Perifosine is an oral Akt inhibitor which inhibits proliferation of different tumor cell lines with IC50s of 0.6-8.9 μM.
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Perifosine Estructura química
No. CAS : 157716-52-4
This product is a controlled substance and not for sale in your territory.
Based on 14 publication(s) in Google Scholar
Perifosine purchased from MedChemExpress. Usage Cited in:
Front Oncol. 2021 Apr 12;11:608570.
[Abstract]
The rescue test of PI3K/Akt/mTOR signaling in response to 17α-PG in MDA-MB-453/BCRP cells. The cells are starved for 48 h and then treated with 1,000 nM 17α-PG combined with siAkt or Perifosine.
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Descripciòn
Perifosine is an oral Akt inhibitor which inhibits proliferation of different tumor cell lines with IC50s of 0.6-8.9 μM.
IC50 & Target[1]
Autophagy
In Vitro
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% FCS-supplemented media, the IC50 for 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 p21WAF1, irrespective of p53 function, and may be exploited clinically because the majority of human malignancies harbor p53 mutations. Perifosine (20 μM) induces both G1-S and G2-M cell cycle arrest, together with p21WAF1 expression in both p53 wild-type and p53-/- clones[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Perifosine Related Antibodies
In Vivo
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ensayo clínico
Peso molecular
461.66
Fòrmula
C25H52NO4P
No. CAS
157716-52-4
Appearance
Solid
Color
White to off-white
SMILES
[O-]P(OC1CC[N+](C)(CC1)C)(OCCCCCCCCCCCCCCCCCC)=O
Envío
Room temperature in continental US; may vary elsewhere.
Almacenamiento
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
Solvente y solubilidad
In Vitro:
H2O : 100 mg/mL (216.61 mM; Need ultrasonic)
DMF : < 1 mg/mL (insoluble)
DMSO : < 1 mg/mL (insoluble or slightly soluble)
Preparing Stock Solutions
ConcentrationSolventMass
1 mg
5 mg
10 mg
1 mM
2.1661 mL
10.8305 mL
21.6610 mL
5 mM
0.4332 mL
2.1661 mL
4.3322 mL
10 mM
0.2166 mL
1.0830 mL
2.1661 mL
View the Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
*
Note: If you choose water as the stock solution, please dilute it to the working solution,
then filter and sterilize it with a 0.22 μm filter before use.
This equation is commonly abbreviated as: C1V1 = C2V2
In Vivo:
For the following dissolution methods, please prepare the working solution directly.
It is recommended to prepare fresh solutions and use them promptly within a short period of time. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution.
If precipitation or phase separation occurs during preparation,
heat and/or sonication can be used to aid dissolution.
Protocol 1
Add each solvent one by one: PBS
Solubility: 50 mg/mL (108.30 mM); Clear solution; Need ultrasonic
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage
mg/kg
Animal weight (per animal)
g
Dosing volume (per animal)
μL
Number of animals
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration:
mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
[1]. Momota H, et al. Perifosine inhibits multiple signaling pathways in glial progenitors and cooperates with temozolomide to arrest cell proliferation in gliomas in vivo. Cancer Res, 2005, 65(16), 7429-7435.
[Content Brief]
[2]. Vyomesh Patel, et al. Perifosine, a novel alkylphospholipid, induces p21(WAF1) expression in squamous carcinoma cells through a p53-independent pathway, leading to loss in cyclin-dependent kinase activity and cell cycle arrest. Cancer Res, 2002, 62(5), 14
[Content Brief]
[3]. Chen L, et al. Rapamycin has paradoxical effects on S6 phosphorylation in rats with and without seizures. Epilepsia. 2012 Nov;53(11):2026-33.
