中文名称: | Perifosine | ||||
---|---|---|---|---|---|
英文名称: | Perifosine | ||||
别名: | 哌立福新 KRX-0401;4-((Hydroxy(octadecyloxy)phosphinyl)oxy)-1,1-dimethylpiperidinium inner salt | ||||
CAS No: | 157716-52-4 | 分子式: | C25H52NO4P | 分子量: | 461.66 |
CAS No: | 157716-52-4 | ||||
分子式: | C25H52NO4P | ||||
分子量: | 461.66 | ||||
EINEC: | 639966 | ||||
EINEC: | 639966 |
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: |
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. |
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
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 )