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.
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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.
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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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