Perifosine (KRX-0401)
Catalog No.S1037 Synonyms: NSC639966
Molecular Weight(MW): 461.66
Perifosine (KRX-0401) is a novel Akt inhibitor with IC50 of 4.7 μM in MM.1S cells, targets pleckstrin homology domain of Akt. Phase 3.
16 Customer Reviews
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Tumor growth of 827 GSC-derived xenografts treated with an AKT inhibitor perifosine (30 mg/kg body weight). Twenty-three days after tumor implantation in mice, perifosine was administered by intraperitoneal injection (daily for 5 days). Error bars represent SD. Five mice per group, *p < 0.01.
Cancer Cell 2013 23, 839-52. Perifosine (KRX-0401) purchased from Selleck.
Immunoblot analysis of pY-STAT3, EZH2, AKT, and trimethylated H3K27 in lysates from xenograft tumors treated with an AKT inhibitor perifosine.
Cancer Cell 2013 23, 839-52. Perifosine (KRX-0401) purchased from Selleck.
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Co-IP analysis of methylated STAT3 in GBM xenograft tumors treated with perifosine.AKT inhibition in vivo decreased STAT3 methylation and pY-STAT3, but increased global levels of H3K27 trimethylation.
Cancer Cell 2013 23, 839-52. Perifosine (KRX-0401) purchased from Selleck.
IF staining of pS21 EZH2 and pY-STAT3 on the frozen sections of GBM xenografts treated with vehicle or perifosine. Nuclei were stained with DAPI. Bar represents 10 microns.
Cancer Cell 2013 23, 839-52. Perifosine (KRX-0401) purchased from Selleck.
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NRP-152 cells were transfected with Id1-luciferase reporter element as described in the figure and then incubated with±perifosine (10 nmol/L) for 2 hours, followed by±LR3-IGF-I (10 nmol/L) for 24 hours. Cells were then treated with ±BMP4 and assayed for luciferase 2 hours later.
Cancer Res 2010 70, 9106-9117. Perifosine (KRX-0401) purchased from Selleck.
Alkylphospholipid-induced morphological changes in HepG2 cells. Cell morphology was examined with an inverted microscope(20× original magnification). The morphology of HepG2 cells incubated with MEM/10% FBS is shown in the absence of any addition (control, A), or in the presence of 25 μM of HePC (B), edelfosine (C), ErPC (D) or perifosine (E) for 24 h. ErPC, erucylphosphocholine; FBS, fetal bovine serum; HePC, hexadecylphosphocholine; MEM, minimal essential medium.
Brit J Pharmacol 2010 160, 355–366. Perifosine (KRX-0401) purchased from Selleck.
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LAT2 is degraded by proteasomes after treatment with alkylphospholipids. A, 3-h treatment of NB4 cells before exposure to the proteasome inhibitor MG132 (10 μM) prevented the reduction of LAT2 induced by 25 μM ODPC. B, C, a similar effect was observed after exposure (30 min) of NB4 cells to the proteasome inhibitor MLN9708 (5 μM) followed by treatment with 25 μM ODPC (B) or 25 μM perifosine (C).Mol Cell Proteomics 2012 11(12), 1898-1912 . Perifosine (KRX-0401) purchased from Selleck.
(a) Validation of the global proteome and acetylome results. AS and BE2 cells were treated with 10 μM of perifosine for 16 h. Total proteins were extracted and 30 μg of protein was analyzed for integrin β5 and acetyl-Histone H2B (Lys12) by western blotting. GAPDH was used as loading control.
Sci Rep, 2017, 7:41950. Perifosine (KRX-0401) purchased from Selleck.
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Knockdown of BRCA1 sensitizes cells to PI3K/AKT pathway inhibitors. MCF7 cells transfected with either BRCA1-siRNA or control-siRNA were treated with increasing amounts of inhibitors targeting the PI3K/AKT pathway for 48 h in triplicate. Viable cells were measured by MTT assay.
Mol Carcinog 2012 ahead of print. Perifosine (KRX-0401) purchased from Selleck.
Established cell lines (A549 and H460 lines) were un-stimulated (“C”, same for all figures), or treated with indicated concentration of perifosine (0.3-10 μM) or plus ABT-737 (100 nM), cells were then cultured for indicated time, and cell growth was tested by MTT assay (a, b, d, e) or by colony formation assay (c and f). “Prf” stands for perifosine (Same for all figures). The results presented were representative of three independent experiments. The values were expressed as the means ± SD. *p < 0.05 vs “C” group. #p < 0.05 compared with the perifosine only group without ABT-737 co-treatment.
Biochem Biophys Res Commun, 2016, 473(4):1170-6. Perifosine (KRX-0401) purchased from Selleck.
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Western blotting analysis demonstrating Ser473p-Akt and total Akt levels in HepG2 cells and Bel-7402 cells treated with increasing concentrations of perifosine for 24 h. Betaactin served as loading control. Bands were analyzed by Glyco Band-Scan software. Each bar corresponds to the mean ±SD for at least three independent experiments. * P<0.05,** P<0.01 vs. control, Student,s t test
Cytotechnology 2010 62, 449-460. Perifosine (KRX-0401) purchased from Selleck.
Induction of apoptosis in hepatoma cells by treatment for 48 h with 10 μM perifosine. The treated cells were stained with DAPI and the apoptotic morphological changes in the nuclear chromatin were observed under a fluorescent microscope.
