Perifosine is an oralAktinhibitor which inhibits proliferation of different tumor cell lines withIC₅₀s of 0.6-8.9 μM.

The IC₅₀for growth of Ntv-a/LacZ cell lines is determined by MTT assay. When the cells are cultured for 48 hours in 10% FCS-supplemented media, the IC₅₀for cells with constitutively active PDGF, Ras, or Akt signaling is similar and found to be ~45 μM^[1].Perifosine, a oral-bioavailable alkylphospholipid (ALK), on the cell cycle kinetics of immortalized keratinocytes (HaCaT) as well as head and neck squamous carcinoma cells. Proliferation is assessed by the incorporation of [³H]thymidine into cellular DNA. Exposure to Perifosine (0.1-30 μM) for 24 h results in a dose-dependent inhibition of [³H]thymidine uptake in all cell lines tested. The IC₅₀s for growth are between 0.6 and 8.9 μM, reaching IC₈₀s of ~10 μM. Perifosine blocks cell cycle progression of head and neck squamous carcinoma cells at G₁-S and G₂-M by inducing p21^WAF1, irrespective of p53 function, and may be exploited clinically because the majority of human malignancies harborp53mutations. Perifosine (20 μM) induces both G₁-S and G₂-M cell cycle arrest, together with p21^WAF1expression in bothp53wild-type andp53^-/-clones^[2].

Mice are identified with tumors by bioluminescence imaging and either treated them with 100 mg/kg Temozolomide, or 30 mg/kg Perifosine, or a combination with 100 mg/kg Temozolomide and 30 mg/kg Perifosine (Temozolomide+Perifosine) for 3 to 5 days. The mice are sacrificed and tumors analyzed histologically for cell proliferation by Ki-67 immunostaining. Ki-67 staining index is significantly reduced in mice treated with either Temozolomide (Ki-67 staining index=5.5±1.2%, n=4, P=0.0019) or Perifosine (Ki-67 staining index=3.2±1.1%, n=3, P=0.001) compared with Control, demonstrating the inhibitory effect on proliferation. Most importantly, the tumors treated with Temozolomide+Perifosine have the lowest Ki-67 staining index (1.7±1.2%, n=3, P=0.0005). The additional treatment with Perifosine results in a significantly lower proliferation rate than Temozolomide alone (P=0.0087)^[1]. Perifosine markedly decreases p-Akt from 10 min to 24 hours and subsequently, moderately decreased p-S6 from 1h to 24 h after injection^[3].

461.66

Solid

C₂₅H₅₂NO₄P

157716-52-4

哌立福新；派立福新

Room temperature in continental US; may vary elsewhere.

H₂O : 100 mg/mL(216.61 mM;Need ultrasonic)

DMF :< 1 mg/mL(insoluble)

DMSO :< 1 mg/mL(insoluble or slightly soluble)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： PBS

  Solubility: 50 mg/mL (108.30 mM); Clear solution; Need ultrasonic