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 Mm\ESpVv[3Srb36gRZN{[Xl? NYm3RldqOTByIH7N MVyzJIg> NYT0W2psTE2VTx?= NGDmcHdqdmirYnn0d{BzWk6DIIP5cpRp\XOrcx?= MmDhNlU3QTFzNUi=
HUVECs  M3nObGZ2dmO2aX;uJGF{e2G7 NFXQXWk2ODCwTR?= NHvwV2IyKGh? NEXmPYxT\WS3Y3XzJGRVYC2Wcnnn[4Vz\WRiRX7kc5Rp\WyrYXygSJl{\nWwY4Tpc44> NFvTS3EzPTZ|NEWzPC=>
A549 MkfXSpVv[3Srb36gRZN{[Xl? NHn2ZXAxNjIEoN88US=> M3\je|I1KGh? NXnxb|F{\GWlcnXhd4V{KHSqZTDy[YxifGm4ZTDQT2Mu|rFibHX2[Ywhd25iY3XscEBu\W2kcnHu[UBkd3S{ZXH0[YQhSVNvSW[= NUDpfZpsOjV{MUixOlE>
A549 MmLzSpVv[3Srb36gRZN{[Xl? NWrmXYxFOC5zwrFOwG0> MmrkNlQhcA>? M3nrdZJm\HWlZYOgeIhmKGW6cILld5Nqd25ibHX2[Yx{KG:oIF3NVE0zNCCPTWCtPUBidmRiaX70[YdzcW5izsKx NVfoToFoOjV{MUixOlE>
A549 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYSzZoRZOC5zwrFOwG0> M3j0XlI1KGh? M{DaO4VvcGGwY3XzJIdzd3e2aDDpcohq[mm2aX;uJINwfHKnYYTl[EB4cXSqIFHTMWlX NFfMN3EzPTJzOEG2NS=>
Mel202 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFqyenoxNjVizszN MXuzJIg> MlTlSG1UVw>? NEjqW3VmdmijbnPld{BKWi2rbnT1Z4VlKHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gQ>? NIHGTW8zPDV7NUO4OS=>
92.1 Ml\2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUGwMlUh|ryP NHLrcYM{KGh? NXuyUIFETE2VTx?= M3HhZ4VvcGGwY3XzJGlTNWmwZIXj[YQhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6 M3P4Z|I1PTl3M{i1
OCM3 NXvFVWp4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWT4VIc1OC53IN88US=> M4LNN|MhcA>? NFTmUFBFVVOR MXTlcohidmOnczDJVk1qdmS3Y3XkJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fS=> NYj3eHVoOjR3OUWzPFU>
Mel202 M3PUdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnrnNE42KM7:TR?= NVLPfmQ1OyCq MkXHSG1UVw>? NXLBUpV[cW6lcnXhd4V{KEmULXnu[JVk\WRiY3XscEBkgWOuZTDhdpJme3UEoB?= MV[yOFU6PTN6NR?=
92.1 MlPaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY[wMlUh|ryP MWqzJIg> Mmj5SG1UVw>? MVnpcoNz\WG|ZYOgTXIucW6mdXPl[EBk\WyuIHP5Z4xmKGG{cnXzeOKh MVuyOFU6PTN6NR?=
OCM3 M1HkVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHrRVnAxNjVizszN MWGzJIg> M4rqS2ROW09? NWjU[WVEcW6lcnXhd4V{KEmULXnu[JVk\WRiY3XscEBkgWOuZTDhdpJme3UEoB?= NUexOIdvOjR3OUWzPFU>
Jeko-1 NUXrTpVbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkS3NE01KM7:TR?= NWXGb2M2TE2VTx?= M{\GTYlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NEDuTmgzPDN4MkmzOS=>
Mino NE\nOFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVWwMVQh|ryP MVzEUXNQ MXTpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MmrMNlQ{PjJ7M{W=
Rec-1 NF7n[3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1PaUlAuPCEQvF2= NUXPOYJHTE2VTx?= MX7pcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NIfpfnEzPDN4MkmzOS=>
SP49 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYmwMVQh|ryP NXvGPYtqTE2VTx?= M{DOfYlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> MXuyOFM3Ojl|NR?=
Jeko-1 MmiwSpVv[3Srb36gRZN{[Xl? MXSyMlUh|ryPwrC= NUi3N3o{OTJiaB?= NUXaNYRUTE2VTx?= MU\kc5dvemWpdXzheIV{KE6ILd86RkB1[XKpZYSg[4Vv\XN? NEK1PIIzPDN4MkmzOS=>
Mino NWLsW3BwTnWwY4Tpc44hSXO|YYm= MkD6Nk42KM7:TdMg MWixNkBp MmXVSG1UVw>? MYnkc5dvemWpdXzheIV{KE6ILd86RkB1[XKpZYSg[4Vv\XN? M2exOVI1OzZ{OUO1
Rec-1 MYHGeY5kfGmxbjDBd5NigQ>? M2TWZ|IvPSEQvF5CpC=> Mny5NVIhcA>? MXLEUXNQ NHjUUFNld3ewcnXneYxifGW|IF7GMe67SiC2YYLn[ZQh\2WwZYO= NHXWTW4zPDN4MkmzOS=>
SP49 M4G3TWZ2dmO2aX;uJGF{e2G7 NUnXUW9rOi53IN88UeKh NX7zZ2FZOTJiaB?= NFz0TGZFVVOR NHvGeWxld3ewcnXneYxifGW|IF7GMe67SiC2YYLn[ZQh\2WwZYO= M1LrWFI1OzZ{OUO1
CD3+ T  MVPGeY5kfGmxbjDBd5NigQ>? NH;sN24xNTVyMDDuUS=> NGLmUZgyKGh? NGm2W3pqdmirYnn0d{BPTi4QulKgdIhwe3Cqb4L5cIF1cW:wIHnuJIEh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ NIr4XnMzOzV5M{K4Ny=>
