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 M4rDeGZ2dmO2aX;uJGF{e2G7 M{nEWVExOCCwTR?= NVWyT4wxOyCq NEXJS|RFVVOR Mnm5bY5pcWKrdIOgdnJPSSC|eX70bIV{cXN? NFXtSVYzPTZ7MUG1PC=>
HUVECs  MX7GeY5kfGmxbjDBd5NigQ>? M1H0OVUxOG6P MYWxJIg> Mk[0VoVlfWOnczDEWHguXHKrZ3fldoVlKEWwZH;0bIVtcWGuIFT5d4Z2dmO2aX;u M{jBWFI2PjN2NUO4
A549 MXjGeY5kfGmxbjDBd5NigQ>? NXfT[XZKOC5zwrFOwG0> MWOyOEBp NFjDW5Vl\WO{ZXHz[ZMhfGinIILlcIF1cX[nIGDLR{3PuSCuZY\lcEBwdiClZXzsJI1mdWK{YX7lJINwfHKnYYTl[EBCWy2LVh?= M1jER|I2OjF6MU[x
A549 Mkn5SpVv[3Srb36gRZN{[Xl? Ml71NE4yyqEQvF2= M1vs[|I1KGh? MUXy[YR2[2W|IITo[UBmgHC{ZYPzbY9vKGyndnXsd{Bw\iCPTWCtNkwhVU2SLUmgZY5lKGmwdHXndolvKM7{MR?= NIjpPI4zPTJzOEG2NS=>
A549 MojOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;CNE4yyqEQvF2= NWC4N4FzOjRiaB?= NGTVUZpmdmijbnPld{Boem:5dHigbY5pcWKrdHnvckBkd3S{ZXH0[YQhf2m2aDDBV{1KXg>? NHvifo0zPTJzOEG2NS=>
Mel202 NHnNOXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXKwMlUh|ryP Ml;WN{Bp NFHT[mNFVVOR MUHlcohidmOnczDJVk1qdmS3Y3XkJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fS=> MlnYNlQ2QTV|OEW=
92.1 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PJe|AvPSEQvF2= MX[zJIg> MXrEUXNQ MX;lcohidmOnczDJVk1qdmS3Y3XkJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fS=> NHHz[lAzPDV7NUO4OS=>
OCM3 NYfDOldbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3roNlAvPSEQvF2= NIfqc4c{KGh? M2[xT2ROW09? NHvuS3RmdmijbnPld{BKWi2rbnT1Z4VlKHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gQ>? NXrMTYFxOjR3OUWzPFU>
Mel202 M4DMSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWmwRWlMOC53IN88US=> M1\lUVMhcA>? NFi0Z4RFVVOR M3vsU4lv[3KnYYPld{BKWi2rbnT1Z4VlKGOnbHygZ5lkdGViYYLy[ZN1yqB? MoDaNlQ2QTV|OEW=
92.1 NV\5cGhET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rn[lAvPSEQvF2= NXTEfWUyOyCq NImyVHJFVVOR MoPSbY5kemWjc3XzJGlTNWmwZIXj[YQh[2WubDDjfYNt\SCjcoLld5TDqA>? NFnHO3YzPDV7NUO4OS=>
OCM3 NILQemVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYCwMlUh|ryP NXPJTXNEOyCq NXjITXZyTE2VTx?= Mn25bY5kemWjc3XzJGlTNWmwZIXj[YQh[2WubDDjfYNt\SCjcoLld5TDqA>? MnHVNlQ2QTV|OEW=
Jeko-1 NYDVOm5PT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILMb|gxNTRizszN NXrQb2tmTE2VTx?= Ml64bY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NVrSXHNNOjR|NkK5N|U>
Mino NWDld2YzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYWwMVQh|ryP M3OycWROW09? NV7oXldKcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? MojLNlQ{PjJ7M{W=
Rec-1 M3jlUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPXNE01KM7:TR?= NX3OdldNTE2VTx?= NXnuSnJxcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NVKxeZFsOjR|NkK5N|U>
SP49 NGP2Z3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWqwMVQh|ryP NUTKO5F3TE2VTx?= MUjpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 M3TkbFI1OzZ{OUO1
Jeko-1 NHnTZmhHfW6ldHnvckBCe3OjeR?= Mn36Nk42KM7:TdMg NXHuc5BYOTJiaB?= NXX6dlZwTE2VTx?= MXrkc5dvemWpdXzheIV{KE6ILd86RkB1[XKpZYSg[4Vv\XN? NXzZcnV{OjR|NkK5N|U>
Mino NH\oZ3pHfW6ldHnvckBCe3OjeR?= MljxNk42KM7:TdMg MYCxNkBp NEXEd2dFVVOR NXvPXWc4\G:5boLl[5Vt[XSnczDOSk3PwkJidHHy[4V1KGenbnXz NU\PcHhmOjR|NkK5N|U>
Rec-1 M3nsSmZ2dmO2aX;uJGF{e2G7 NEK0c4UzNjVizszNxsA> NYDCeI9tOTJiaB?= M3\tbWROW09? M3PqVoRwf26{ZXf1cIF1\XNiTl[t{tpDKHSjcnfleEBo\W6ncx?= MVOyOFM3Ojl|NR?=
SP49 MVPGeY5kfGmxbjDBd5NigQ>? MUOyMlUh|ryPwrC= MonmNVIhcA>? NYi2UW9OTE2VTx?= M33tZYRwf26{ZXf1cIF1\XNiTl[t{tpDKHSjcnfleEBo\W6ncx?= NUTZPGhLOjR|NkK5N|U>
