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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Cited by 10 Publications

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 MYnGeY5kfGmxbjDBd5NigQ>? NXTkTVJ7OTByIH7N M3jqXVMhcA>? M33lOWROW09? NGXBRmJqdmirYnn0d{BzWk6DIIP5cpRp\XOrcx?= NW\U[lRSOjV4OUGxOVg>
HUVECs  M4fMW2Z2dmO2aX;uJGF{e2G7 M{HtXFUxOG6P M37xdVEhcA>? NGSzbFRT\WS3Y3XzJGRVYC2Wcnnn[4Vz\WRiRX7kc5Rp\WyrYXygSJl{\nWwY4Tpc44> M3OxXVI2PjN2NUO4
A549 MXLGeY5kfGmxbjDBd5NigQ>? MUGwMlHDqM7:TR?= MUCyOEBp MnzJ[IVkemWjc3XzJJRp\SC{ZXzheIl3\SCSS1Ot{tEhdGW4ZXygc44h[2WubDDt[Y1jemGwZTDjc5Rz\WG2ZXSgRXMuUVZ? M2L1elI2OjF6MU[x
A549 M3fSfGZ2dmO2aX;uJGF{e2G7 MUWwMlHDqM7:TR?= M4Tp[|I1KGh? Ml7SdoVlfWOnczD0bIUh\XiycnXzd4lwdiCuZY\lcJMhd2ZiTV3QMVItKE2PUD25JIFv\CCrboTl[5JqdiEQskG= MVuyOVIyQDF4MR?=
A549 MnK3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXzNE4yyqEQvF2= MUmyOEBp MXvlcohidmOnczDndo94fGhiaX7obYJqfGmxbjDjc5Rz\WG2ZXSge4l1cCCDUz3JWi=> MWKyOVIyQDF4MR?=
Mel202 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmf6NE42KM7:TR?= MoTGN{Bp NUe2fHk1TE2VTx?= MkXl[Y5p[W6lZYOgTXIucW6mdXPl[EBz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJk> MVGyOFU6PTN6NR?=
92.1 NETKXlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonFNE42KM7:TR?= M3jlfVMhcA>? M16xZWROW09? MlTr[Y5p[W6lZYOgTXIucW6mdXPl[EBz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJk> NF7kWWIzPDV7NUO4OS=>
OCM3 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXOwMlUh|ryP M3zFdFMhcA>? NI\3NYpFVVOR NVTMbFhX\W6qYX7j[ZMhUVJvaX7keYNm\CC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHl? M4XFU|I1PTl3M{i1
Mel202 MoHHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4PQeVAvPSEQvF2= MlHwN{Bp Ml7hSG1UVw>? MUDpcoNz\WG|ZYOgTXIucW6mdXPl[EBk\WyuIHP5Z4xmKGG{cnXzeOKh MlXzNlQ2QTV|OEW=
92.1 NF\BN3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jpW|AvPSEQvF2= NX\mSnZtOyCq MlXLSG1UVw>? NGm5Zo9qdmO{ZXHz[ZMhUVJvaX7keYNm\CClZXzsJIN6[2ynIHHydoV{fMLi MlfTNlQ2QTV|OEW=
OCM3 M2DaZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\NOFAvPSEQvF2= Mn3SN{Bp Mn;6SG1UVw>? NE\VSXNqdmO{ZXHz[ZMhUVJvaX7keYNm\CClZXzsJIN6[2ynIHHydoV{fMLi MoLBNlQ2QTV|OEW=
Jeko-1 NILCeYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;CSZUxNTRizszN M1TDVWROW09? NXezUmh6cW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? M1\SSlI1OzZ{OUO1
Mino MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPONE01KM7:TR?= MoPTSG1UVw>? MlXDbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> M4TDblI1OzZ{OUO1
Rec-1 NG\4RnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzHdoZlOC12IN88US=> NXf5OGNYTE2VTx?= NF;GNllqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 MVOyOFM3Ojl|NR?=
SP49 NIj1NJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUiwMVQh|ryP M1TNRmROW09? M{\6SolvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> MkKyNlQ{PjJ7M{W=
Jeko-1 M4HtOGZ2dmO2aX;uJGF{e2G7 M2jDclIvPSEQvF5CpC=> NIi0PIcyOiCq M4rLfWROW09? NEHIbFRld3ewcnXneYxifGW|IF7GMe67SiC2YYLn[ZQh\2WwZYO= M{HqN|I1OzZ{OUO1
Mino MVXGeY5kfGmxbjDBd5NigQ>? MkDyNk42KM7:TdMg Mn:2NVIhcA>? MnTpSG1UVw>? NEjtOnpld3ewcnXneYxifGW|IF7GMe67SiC2YYLn[ZQh\2WwZYO= NXTGWpI{OjR|NkK5N|U>
Rec-1 MV;GeY5kfGmxbjDBd5NigQ>? NWnB[mVLOi53IN88UeKh MUKxNkBp MkfKSG1UVw>? NUmxZ5I4\G:5boLl[5Vt[XSnczDOSk3PwkJidHHy[4V1KGenbnXz MnuyNlQ{PjJ7M{W=
SP49 NFfOOFdHfW6ldHnvckBCe3OjeR?= MlTBNk42KM7:TdMg NGPpfogyOiCq NFjCZ3VFVVOR NWjmWIp2\G:5boLl[5Vt[XSnczDOSk3PwkJidHHy[4V1KGenbnXz NEPZS4EzPDN4MkmzOS=>
CD3+ T  MmLDSpVv[3Srb36gRZN{[Xl? MUCwMVUxOCCwTR?= NFHrO3kyKGh? NULzS4pkcW6qaXLpeJMhVkZvzsrCJJBpd3OyaH;yfYxifGmxbjDpckBiKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= NWPkb4VYOjN3N{OyPFM>
