中文名称: Perifosine
英文名称: Perifosine
CAS No: 157716-52-4
分子式: C25H52NO4P
分子量: 461.66
EINEC: 639966
P10091 Perifosine ≥98% (psaitong)
包装规格:
5mg 25mg 100mg in glass bottle
溶解性:
溶于水(8mg/ml)
产品描述:

基本信息

产品编号:P10091

产品名称:Perifosine

CAS:

157716-52-4

 

储存条件

粉末

-20℃

四年

 

 

分子式:

C25H52NO4P

溶于液体

-80℃

六个月

分子量

461.66

-20℃

一个月

化学名: 

 

 

Solubility (25°C)

 

体外

DMSO

92mg/mL (199.28mM)

Ethanol

92mg/mL (199.28mM)

Water

Insoluble

体内(现配现用)

water

8mg/mL

1mg/ml表示微溶或不溶。

普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。

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。

 

制备储备液

 

浓度

 

溶液体积

质量

 

1mg

 

5mg

 

10mg

1mM

2.1661mL

10.8305mL

21.6610mL

5mM

0.4332mL

2.1661mL

4.3322mL

10mM

0.2166mL

1.0830mL

2.1661mL

50mM

0.0433mL

0.2166mL

0.4332mL

 

生物活性

产品描述

一种Akt抑制剂。

靶点/IC50

Akt

Autophagy

 

体外研究

The IC50 for growth of Ntv-a/LacZ cell lines is determined by MTT assay. When the cells are cultured for 48 hours in 10% FCSsupplemented media, the IC50 for cells with constitutively active PDGF, Ras, or Akt signaling is similar and found to be ~45μ M.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 (0.1-30μM) for 24h results in a dose-dependent inhibition of [3H]thymidine uptake in all progression of head and neck squamous carcinoma cells at G1-S and G2-M by inducing p21WAF1, irrespective of p53 function, and may be exploited clinically because the majority of human malignancies harbor p53 mutations. Perifosine (20μM) induces both G1-S and G2-M cell cycle arrest, together with p21WAF1 expression in both p53 wild-type and p53-/- clones.

 

体内研究

Mice are identified with tumors by bioluminescence imaging and either treated them with 100mg/kg Temozolomide, or 30mg/kg Perifosine, or a combination with 100mg/kg Temozolomide and 30mg/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). Perifosine markedly decreases p-Akt from 10 min to 24 hours and subsequently, moderately decreased p-S6 from 1h to 24h after injection.

 

推荐实验方法(仅供参考)

激酶实验:

Exponentially growing cells (HN12, HN30, and HaCaT) are lysed, and 500μg of total cellular protein are used to immunoprecipitate active cdc2 and cdk2 complexes. After capturing with gammabind G Sepharose and subsequent washes, the active immune complexes are assessed for activity in the presence of increasing concentrations of Perifosine (0.1-30μM) or flavopiridol (300nM) in the kinase assay buffer containing [γ-32P]ATP (3000 Ci/mmol) and 0.2mg/mL histone H1, 25μM ATP. Reactions are incubated at 37°C for 30 min and terminated by the addition of SDS-gel loading buffer, resolved in SDSPAGE, and dried gels are subjected to autoradiography and phosphorimaging.

 

细胞实验:

 

Cell proliferation studies by measuring the uptake of [3H]thymidine is performed. Briefly, HNSCC and HaCaT cells (1-2×104/well) are grown overnight in 24-well plates and exposed to either Perifosine (0.1-30μM) or PBS (control). After treatment (24-48h), cells are pulsed with [3H]thymidine (1 μCi/well) for 4-6h, fixed (5% trichloroacetic acid), and solubilized (0.5M NaOH) before scintillation counting. Experiments are performed in triplicates.

 

动物实验:

 

Mice

Drug treatment of tumor-bearing mice. Image-positive Ef-luc Ntv-a mice are treated daily with i.p. administration of buffer alone as a control, or i.p. administration of 100mg/kg Temozolomide, or oral administration of 30 mg/kg Perifosine, or a combination with Perifosine and Temozolomide for 3 to 5 days. The mean doses of the treatments are: Control, 5 (all five); Temozolomide, 3.75 (three to five); Perifosine, 3.75 (three to four); and Perifosine+Temozolomide, 3 (all three). Control buffer solution consisted of 5% DMSO and 1% Tween 80 in distilled water. Rats To further determine whether the paradoxical effect of rapamycin on S6 phosphorylation is related to upstream signals of Akt-mTOR, rats are treated with Perifosine (20mg/kg, ip, once), an Akt inhibitor, 30 min before rapamycin administration. Rats are sacrificed 1 h or 6 h after rapamycin injection.

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

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    *选择对应的单位 *空出希望得到的变量,填写另外两个变量

用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )

  • * = *

连续稀释计算器方程

  • 连续稀释

  • 初始浓度:
  • 稀释倍数:
  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):