CD3+ T  M2Hq[WZ2dmO2aX;uJGF{e2G7 NVTL[2w3OC13MECgcm0> MlzJNUBp NYLaOFJ2cW6qaXLpeJMhVkZvzsrCJJBpd3OyaH;yfYxifGmxbjDpckBiKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= MoHQNlM2PzN{OEO=
Mel202 NYXEUnNYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUmwMVUh|ryP MkTIO|IhcA>? NF\ZcJdFVVOR NYPne41HcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? M2rQbFIzPjV|OU[4
Omm1.3 NFn2UlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTz[oxUOC13IN88US=> MXK3NkBp MmPpSG1UVw>? MnrabY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> M2LlPFIzPjV|OU[4
92.1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE[yflQxNTVizszN M2DKb|czKGh? M1\CNGROW09? M3HEZ4lvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> MXWyNlY2Ozl4OB?=
Mel202 Mn7tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEjXfpQ2KM7:TR?= NHS1SXIzPCCq NUX6NYMxTE2VTx?= M2H5SYlv\HWlZYOgS|Eh[XK{ZYP0xsA> NFfDfnIzOjZ3M{m2PC=>
Omm1.3 MofrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWC1JO69VQ>? M2ThSlI1KGh? NWPXfY1zTE2VTx?= MnLJbY5lfWOnczDHNUBienKnc4VCpC=> M4DOTVIzPjV|OU[4
92.1 NFXpUmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1PYc|Uh|ryP MWiyOEBp Mo\vSG1UVw>? MYHpcoR2[2W|IFexJIFzemW|dNMg NV;lUVZTOjJ4NUO5Olg>
Mel202 Ml3vRZBweHSxc3nzJGF{e2G7 MUO1JO69VQ>? M4TxfFczKGh? MWLEUXNQ M4PwSIlv\HWlZYOgZZBweHSxc3nzJJNtcWeqdHz5 M3\yTFIzPjV|OU[4
Omm1.3 MnPyRZBweHSxc3nzJGF{e2G7 NHLPUZE2KM7:TR?= NEKxOXI4OiCq M2DWOmROW09? MWLpcoR2[2W|IHHwc5B1d3Orcx?= NEnlSGczOjZ3M{m2PC=>
92.1 M4rmVmFxd3C2b4Ppd{BCe3OjeR?= Ml\rOUDPxE1? Ml\aO|IhcA>? M{\oWWROW09? MnjqbY5lfWOnczDhdI9xfG:|aYOgd4lodmmoY3HueIx6 M1X6[FIzPjV|OU[4
Mel202 MVXGeY5kfGmxbjDBd5NigQ>? NHfSTIg2KM7:TR?= NXrvR3MxOjRiaB?= NUPXXJlTcW6qaXLpeJMh\XiycnXzd4lwdiCjbnSgdIhwe3Cqb4L5cIF1cW:wIH;mJHBMSyCrc3;mc5Juew>? NYG4OnhVOjJ4NUO5Olg>
Omm1.3 M3LxcGZ2dmO2aX;uJGF{e2G7 NFj6bpI2KM7:TR?= NEPTR|YzPCCq MVvpcohq[mm2czDlfJBz\XO|aX;uJIFv\CCyaH;zdIhwenmuYYTpc44hd2ZiUFvDJIl{d2[xcn3z M4LPR|IzPjV|OU[4
92.1 MUTGeY5kfGmxbjDBd5NigQ>? MmXSOUDPxE1? NImw[FkzPCCq NWfaRYRJcW6qaXLpeJMh\XiycnXzd4lwdiCjbnSgdIhwe3Cqb4L5cIF1cW:wIH;mJHBMSyCrc3;mc5Juew>? MV:yNlY2Ozl4OB?=
HBL1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3i2SFAvOTZvMkCg{txO NF\FcIg2KGR? MWHJR|UxRTBwNTFOwG0> Mm\CNlE{OjR7MkC=
TMD8 MorBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlraNE4yPi1{MDFOwG0> M2THd|Uh\A>? MYrJR|UxRTBwMjFOwG0> MmKzNlE{OjR7MkC=
OCI-Ly10 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\yPFVsOC5zNj2yNEDPxE1? NFXOSZM2KGR? NF7PWZlKSzVyPUGuN{DPxE1? MlvmNlE{OjR7MkC=
U2932 NGr4ZpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFGzTmwxNjF4LUKwJO69VQ>? MVu1JIQ> MWrJR|UxRTFyIN88US=> MYKyNVMzPDl{MB?=
OCI-Ly3 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnTwNE4yPi1{MDFOwG0> NIXRVmY2KGR? M3jHW2lEPTExvK6yNEDPxE1? MXGyNVMzPDl{MB?=
SuDHL2 MkXPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWCwMlE3NTJyIN88US=> NH[wbnU2KGR? MkHtTWM2OO,:nkKwJO69VQ>? M3q0cVIyOzJ2OUKw
SuDHL4 NV60[4NtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17WTVAvOTZvMkCg{txO NF;J[Vc2KGR? MlHiTWM2OO,:nkKwJO69VQ>? NX3XUWd3OjF|MkS5NlA>
DB MoHZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXPUXdIOC5zNj2yNEDPxE1? M1HjbVUh\A>? MlvwTWM2OO,:nkKwJO69VQ>? M3PET|IyOzJ2OUKw
Jurkat IL-2 NInLU5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVn5XItUUUN3ME22MlcyKMLzIEOuO|Yh|ryP NUnxSGJsOTl7NECyOVk>
PBMC IL-2 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHWTWM2OD12Lki0JOKyKDFwN{CgJO69VQ>? M1z5[VE6QTRyMkW5

... 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