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

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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 MYTGeY5kfGmxbjDBd5NigQ>? MXSxNFAhdk1? Mk\1N{Bp NYn2OmlyTE2VTx?= NFXad29qdmirYnn0d{BzWk6DIIP5cpRp\XOrcx?= MUGyOVY6OTF3OB?=
HUVECs  Ml6ySpVv[3Srb36gRZN{[Xl? NFrKOYs2ODCwTR?= NVXHSGM{OSCq NV22fphvWmWmdXPld{BFXFhvVILp[4dmemWmIFXu[I91cGWuaXHsJGR6e2[3bnP0bY9v NH7md3gzPTZ|NEWzPC=>
A549 M3;IRmZ2dmO2aX;uJGF{e2G7 M{jsNFAvOcLizszN M1LUdlI1KGh? MX;k[YNz\WG|ZYOgeIhmKHKnbHH0bZZmKFCNQz5OtUBt\X[nbDDvckBk\WyuIH3lcYJz[W6nIHPveJJm[XSnZDDBV{1KXg>? MnLyNlUzOThzNkG=
A549 NFHiSJlHfW6ldHnvckBCe3OjeR?= NGjSTnMxNjIEoN88US=> NYXxU4MxOjRiaB?= NVXJNpM{emWmdXPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdHNib3[gUW1RNTJuIF3NVE06KGGwZDDpcpRm\3KrbjFOtlE> NXqwVlIzOjV{MUixOlE>
A549 NUXFZYtQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH36R3kxNjIEoN88US=> M4DmWFI1KGh? NVHZTXhz\W6qYX7j[ZMh\3Kxd4ToJIlvcGmkaYTpc44h[2:2cnXheIVlKHerdHigRXMuUVZ? M2K3UVI2OjF6MU[x
Mel202 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rlNlAvPSEQvF2= M{XmUVMhcA>? NID1OVdFVVOR MUPlcohidmOnczDJVk1qdmS3Y3XkJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fS=> Ml\CNlQ2QTV|OEW=
92.1 MofXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2fOe|AvPSEQvF2= NFnFbZY{KGh? M1fNUWROW09? M{\0ZYVvcGGwY3XzJGlTNWmwZIXj[YQhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6 MV6yOFU6PTN6NR?=
OCM3 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYj1UWtYOC53IN88US=> NXm0TmoyOyCq MlPESG1UVw>? Mkjs[Y5p[W6lZYOgTXIucW6mdXPl[EBz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJk> NXHSOZVvOjR3OUWzPFU>
Mel202 M{jLcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M171e|AvPSEQvF2= MlXTN{Bp NGDPeWVFVVOR NF[zSG5qdmO{ZXHz[ZMhUVJvaX7keYNm\CClZXzsJIN6[2ynIHHydoV{fMLi MonDNlQ2QTV|OEW=
92.1 Moi1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVSwMlUh|ryP NFHyb|g{KGh? NX\j[ZA6TE2VTx?= NWLBTWlIcW6lcnXhd4V{KEmULXnu[JVk\WRiY3XscEBkgWOuZTDhdpJme3UEoB?= MlvJNlQ2QTV|OEW=
OCM3 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUWwMlUh|ryP NV;GXW86OyCq NWPFdXV1TE2VTx?= NFnZXWNqdmO{ZXHz[ZMhUVJvaX7keYNm\CClZXzsJIN6[2ynIHHydoV{fMLi MmXUNlQ2QTV|OEW=
Jeko-1 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\CXIpxOC12IN88US=> MofNSG1UVw>? M2\RZolvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> MonCNlQ{PjJ7M{W=
Mino M1[2cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYGwMVQh|ryP NY\xT5R4TE2VTx?= NFXQ[XZqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 NYT4V2F5OjR|NkK5N|U>
Rec-1 M3yxXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXewMVQh|ryP M3XUb2ROW09? NIfsWFlqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 NVzLVJJ6OjR|NkK5N|U>
SP49 M{\1ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2i3V|AuPCEQvF2= Mn;pSG1UVw>? NFjYVmpqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 NXvuXVJwOjR|NkK5N|U>
Jeko-1 MVLGeY5kfGmxbjDBd5NigQ>? NEX5Vo4zNjVizszNxsA> MnnJNVIhcA>? NHvve3pFVVOR NIT4XHdld3ewcnXneYxifGW|IF7GMe67SiC2YYLn[ZQh\2WwZYO= MXKyOFM3Ojl|NR?=
Mino NEW2dGFHfW6ldHnvckBCe3OjeR?= MoLSNk42KM7:TdMg MWqxNkBp MV7EUXNQ M1TjWIRwf26{ZXf1cIF1\XNiTl[t{tpDKHSjcnfleEBo\W6ncx?= MV:yOFM3Ojl|NR?=
Rec-1 Mn;sSpVv[3Srb36gRZN{[Xl? MX:yMlUh|ryPwrC= NFPMNo8yOiCq NWfwUG5xTE2VTx?= M{XnboRwf26{ZXf1cIF1\XNiTl[t{tpDKHSjcnfleEBo\W6ncx?= NHPmVnkzPDN4MkmzOS=>
SP49 MUDGeY5kfGmxbjDBd5NigQ>? MVqyMlUh|ryPwrC= NH34S2oyOiCq NXS0UoFWTE2VTx?= Mle0[I94dnKnZ4XsZZRmeyCQRj5OvmIhfGG{Z3X0JIdmdmW| MWCyOFM3Ojl|NR?=