Cytotechnology 2010 62, 449-460. Perifosine (KRX-0401) purchased from Selleck.
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Western blotting assay showing cleavage of caspase-3, caspase-9 and PARP in response to perifosine treatment in hepatoma cells. Each bar corresponds to the mean ±SD for at least three independent experiments. * P<0.05, ** P<0.01 vs. control, Student,s t test
Cytotechnology 2010 62, 449-460. Perifosine (KRX-0401) purchased from Selleck.
This chart showed the change of the stable transfection cells in centrosome separation after the cells were treated with perifosine(1 μM) 6 hours, 12 hours and 24 hours. "C" means the control group, and "P" means the group treated with perifosine
2010 Zhao Jing PHD Medical College of Peking University. Perifosine (KRX-0401) purchased from Selleck.
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TEIF (telomerase transcriptional elements-interacting factor)gene is a novel human gene and cloned from the expression library of HeLa cell through the hTERT promoter-based yeast one-hybrid assay. And now we are trying to find the interaction between TEIF and the EGF pathway.
2010 Zhao Jing PHD Medical College of Peking University . Perifosine (KRX-0401) purchased from Selleck.
After starved in serum-free medium for 24h,T47D cells incubated with the indicated concentrations of Perifosine for 3h,followed by 15-minute stimolation of 100ng/ml EGF.
2010 Dr. Zhang of Tianjin Medical University. Perifosine (KRX-0401) purchased from Selleck.
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Biological Activity
| Description | Perifosine (KRX-0401) is a novel Akt inhibitor with IC50 of 4.7 μM in MM.1S cells, targets pleckstrin homology domain of Akt. Phase 3. | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| In vitro |
Perifosine develops anti-proliferative properties with IC50 of 0.6-8.9 μM in immortalized keratinocytes (HaCaT), and head and neck squamous carcinoma cells. [1] Perifosine strongly reduces phosphorylation levels of Akt and extracellular signal-regulated kinase (Erk) 1/2, induces cell cycle arrest in G1 and G2, and causes dose-dependent growth inhibition of mouse glial progenitors. [2] Perifosine (10 μM) completely inhibits the phosphorylation of Akt in MM.1S cells. [3] A recent study demonstrates Perifosine induces cell cycle arrest and apoptosis in human hepatocellular carcinoma cell lines by blockade of Akt phosphorylation. [4] |
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| Cell Data |
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| In vivo | Perifosine combining with temozolomide reduces tumor proliferation (a PDGF-driven gliomagenesis) in vivo. The results indicate that Perifosine is an effective drug in gliomas in which Akt and Ras-Erk 1/2 pathways are frequently activated, and may be new candidate for glima treatment in the clinic. [2] Both oral daily and weekly administration of Perifosine significantly reduce human MM tumor growth and increase survival, compared with control animals treated with PBS vehicle only. [3] Perifosine induces thrombocytosis and leukocytosis and increases myelopoiesis in murine marrow and spleen, whereas it causes apoptosis in myeloma xenografts. [5] |
Protocol
| Kinase Assay:[3] |
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Akt kinase assay: MM.1S cells are cultured in the presence or absence of perifosine (5 μM, 6 hours) and then stimulated with IL-6 (20 ng/mL, 10 minutes). In vitro akt kinase assay is then carried out using the Akt Kinase Assay Kit. |
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| Cell Research:[2] |
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| Animal Research:[3] |
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Solubility (25°C)
| In vitro | Ethanol | 15 mg/mL (32.49 mM) |
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| Water | 8 mg/mL (17.32 mM) | |
| DMSO | Insoluble | |
| In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): water For best results, use promptly after mixing. |
8mg/mL |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 461.66 |
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| Formula | C25H52NO4P |
| CAS No. | 157716-52-4 |
| Storage | powder |
| in solvent | |
| Synonyms | NSC639966 |
Bio Calculators
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Molarity Calculator
Clinical Trial Information
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT01051557 | Terminated | Adult Anaplastic Astrocytoma|Adult Anaplastic Oligodendroglioma|Adult Diffuse Astrocytoma|Adult Giant Cell Glioblastoma|Adult Glioblastoma|Adult Gliosarcoma|Adult Mixed Glioma|Adult Oligodendroglioma|Recurrent Adult Brain Neoplasm | National Cancer Institute (NCI) | January 27 2010 | Phase 1|Phase 2 |
| NCT01224730 | Completed | Cancer | AEterna Zentaris | January 24 2012 | Phase 1 |
| NCT02238496 | Unknown status | Brain Tumor Recurrent|Glioblastoma|Anaplastic Astrocytoma|Anaplastic Oligodendroglioma|Mixed Glioma | Andrew Lassman|Pfizer|AEterna Zentaris|Columbia University | July 2014 | Phase 2 |
| NCT01097018 | Completed | Colorectal Cancer | AEterna Zentaris | April 2010 | Phase 3 |
| NCT01049841 | Completed | Pediatric Solid Tumors | Memorial Sloan Kettering Cancer Center|University of Wisconsin Madison|Duke University|NATL COMP CA NETWORK|Pfizer|AEterna Zentaris | January 2010 | Phase 1 |
| NCT01002248 | Terminated | Multiple Myeloma | AEterna Zentaris|Dana-Farber Cancer Institute | December 2009 | Phase 3 |
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