Catalog No.S2791 Synonyms: AEB071
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.
Cited by 5 Publications
2 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.
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2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
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|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.|
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.  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. 
|In vivo||Sotrastaurin (80 mg/kg) results in significant inhibition of in vivo tumor growth in a subcutaneous TMD8 xenograft model in SCID.  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. |
|In vitro||DMSO||87 mg/mL (198.41 mM)|
|Ethanol||2 mg/mL (4.56 mM)|
|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.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02273219||Recruiting||Uveal Melanoma||Richard D. Carvajal|Columbia University||November 2014||Phase 1|
|NCT01854606||Active, not recruiting||CD79 Mutant or ABC-subtype Diffuse Large B-Cell Lymphoma||Novartis Pharmaceuticals|Novartis||December 2013||Phase 1|Phase 2|
|NCT01801358||Terminated||Uveal Melanoma||Array BioPharma||August 2013||Phase 1|Phase 2|
|NCT01430416||Recruiting||Uveal Melanoma||Novartis Pharmaceuticals|Novartis||December 2011||Phase 1|
|NCT01402440||Terminated||Diffuse Large B-Cell Lymphoma||Novartis Pharmaceuticals|Novartis||November 2011||Phase 1|
|NCT00572585||Terminated||Ulcerative Colitis||Novartis Pharmaceuticals|Novartis||April 2010||Phase 2|
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.
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Frequently Asked Questions
Could you give me the information about how to prepare Sotrastaurin for oral administration in mice?
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.