[Content Brief]
Ensayo de quinasas
[2]
Exponentially growing cells (HN12, HN30, and HaCaT) are lysed, and 500 μg 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 (0.1-30 μM) or flavopiridol (300 nM) in the kinase assay buffer containing [γ-32P]ATP (3000 Ci/mmol) and 0.2 mg/mL histone H1, 25 μM ATP. Reactions are incubated at 37°C for 30 min and terminated by the addition of SDS-gel loading buffer, resolved in SDS-PAGE, and dried gels are subjected to autoradiography and phosphorimaging[2].
MCE no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.
Ensayo celular
[2]
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 (0.1-30 μM) or PBS (control). After treatment (24-48 h), cells are pulsed with [3H]thymidine (1 μCi/well) for 4-6 h, fixed (5% trichloroacetic acid), and solubilized (0.5 M NaOH) before scintillation counting. Experiments are performed in triplicates[2].
MCE no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.
Administraciòn de animales
[1][3]
Mice[1] 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 100 mg/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[3] 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 (20 mg/kg, ip, once), an Akt inhibitor, 30 min before rapamycin administration. Rats are sacrificed 1 h or 6 h after rapamycin injection.
MCE no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.
Referencias
[1]. Momota H, et al. Perifosine inhibits multiple signaling pathways in glial progenitors and cooperates with temozolomide to arrest cell proliferation in gliomas in vivo. Cancer Res, 2005, 65(16), 7429-7435.
[Content Brief]
[2]. Vyomesh Patel, et al. Perifosine, a novel alkylphospholipid, induces p21(WAF1) expression in squamous carcinoma cells through a p53-independent pathway, leading to loss in cyclin-dependent kinase activity and cell cycle arrest. Cancer Res, 2002, 62(5), 14
[Content Brief]
[3]. Chen L, et al. Rapamycin has paradoxical effects on S6 phosphorylation in rats with and without seizures. Epilepsia. 2012 Nov;53(11):2026-33.
[Content Brief]
[1]. Momota H, et al. Perifosine inhibits multiple signaling pathways in glial progenitors and cooperates with temozolomide to arrest cell proliferation in gliomas in vivo. Cancer Res, 2005, 65(16), 7429-7435.
[2]. Vyomesh Patel, et al. Perifosine, a novel alkylphospholipid, induces p21(WAF1) expression in squamous carcinoma cells through a p53-independent pathway, leading to loss in cyclin-dependent kinase activity and cell cycle arrest. Cancer Res, 2002, 62(5), 14
[3]. Chen L, et al. Rapamycin has paradoxical effects on S6 phosphorylation in rats with and without seizures. Epilepsia. 2012 Nov;53(11):2026-33.
Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Optional Solvent
ConcentrationSolventMass
1 mg
5 mg
10 mg
25 mg
H2O
1 mM
2.1661 mL
10.8305 mL
21.6610 mL
54.1524 mL
5 mM
0.4332 mL
2.1661 mL
4.3322 mL
10.8305 mL
10 mM
0.2166 mL
1.0830 mL
2.1661 mL
5.4152 mL
15 mM
0.1444 mL
0.7220 mL
1.4441 mL
3.6102 mL
20 mM
0.1083 mL
0.5415 mL
1.0830 mL
2.7076 mL
25 mM
0.0866 mL
0.4332 mL
0.8664 mL
2.1661 mL
30 mM
0.0722 mL
0.3610 mL
0.7220 mL
1.8051 mL
40 mM
0.0542 mL
0.2708 mL
0.5415 mL
1.3538 mL
50 mM
0.0433 mL
0.2166 mL
0.4332 mL
1.0830 mL
60 mM
0.0361 mL
0.1805 mL
0.3610 mL
0.9025 mL
80 mM
0.0271 mL
0.1354 mL
0.2708 mL
0.6769 mL
100 mM
0.0217 mL
0.1083 mL
0.2166 mL
0.5415 mL
*
Note: If you choose water as the stock solution, please dilute it to the working solution,
then filter and sterilize it with a 0.22 μm filter before use.
Perifosine Related Classifications
PI3K/Akt/mTORAutophagyApoptosis
AktAutophagyApoptosis
Help & FAQs
Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.
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