Perifosine (KRX-0401)

MM.1S MM cells are inoculated subcutaneously in the right flank of Beige-nude-xid (BNX) mice (5 to 6 weeks old).

Piperidinium, 4-[[hydroxy(octadecyloxy)phosphinyl]oxy]-1, 1-dimethyl-, inner salt

0, 15, 30 and 45 uM

250 mg/kg/wk or 36 mg/kg/d

4.7 uM [1], 4.7 uM [1], 4.7 uM [1], 4.7 uM [1], 4.7 uM [1], 4.7 uM [1]

Perifosine combining with temozolomide reduces tumor proliferation (a PDGF-driven gliomagenesis) in vivo. The results indicate that Perifosine is an effective drug in gliomas in which Akt and Ras-Erk 1/2 pathways are frequently activated, and may be new candidate for glima treatment in the clinic. [2] Both oral daily and weekly administration of Perifosine significantly reduce human MM tumor growth and increase survival, compared with control animals treated with PBS vehicle only. [3] Perifosine induces thrombocytosis and leukocytosis and increases myelopoiesis in murine marrow and spleen, whereas it causes apoptosis in myeloma xenografts. [5]

[3], Akt kinase assay, MM.1S cells are cultured in the presence or absence of perifosine (5 uM, 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.

461, 66

Data from [Cytotechnology, 2010, 62, 449-460], Perifosinepurchased from Selleck, Induction of apoptosis in hepatoma cells by treatment for 48 h with 10 M perifosine. The treated cells were stained with DAPI and the apoptotic morphological changes in the nuclear chromatin were observed under a fluorescent microscope.

DMSO <1 mg/mL, Water 8 mg/mL, Ethanol 15 mg/mL