Perifosine
Based on 19 publication(s) in Google Scholar
Perifosine is an oral Akt inhibitor which inhibits proliferation of different tumor cell lines with IC50s of 0.6-8.9 μM.
For research use only. We do not sell to patients.
- Purity: 99.91%
- CAS No.: 157716-52-4
- Formula: C25H52NO4P
- Molecular Weight:461.66
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) Perifosine
More- Cancer Res. 2026 Jan 14. [Abstract]
- Acta Pharm Sin B. 2023 Oct;13(10):4253-4272. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Int J Biol Sci. 2016 Mar 30;12(5):607-16. [Abstract]
- Cell Death Dis. 2024 May 14;15(5):338. [Abstract]
- Cell Commun Signal. 2024 Jul 17;22(1):364. [Abstract]
- Int J Biol Macromol. 2025 Jan 23:140289. [Abstract]
- Biomed Pharmacother. 2024 Aug 8:178:117279. [Abstract]
- Biochem Pharmacol. 2026 May:247:117804. [Abstract]
- J Cell Mol Med. 2026 Feb;30(3):e71018. [Abstract]
- Cell Signal. 2025 Jul:131:111706. [Abstract]
- Exp Cell Res. 2021 Sep 15;406(2):112752. [Abstract]
- Mol Med Rep. 2020 Aug;22(2):895-905. [Abstract]
- Front Oncol. 2021 Apr 12;11:608570. [Abstract]
- Mol Immunol. 2023 Mar:155:27-43. [Abstract]
- J Cell Biochem. 2020 Mar;121(3):2343-2353. [Abstract]
- SSRN. 2025 Nov 25.
- Masaryk University. 2020 Jul.
- Preprints. 2020 Apr.
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WB
Biological Activity
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Autophagy |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
4.17 μM
Compound: perifosine
|
Cytotoxicity against human A549 cells after 24 to 72 hrs by haemocytometry
Cytotoxicity against human A549 cells after 24 to 72 hrs by haemocytometry
|
[PMID: 24900620] |
| A549 | IC50 |
5.3 μM
Compound: 2, OPP
|
Inhibition of Akt phosphorylation in insulin-stimulated human A549 cells treated 2 hrs before insulin stimulation measured after 30 mins by ELISA
Inhibition of Akt phosphorylation in insulin-stimulated human A549 cells treated 2 hrs before insulin stimulation measured after 30 mins by ELISA
|
[PMID: 22138309] |
| A549 | IC50 |
5.3 μM
Compound: 2, OPP
|
Inhibition of Akt phosphorylation in human insulin-stimulated A549 cells incubated for 2 hrs prior to insulin-induction measured after 30 mins by ELISA
Inhibition of Akt phosphorylation in human insulin-stimulated A549 cells incubated for 2 hrs prior to insulin-induction measured after 30 mins by ELISA
|
[PMID: 23415083] |
| A549 | IC50 |
7 μM
Compound: 2, OPP
|
Cytotoxicity against human A549 cells after 24 hrs by FACS analysis
Cytotoxicity against human A549 cells after 24 hrs by FACS analysis
|
[PMID: 22138309] |
| A549 | IC50 |
7 μM
Compound: 2, OPP
|
Cytotoxicity against human A549 cells by flow cytometric analysis
Cytotoxicity against human A549 cells by flow cytometric analysis
|
[PMID: 23415083] |
| ACHN | GI50 |
4.56 μM
Compound: Perifosine
|
Growth inhibition of human ACHN cells by sulforhodamine B assay
Growth inhibition of human ACHN cells by sulforhodamine B assay
|
[PMID: 21543141] |
| ACHN | GI50 |
4.56 μM
Compound: Perifosine
|
Growth inhibition of human ACHN cells by SRB assay
Growth inhibition of human ACHN cells by SRB assay
|
[PMID: 23266181] |
| ACHN | GI50 |
4.56 μM
Compound: Perifosine
|
Antiproliferative activity against human ACHN cells by SRB assay
Antiproliferative activity against human ACHN cells by SRB assay
|
[PMID: 23567950] |
| ACHN | GI50 |
4.56 μM
Compound: Perifosine
|
Growth inhibition of human ACHN cells after 48 hrs by SRB assay
Growth inhibition of human ACHN cells after 48 hrs by SRB assay
|
[PMID: 24095759] |
| HCT-15 | GI50 |
1.25 μM
Compound: Perifosine
|
Growth inhibition of human HCT15 cells by sulforhodamine B assay
Growth inhibition of human HCT15 cells by sulforhodamine B assay
|
[PMID: 21543141] |
| HCT-15 | GI50 |
1.25 μM
Compound: Perifosine
|
Growth inhibition of human HCT15 cells by SRB assay
Growth inhibition of human HCT15 cells by SRB assay
|
[PMID: 23266181] |
| HCT-15 | GI50 |
1.25 μM
Compound: Perifosine
|
Antiproliferative activity against human HCT15 cells by SRB assay
Antiproliferative activity against human HCT15 cells by SRB assay
|
[PMID: 23567950] |
| HCT-15 | GI50 |
1.25 μM
Compound: Perifosine
|
