxTXU2KM7:TR?= NUe3VGY6OjRiaB?= MUnpcohq[mm2czDlfJBz\XO|aX;uJIFv\CCyaH;zdIhwenmuYYTpc44hd2ZiUFvDJIl{d2[xcn3z MkXvNlI3PTN7Nki=
92.1 NEDDVJNHfW6ldHnvckBCe3OjeR?= MUC1JO69VQ>? MVGyOEBp NYHQd3lScW6qaXLpeJMh\XiycnXzd4lwdiCjbnSgdIhwe3Cqb4L5cIF1cW:wIH;mJHBMSyCrc3;mc5Juew>? M2H0WlIzPjV|OU[4
HBL1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4H6UlAvOTZvMkCg{txO MYi1JIQ> MmGxTWM2OD1yLkWg{txO M3TYXFIyOzJ2OUKw
TMD8 M2i5eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnKTlExNjF4LUKwJO69VQ>? NVP1OGprPSCm NUfRdWJ4UUN3ME2wMlIh|ryP NEDLOJAzOTN{NEmyNC=>
OCI-Ly10 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjWZnh3OC5zNj2yNEDPxE1? NX3VUmM5PSCm MmrLTWM2OD1zLkOg{txO MojKNlE{OjR7MkC=
U2932 NFLRTJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\SdFExNjF4LUKwJO69VQ>? NX\Lc4M1PSCm NXH4S5B[UUN3ME2xNEDPxE1? M3eyTlIyOzJ2OUKw
OCI-Ly3 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVKwMlE3NTJyIN88US=> MoTGOUBl MXfJR|Ux97zgMkCg{txO MnnjNlE{OjR7MkC=
SuDHL2 NXjhbHR[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DlXVAvOTZvMkCg{txO NIXxWpc2KGR? M{DtWWlEPTExvK6yNEDPxE1? M1:0c|IyOzJ2OUKw
SuDHL4 MnPnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXOwMlE3NTJyIN88US=> NGrR[Ik2KGR? MoXLTWM2OO,:nkKwJO69VQ>? NIHzW3EzOTN{NEmyNC=>
DB MmC2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2f2dFAvOTZvMkCg{txO M2rxPFUh\A>? MUfJR|Ux97zgMkCg{txO MYmyNVMzPDl{MB?=
Jurkat IL-2 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7uTWM2OD14LkexJOKyKDNwN{[g{txO M3rLZVE6QTRyMkW5
PBMC IL-2 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mln4TWM2OD12Lki0JOKyKDFwN{CgJO69VQ>? MoO5NVk6PDB{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
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