产品信息
抗原名称
PKCθ；PKCβ1；PKCα；PKCη；PKCδ
商品描述
Sotrastaurin is a protein kinase C inhibitor for the prevention of transplant rejection and treatment of psoriasis.
分子量
438.48
纯度
>98%
可溶性
DMSO ：87 mg/mL (198.41 mM)
外观
powder
In vitro(体外研究)
In cell-free kinase assays, Sotrastaurin (AEB071) inhibited PKC, with K(i) values in the subnanomolar to low nanomolar range. Upon T-cell stimulation, AEB071 markedly inhibited in situ PKC catalytic activity. In primary human and mouse T cells, AEB071 treatment effectively abrogated at low nanomolar concentration markers of early T-cell activation. Growth inhibition was observed in GNAQ/GNA11-mutant cells with AEB071 versus no activity in wild-type cells. In the GNAQ-mutant cells, AEB071 decreased phosphorylation of myristoylated alanine-rich C-kinase substrate, a substrate of PKC, along with ERK1/2 and ribosomal S6, but persistent AKT activation was present.
In vivo(体内研究)
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.
背景
别名
AEB071; AEB 071; AEB-071
分子式
C25H22N6O2
CAS号
425637-18-9
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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