Mel202 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HOclAuPSEQvF2= NEjuPVU4OiCq MoL1SG1UVw>? MWPpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 Ml2yNlI3PTN7Nki=
Omm1.3 NYrYSWRCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\tNE02KM7:TR?= MW[3NkBp MXLEUXNQ MknibY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MVKyNlY2Ozl4OB?=
92.1 NWrvUFV[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\HWFAuPSEQvF2= M1rCRlczKGh? MYDEUXNQ MkDNbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MnfaNlI3PTN7Nki=
Mel202 NHHuO4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1roflUh|ryP NEH6bpkzPCCq NVyyUVNzTE2VTx?= M1HsRYlv\HWlZYOgS|Eh[XK{ZYP0xsA> MU[yNlY2Ozl4OB?=
Omm1.3 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnITXNNPSEQvF2= NXy3Tlh1OjRiaB?= MXLEUXNQ MU\pcoR2[2W|IFexJIFzemW|dNMg Mnu4NlI3PTN7Nki=
92.1 MlvuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;EOVI2KM7:TR?= NEDSNVAzPCCq MlnNSG1UVw>? M{HuOolv\HWlZYOgS|Eh[XK{ZYP0xsA> MYKyNlY2Ozl4OB?=
Mel202 NFfSU25CeG:ydH;zbZMhSXO|YYm= NV;xe|BvPSEQvF2= M{PmNlczKGh? MV\EUXNQ NWr3UIxscW6mdXPld{BieG:ydH;zbZMhe2yrZ3j0cJk> NH36cWUzOjZ3M{m2PC=>
Omm1.3 MmfnRZBweHSxc3nzJGF{e2G7 M3i0flUh|ryP MWm3NkBp NHvtN4ZFVVOR MkPIbY5lfWOnczDhdI9xfG:|aYO= NWfBRYtTOjJ4NUO5Olg>
92.1 NFTQ[lNCeG:ydH;zbZMhSXO|YYm= MkPMOUDPxE1? M2Lv[lczKGh? NXvWN5BsTE2VTx?= MVzpcoR2[2W|IHHwc5B1d3OrczDzbYdvcW[lYX70cJk> MUWyNlY2Ozl4OB?=
Mel202 NYCwfYdqTnWwY4Tpc44hSXO|YYm= MXO1JO69VQ>? MVmyOEBp MlzrbY5pcWKrdIOg[ZhxemW|c3nvckBidmRicHjvd5Bpd3K7bHH0bY9vKG:oIGDLR{Bqe2:ob4Ltdy=> M3qzV|IzPjV|OU[4
Omm1.3 MVjGeY5kfGmxbjDBd5NigQ>? MYS1JO69VQ>? NWXnWYFKOjRiaB?= NIDoVnhqdmirYnn0d{BmgHC{ZYPzbY9vKGGwZDDwbI9{eGixconsZZRqd25ib3[gVGtEKGm|b3\vdo1{ NX;uelhiOjJ4NUO5Olg>
92.1 M3HudGZ2dmO2aX;uJGF{e2G7 M3zWcFUh|ryP MWeyOEBp NFflTXVqdmirYnn0d{BmgHC{ZYPzbY9vKGGwZDDwbI9{eGixconsZZRqd25ib3[gVGtEKGm|b3\vdo1{ NY\uSXBkOjJ4NUO5Olg>
HBL1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUfSNIJYOC5zNj2yNEDPxE1? NWPPbJFPPSCm NU\4[YFZUUN3ME2wMlUh|ryP MmKyNlE{OjR7MkC=
TMD8 NY\lTXJ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjTNE4yPi1{MDFOwG0> M33WWFUh\A>? NXrIeJRzUUN3ME2wMlIh|ryP NFfWT|IzOTN{NEmyNC=>
OCI-Ly10 NFzEbmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUGwMlE3NTJyIN88US=> M{\O[VUh\A>? NGrMS|VKSzVyPUGuN{DPxE1? M{PhSVIyOzJ2OUKw
U2932 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TJ[FAvOTZvMkCg{txO MVK1JIQ> NFv1NpJKSzVyPUGwJO69VQ>? M{DlNFIyOzJ2OUKw
OCI-Ly3 NUHWdHljT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWWwMlE3NTJyIN88US=> NV\EWW8yPSCm MoXkTWM2OO,:nkKwJO69VQ>? Mn2zNlE{OjR7MkC=
SuDHL2 NHrtXIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYj3SpJLOC5zNj2yNEDPxE1? NEe2Oos2KGR? NISzclVKSzVy78{eNlAh|ryP NGHl[JczOTN{NEmyNC=>
SuDHL4 NVvYZnpkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVKwMlE3NTJyIN88US=> NFzreIM2KGR? MnH1TWM2OO,:nkKwJO69VQ>? NVj4b4ptOjF|MkS5NlA>
DB MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPSNE4yPi1{MDFOwG0> NVHHN|NRPSCm MV7JR|Ux97zgMkCg{txO NGGxXYozOTN{NEmyNC=>
Jurkat IL-2 NGKxPItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk[yTWM2OD14LkexJOKyKDNwN{[g{txO M3XyRlE6QTRyMkW5
PBMC IL-2 NYHZT5NTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjQTWM2OD12Lki0JOKyKDFwN{CgJO69VQ>? NXTIVoV[OTl7NECyOVk>

... 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
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
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
NCT01854606 Completed CD79 Mutant or ABC-subtype Diffuse Large B-Cell Lymphoma Novartis Pharmaceuticals|Novartis December 5 2013 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