Growth inhibition of human HCT15 cells after 48 hrs by SRB assay
Growth inhibition of human HCT15 cells after 48 hrs by SRB assay
|
[PMID: 24095759] |
| MCF7 | IC50 |
13.3 μM
Compound: 2, OPP
|
Cytotoxicity against human MCF7 cells after 24 hrs by FACS analysis
Cytotoxicity against human MCF7 cells after 24 hrs by FACS analysis
|
[PMID: 22138309] |
| MCF7 | IC50 |
13.3 μM
Compound: 2, OPP
|
Cytotoxicity against human MCF7 cells by flow cytometric analysis
Cytotoxicity against human MCF7 cells by flow cytometric analysis
|
[PMID: 23415083] |
| MCF7 | IC50 |
75.8 μM
Compound: OPP
|
Inhibitory concentration against MCF-7 cells gwoth
Inhibitory concentration against MCF-7 cells gwoth
|
[PMID: 16190765] |
| MDA-MB-231 | GI50 |
2.86 μM
Compound: Perifosine
|
Growth inhibition of human MDA-MB-231 cells by sulforhodamine B assay
Growth inhibition of human MDA-MB-231 cells by sulforhodamine B assay
|
[PMID: 21543141] |
| MDA-MB-231 | GI50 |
2.86 μM
Compound: Perifosine
|
Growth inhibition of human MDA-MB-231 cells by SRB assay
Growth inhibition of human MDA-MB-231 cells by SRB assay
|
[PMID: 23266181] |
| MDA-MB-231 | GI50 |
2.86 μM
Compound: Perifosine
|
Antiproliferative activity against human MDA-MB-231 cells by SRB assay
Antiproliferative activity against human MDA-MB-231 cells by SRB assay
|
[PMID: 23567950] |
| MDA-MB-231 | GI50 |
2.86 μM
Compound: Perifosine
|
Growth inhibition of human MDA-MB-231 cells after 48 hrs by SRB assay
Growth inhibition of human MDA-MB-231 cells after 48 hrs by SRB assay
|
[PMID: 24095759] |
| NCI-H23 | GI50 |
4.21 μM
Compound: Perifosine
|
Growth inhibition of human NCI-H23 cells by sulforhodamine B assay
Growth inhibition of human NCI-H23 cells by sulforhodamine B assay
|
[PMID: 21543141] |
| NCI-H23 | GI50 |
4.21 μM
Compound: Perifosine
|
Growth inhibition of human NCI-H23 cells by SRB assay
Growth inhibition of human NCI-H23 cells by SRB assay
|
[PMID: 23266181] |
| NCI-H23 | GI50 |
4.21 μM
Compound: Perifosine
|
Antiproliferative activity against human NCI-H23 cells by SRB assay
Antiproliferative activity against human NCI-H23 cells by SRB assay
|
[PMID: 23567950] |
| NCI-H23 | GI50 |
4.21 μM
Compound: Perifosine
|
Growth inhibition of human NCI-H23 cells after 48 hrs by SRB assay
Growth inhibition of human NCI-H23 cells after 48 hrs by SRB assay
|
[PMID: 24095759] |
| NUGC-3 | GI50 |
0.54 μM
Compound: Perifosine
|
Growth inhibition of human NUGC3 cells by sulforhodamine B assay
Growth inhibition of human NUGC3 cells by sulforhodamine B assay
|
[PMID: 21543141] |
| NUGC-3 | GI50 |
0.54 μM
Compound: Perifosine
|
Growth inhibition of human NUGC3 cells by SRB assay
Growth inhibition of human NUGC3 cells by SRB assay
|
[PMID: 23266181] |
| NUGC-3 | GI50 |
0.54 μM
Compound: Perifosine
|
Antiproliferative activity against human NUGC3 cells by SRB assay
Antiproliferative activity against human NUGC3 cells by SRB assay
|
[PMID: 23567950] |
| NUGC-3 | GI50 |
0.54 μM
Compound: Perifosine
|
Growth inhibition of human NUGC3 cells after 48 hrs by SRB assay
Growth inhibition of human NUGC3 cells after 48 hrs by SRB assay
|
[PMID: 24095759] |
| PC-3 | GI50 |
0.44 μM
Compound: Perifosine
|
Growth inhibition of human PC3 cells by sulforhodamine B assay
Growth inhibition of human PC3 cells by sulforhodamine B assay
|
[PMID: 21543141] |
| PC-3 | GI50 |
0.44 μM
Compound: Perifosine
|
Growth inhibition of human PC3 cells by SRB assay
Growth inhibition of human PC3 cells by SRB assay
|
[PMID: 23266181] |
| PC-3 | GI50 |
0.44 μM
Compound: Perifosine
|
Antiproliferative activity against human PC3 cells by SRB assay
Antiproliferative activity against human PC3 cells by SRB assay
|
[PMID: 23567950] |
| PC-3 | GI50 |
0.44 μM
Compound: Perifosine
|
Growth inhibition of human PC3 cells after 48 hrs by SRB assay
Growth inhibition of human PC3 cells after 48 hrs by SRB assay
|
[PMID: 24095759] |
| RBL-2H3 | IC50 |
5 μM
Compound: 5
|
Inhibition of rat RBL2H3 cell granulation assessed as reduction of beta hexasaminidase release
Inhibition of rat RBL2H3 cell granulation assessed as reduction of beta hexasaminidase release
|
[PMID: 20153565] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 157716-52-4
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Appearance Solid