Mel202 NWexT2lET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVqwMVUh|ryP MlKyO|IhcA>? NGi1UXJFVVOR M2LsOYlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> MVyyNlY2Ozl4OB?=
Omm1.3 M1Tve2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGn0NXcxNTVizszN NYTnd4hvPzJiaB?= NUPMe4t2TE2VTx?= MYLpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 M4L4dVIzPjV|OU[4
92.1 MknFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmfXNE02KM7:TR?= NWrYSoN{PzJiaB?= MV3EUXNQ MVLpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 Mom5NlI3PTN7Nki=
Mel202 Mm\3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrvUpg2KM7:TR?= MUOyOEBp NGXx[mRFVVOR NUjuR3RqcW6mdXPld{BIOSCjcoLld5TDqA>? M4C0c|IzPjV|OU[4
Omm1.3 Mn3HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PDeVUh|ryP NHH2[HIzPCCq NVXxTGpQTE2VTx?= MUPpcoR2[2W|IFexJIFzemW|dNMg M4q0N|IzPjV|OU[4
92.1 NHzmW2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXUO4tDPSEQvF2= NEfmUIUzPCCq NEfIU5dFVVOR MWnpcoR2[2W|IFexJIFzemW|dNMg MkHYNlI3PTN7Nki=
Mel202 MV;BdI9xfG:|aYOgRZN{[Xl? NV7jR2RtPSEQvF2= M{nZNVczKGh? NIrLeotFVVOR M33ueIlv\HWlZYOgZZBweHSxc3nzJJNtcWeqdHz5 M3TiRVIzPjV|OU[4
Omm1.3 NXHUPVRCSXCxcITvd4l{KEG|c3H5 MVu1JO69VQ>? NIjSXnk4OiCq Mn3RSG1UVw>? M1LGdolv\HWlZYOgZZBweHSxc3nz M{T6fFIzPjV|OU[4
92.1 MmnqRZBweHSxc3nzJGF{e2G7 MlHBOUDPxE1? NVXXdo1GPzJiaB?= M2TTcGROW09? NHH4UZVqdmS3Y3XzJIFxd3C2b4Ppd{B{cWewaX\jZY51dHl? NUW4XnYzOjJ4NUO5Olg>
Mel202 MnT6SpVv[3Srb36gRZN{[Xl? NIqzfnE2KM7:TR?= MYiyOEBp MoPpbY5pcWKrdIOg[ZhxemW|c3nvckBidmRicHjvd5Bpd3K7bHH0bY9vKG:oIGDLR{Bqe2:ob4Ltdy=> M{HDWFIzPjV|OU[4
Omm1.3 NVTCNZhRTnWwY4Tpc44hSXO|YYm= NXe1bFVGPSEQvF2= MnP5NlQhcA>? NHfUeIlqdmirYnn0d{BmgHC{ZYPzbY9vKGGwZDDwbI9{eGixconsZZRqd25ib3[gVGtEKGm|b3\vdo1{ M2XmNFIzPjV|OU[4
92.1 NYX1Xo1kTnWwY4Tpc44hSXO|YYm= M2LvPFUh|ryP Mnj0NlQhcA>? NWi2cZhqcW6qaXLpeJMh\XiycnXzd4lwdiCjbnSgdIhwe3Cqb4L5cIF1cW:wIH;mJHBMSyCrc3;mc5Juew>? MUSyNlY2Ozl4OB?=
HBL1 NHjYSYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXSwMlE3NTJyIN88US=> NUHLTo46PSCm NFnHVIpKSzVyPUCuOUDPxE1? MmLyNlE{OjR7MkC=
TMD8 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3tTpdYOC5zNj2yNEDPxE1? NE\hd282KGR? NFXGVolKSzVyPUCuNkDPxE1? Ml7tNlE{OjR7MkC=
OCI-Ly10 Ml;6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7ZNE4yPi1{MDFOwG0> NILDfXc2KGR? M{\TbmlEPTB;MT6zJO69VQ>? NXnUPWpiOjF|MkS5NlA>
U2932 NVeyT3hUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HCXlAvOTZvMkCg{txO MnfKOUBl Mm\OTWM2OD1zMDFOwG0> MXuyNVMzPDl{MB?=
OCI-Ly3 NUnSW29uT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4e1N|AvOTZvMkCg{txO NVH6RldOPSCm MlXlTWM2OO,:nkKwJO69VQ>? Ml7ZNlE{OjR7MkC=
SuDHL2 NGPQclRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW[wMlE3NTJyIN88US=> NYPCUWxZPSCm NF70N3hKSzVy78{eNlAh|ryP NGHUO3EzOTN{NEmyNC=>
SuDHL4 NF3p[lRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPmPZYxNjF4LUKwJO69VQ>? MV61JIQ> NUnsXJVmUUN3MP-8olIxKM7:TR?= M3vRVFIyOzJ2OUKw
DB MlnOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXm0PGdEOC5zNj2yNEDPxE1? MXy1JIQ> NYLye2VjUUN3MP-8olIxKM7:TR?= NFj4VmQzOTN{NEmyNC=>
Jurkat IL-2 M{P2dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmmwTWM2OD14LkexJOKyKDNwN{[g{txO NI\mT|UyQTl2MEK1PS=>
PBMC IL-2 M1zWRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTRwOESgxtEhOS55MDCg{txO NHu0WmMyQTl2MEK1PS=>

... 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 <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
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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID