Perifosine (KRX-0401) is an oral-active, alkyl-phosphocholine Akt inhibitor with potential antineoplastic activity.

Akt:4.7 μM

在神经胶质瘤中,Perifosine激活Akt和Ras-ERK1/2途径.Perifosine诱导血小板和白细胞增多,导致移植骨髓瘤的凋亡.

在MM.1S细胞中,Perifosine（10 μM ）能够完全抑制Akt的磷酸化。在永生化角质形成细胞和头颈部鳞状癌细胞中（IC50=0.6-8.9 μM）,Perifosine抑制细胞增殖。在小鼠的神经胶质祖细胞中,Perifosine通过减少Akt的磷酸化水平和细胞外信号调节激酶,诱导细胞周期停滞在G1和G2,引起细胞生长抑制。在人类肝癌细胞中,Perifosine通过阻断Akt的磷酸化,诱导细胞周期停滞和细胞凋亡。

Akt kinase assay: MM.1S cells are cultured in the presence or absence of perifosine (5 μM, 6 hours) and then stimulated with IL-6 (20 ng/mL, 10 minutes). In vitro akt kinase assay is then carried out using the Akt Kinase Assay Kit.

Cells are incubated in the medium with 10% FCS for 48 hours with indicated concentration of Periosine. Cell viability is determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. (Cell Proliferation Kit I; Roche). The absorbance at 590 nm is recorded using the 96-well plate reader.(Only for Reference)