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Molecular Weight 461.66
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Formula C25H52NO4P
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Color White to off-white
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SMILES
[O-]P(OC1CC[N+](C)(CC1)C)(OCCCCCCCCCCCCCCCCCC)=O
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Synonyms
KRX-0401; NSC 639966; D21266
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (19)
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Journal Impact Factor
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Most Recent
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Cancer Res
Nerves Stimulates Crosstalk between Gastric Cancer and Group 3 Innate Lymphoid Cells to Enhance Immunosuppression. [Abstract]2026 Jan 14. PMID: 41534088 -
Acta Pharm Sin B
A high-throughput Gaussia luciferase reporter assay for screening potential gasdermin E activators against pancreatic cancer. [Abstract]2023 Oct;13(10):4253-4272. PMID: 37799380 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Int J Biol Sci
Ecological Trade-offs between Migration and Reproduction Are Mediated by the Nutrition-Sensitive Insulin-Signaling Pathway. [Abstract]2016 Mar 30;12(5):607-16. PMID: 27143957 -
Cell Death Dis
METTL8 links mt-tRNA m3C modification to the HIF1α/RTK/Akt axis to sustain GBM stemness and tumorigenicity. [Abstract]2024 May 14;15(5):338. PMID: 38744809 -
Cell Commun Signal
Targeting CCL2-CCR2 signaling pathway alleviates macrophage dysfunction in COPD via PI3K-AKT axis. [Abstract]2024 Jul 17;22(1):364. PMID: 39014433 -
Int J Biol Macromol
Astrocyte-conditional knockout of MOB2 inhibits the phenotypic conversion of reactive astrocytes from A1 to A2 following spinal cord injury in mice. [Abstract]2025 Jan 23:140289. PMID: 39863205 -
Biomed Pharmacother
2024 Aug 8:178:117279. PMID: 39121587 -
Biochem Pharmacol
ATF5 activates LPAR5 to enhance macrophage pro-inflammatory responses to exacerbate rheumatoid arthritis. [Abstract]2026 May:247:117804. PMID: 41690415 -
J Cell Mol Med
17-β-Estradiol Protects Chondrocytes From Senescence and Ameliorates Osteoarthritis Progression via ERα-AKT-FOXO4 Pathway. [Abstract]2026 Feb;30(3):e71018. PMID: 41677002 -
Cell Signal
Paeoniflorin-6'-O-benzene sulfonate inhibits keratinocyte proliferation by restoring GRK2-JAK1 colocalization in mouse model of psoriasis. [Abstract]2025 Jul:131:111706. PMID: 40037425 -
Exp Cell Res
ACBD3 is up-regulated in gastric cancer and promotes cell cycle G1-to-S transition in an AKT-dependent manner. [Abstract]2021 Sep 15;406(2):112752. PMID: 34332983 -
Mol Med Rep
Downregulation of miRNA‑328 promotes the angiogenesis of HUVECs by regulating the PIM1 and AKT/mTOR signaling pathway under high glucose and low serum condition. [Abstract]2020 Aug;22(2):895-905. PMID: 32626978 -
Front Oncol
Rapamycin Antagonizes BCRP-Mediated Drug Resistance Through the PI3K/Akt/mTOR Signaling Pathway in mPRα-Positive Breast Cancer. [Abstract]2021 Apr 12;11:608570. PMID: 33912444
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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Mol Immunol
Myocardial ischemia-reperfusion injury is probably due to the excessive production of mitochondrial ROS caused by the activation of 5-HT degradation system mediated by PAF receptor. [Abstract]2023 Mar:155:27-43. PMID: 36682136 -
J Cell Biochem
Vascular endothelial growth factor enhances tendon-bone healing by activating Yes-associated protein for angiogenesis induction and rotator cuff reconstruction in rats. [Abstract]2020 Mar;121(3):2343-2353. PMID: 31633245 -
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Solvent & Solubility
H2O : 100 mg/mL (216.61 mM; Need ultrasonic)
DMF : < 1 mg/mL (insoluble)
DMSO : < 1 mg/mL (insoluble or slightly soluble)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: PBS
Solubility: 50 mg/mL (108.30 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[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]
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 | Concentration Solvent Mass | 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.