中文名:Sotrastaurin (AEB071)
英文名:Sotrastaurin (AEB071)
纯度:Moligand™,10mM in DMSO
货号:S408260
Cas号:425637-18-9
存储温度:-80℃储存
运输条件:特低温运输
产品介绍:
Information
Sotrastaurin (AEB071) Sotrastaurin (AEB071) is a potent and selective pan- PKC inhibitor, mostly for PKCθ with K i of 0.22 nM in a cell-free assay; inactive to PKCζ. Phase 2.
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. 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.
Cell Data
cell lines:
Concentrations:
Incubation Time:
Powder Purity:≥98%
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关键字: 索特拉斯图林 (AEB071);3-(1H-indol-3-yl)-4-(2-(4-methylpiperazin-1-yl)quinazolin-4-yl)-1H-pyrrole-2,5-dione
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