CD3+ T  MkDCSpVv[3Srb36gRZN{[Xl? NG\ZS|ExNTVyMDDuUS=> NEHhXoQyKGh? NVLHbHFxcW6qaXLpeJMhVkZvzsrCJJBpd3OyaH;yfYxifGmxbjDpckBiKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= NIOzcokzOzV5M{K4Ny=>
Mel202 Mn:4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWGwMVUh|ryP NXHaV3dHPzJiaB?= M1vyZmROW09? MU\pcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NHPQSGMzOjZ3M{m2PC=>
Omm1.3 NUm4fYhZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3lNE02KM7:TR?= MmCwO|IhcA>? MWfEUXNQ NXfWeVNpcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? M1i5UVIzPjV|OU[4
92.1 NHf6SlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\YfGoxNTVizszN NIWzW2s4OiCq M{iwUGROW09? M3HkdYlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> Mn64NlI3PTN7Nki=
Mel202 MnG2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2qxR|Uh|ryP NYDYVo44OjRiaB?= NHHqOopFVVOR MV;pcoR2[2W|IFexJIFzemW|dNMg M1LJ[lIzPjV|OU[4
Omm1.3 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY[1JO69VQ>? M3mzOlI1KGh? MmLzSG1UVw>? NHi4XpdqdmS3Y3XzJGcyKGG{cnXzeOKh NG[0OoozOjZ3M{m2PC=>
92.1 NXLHcHp[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3YOUDPxE1? NEn2UIszPCCq MV3EUXNQ MonZbY5lfWOnczDHNUBienKnc4VCpC=> MkGxNlI3PTN7Nki=
Mel202 NHvLe2FCeG:ydH;zbZMhSXO|YYm= MXK1JO69VQ>? MXW3NkBp NEP6TVhFVVOR NFvYNmxqdmS3Y3XzJIFxd3C2b4Ppd{B{dGmpaITsfS=> NVzqWo1WOjJ4NUO5Olg>
Omm1.3 MWHBdI9xfG:|aYOgRZN{[Xl? M{PtS|Uh|ryP NIfPN3o4OiCq MXfEUXNQ M17XcYlv\HWlZYOgZZBweHSxc3nz NX7uTJE3OjJ4NUO5Olg>
92.1 MmHIRZBweHSxc3nzJGF{e2G7 NF\NOIM2KM7:TR?= M2rmfVczKGh? NIPwcmVFVVOR MUnpcoR2[2W|IHHwc5B1d3OrczDzbYdvcW[lYX70cJk> NGfHb2kzOjZ3M{m2PC=>
Mel202 MVzGeY5kfGmxbjDBd5NigQ>? Mn;mOUDPxE1? M3Gy[FI1KGh? M1S0VolvcGmkaYTzJIV5eHKnc4Ppc44h[W6mIIDoc5NxcG:{eXzheIlwdiCxZjDQT2MhcXOxZn;ycZM> NFLs[3AzOjZ3M{m2PC=>
Omm1.3 MoTySpVv[3Srb36gRZN{[Xl? NHvrbHU2KM7:TR?= MUSyOEBp NGSxSG9qdmirYnn0d{BmgHC{ZYPzbY9vKGGwZDDwbI9{eGixconsZZRqd25ib3[gVGtEKGm|b3\vdo1{ NXXX[XdDOjJ4NUO5Olg>
92.1 Moe1SpVv[3Srb36gRZN{[Xl? M4rvPVUh|ryP MoXUNlQhcA>? NFTXZpdqdmirYnn0d{BmgHC{ZYPzbY9vKGGwZDDwbI9{eGixconsZZRqd25ib3[gVGtEKGm|b3\vdo1{ MmnKNlI3PTN7Nki=
HBL1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Moj0NE4yPi1{MDFOwG0> Mn3uOUBl NIDsNWFKSzVyPUCuOUDPxE1? MUWyNVMzPDl{MB?=
TMD8 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnTUY0xNjF4LUKwJO69VQ>? M2PFcFUh\A>? M4DaRWlEPTB;MD6yJO69VQ>? MoLpNlE{OjR7MkC=
OCI-Ly10 NUm4OW55T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;PNE4yPi1{MDFOwG0> MUO1JIQ> MoW2TWM2OD1zLkOg{txO NFvSRVQzOTN{NEmyNC=>
U2932 NYjwdGNQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWSwMlE3NTJyIN88US=> NHzK[2g2KGR? NV7wU5VUUUN3ME2xNEDPxE1? MYeyNVMzPDl{MB?=
OCI-Ly3 NEjjd2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFPoepMxNjF4LUKwJO69VQ>? MkC3OUBl NWfSd|NnUUN3MP-8olIxKM7:TR?= M3rKT|IyOzJ2OUKw
SuDHL2 MmTwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37JXlAvOTZvMkCg{txO M{HVTVUh\A>? NXKyVYhDUUN3MP-8olIxKM7:TR?= NIPBeG4zOTN{NEmyNC=>
SuDHL4 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\FNE4yPi1{MDFOwG0> NXrQVY1jPSCm MojVTWM2OO,:nkKwJO69VQ>? MlvtNlE{OjR7MkC=
DB MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3nTNFAvOTZvMkCg{txO NUj5bZQxPSCm NXLVfWNjUUN3MP-8olIxKM7:TR?= MYOyNVMzPDl{MB?=
Jurkat IL-2 MlnES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHzNmlKSzVyPU[uO|EhyrFiMz63OkDPxE1? MmW0NVk6PDB{NUm=
PBMC IL-2 NYT0VmJYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIrS[5dKSzVyPUSuPFQhyrFiMT63NEAh|ryP MnLPNVk6PDB{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 slightly soluble or 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
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