Perifosine (KRX-0401)

Catalog No.S1037 Synonyms: NSC639966

Perifosine (KRX-0401) Chemical Structure

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.

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Cited by 49 Publications

16 Customer Reviews

  • 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.

  • 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.

  • 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.

     

    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.

    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.

  • 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.

  • 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.

  • 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.

  • 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.
Targets
Akt [1]
(MM.1S cells)
4.7 μM
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
T24 BC  MkniSpVv[3Srb36gRZN{[Xl? MnnhNE42NzFxMj61JO69VQ>? NIDabVQ{KGh? Mly4doVlfWOnczD0bIUh[mG|YXygR2IhfHm{b4PpcoUheGixc4Doc5J6dGG2aX;uJIxmfmWuczDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= MmXWNlYxQTd6N{O=
T24 BC  MUTD[YxtKF[rYXLpcIl1gSCDc4PhfS=> Mn7oNE42NzFxMj61JO69VQ>? MV6yOEBp NF\JZXlmdmijbnPld{B{d3KjZnXubYIucW6mdXPl[EBk\WyuII\pZYJqdGm2eTDk[YNz\WG|ZR?= NX\rZldlOjZyOUe4O|M>
T24 BC  NFH6e45CeG:ydH;zbZMhSXO|c3H5 NUjsfWFVOi53IN88US=> MnzvNlQhcA>? NYTvPGZEe2Wwc3n0bZpmeyCEQzDj[YxteyC2bzDzc5Ji\mWwaXKtbY5lfWOnZDDhdI9xfG:2aXRCpC=> MmrqNlYxQTd6N{O=
HepG2 M2n1OGZ2dmO2aX;uJGF{e2G7 M{nvV|IxyqEQvF2= NUK4cZlzOjUEoHi= MUHwdo9lfWOnczDhckBqdnSnboPlJIN6fG:ybHHzcYlkKH[jY4XvcIl7[XSrb36gZ49zemW|cH;u[Ilv\yC2bzDhJI5wfGGkbHWg[Ilt[XSjdHnvckBw\iC2aHWgSXIh[2m|dHXycpM> NXXHOYRtOjV7M{SyN|I>
U-87 MG  M3j2UmZ2dmO2aX;uJGF{e2G7 MX[yNOKh|ryP NWSyb3c{OjUEoHi= Mn\ibY5kemWjc3XzJIRwfWKuZT3t[Y1jemGwZTDic5Vv\CC|dIL1Z5R2emW| NVjRdnJUOjV7M{SyN|I>
HepG2 NVW1bHhKTnWwY4Tpc44hSXO|YYm= NHj0engzOMLizszN M13BTlYwOjRiaB?= MV\pcoNz\WG|ZYOgeIhmKGyndnXsd{Bw\iCOQ{OtTWkh[2:2cnXheIVlKHerdHigR3E> NIOw[YIzPTl|NEKzNi=>
U-87 MG  MkPLSpVv[3Srb36gRZN{[Xl? M3nGRlIxyqEQvF2= M{W5dVYwOjRiaB?= MmP4bY5kemWjc3XzJJRp\SCuZY\lcJMhd2ZiTFOzMWlKKGOxdILlZZRm\CC5aYToJGNS MXqyOVk{PDJ|Mh?=
HepG2 NF\BeGJHfW6ldHnvckBCe3OjeR?= NV6zXFVDOjEEoN88US=> M3PmWVYwOjRiaB?= NELrVXJl\WO{ZXHz[ZMhVEN|LVnJJIRm\3KjZHH0bY9vyqCocn;tJFYhcA>? MnXqNlU6OzR{M{K=
U-87 MG  MlfvSpVv[3Srb36gRZN{[Xl? NFzWSpMzOMLizszN MWW2M|I1KGh? NHL4VlBqdmO{ZXHz[ZMhfGinIHH1eI9xcGGpaXOg[ox2gCBiYYSgOkBpKHeqaXzlJIlvcGmkaYTzJJRpcXNiZnz1fEBifCB{NHi= MUiyOVk{PDJ|Mh?=
HepG2 M1TwVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4fIW|IxNzRyIN88US=> MkjGNlQwPDhiaB?= M3jqPIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHLveIghfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ MYKyOVk{PDJ|Mh?=
U-87 MG  M1nYT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYiyNE81OCEQvF2= NFfNO|YzPC92ODDo NUDPdnVVcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZo91cCC2aX3lJIFv\CCmb4PlJIRmeGWwZHXueEBu[W6wZYK= NFz4OXYzPTl|NEKzNi=>
A549 NXrmNWl2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYiwMlMuOTBizszN MYeyOE84OiCq NEXGUFVqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDic5RpKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= MXqyOVY6Pzh7OR?=
H460 M{fBWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVnoZY4yOC5|LUGwJO69VQ>? MkHCNlQwPzJiaB?= MlTxbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYn;0bEB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MVOyOVY6Pzh7OR?=
A549 MkHjRZBweHSxc3nzJGF{e3OjeR?= NYi5W4JEOS9|IN88US=> NXnYdmo6PDhiaB?= NGPGOlBqdmS3Y3XzJIFxd3C2b4Ppdy=> MXmyOVY6Pzh7OR?=
H460 NVrV[3RWSXCxcITvd4l{KEG|c4PhfS=> NE\2OFAyNzNizszN MWG0PEBp NHHVNmFqdmS3Y3XzJIFxd3C2b4Ppdy=> MXiyOVY6Pzh7OR?=
A549 M1jJdWZ2dmO2aX;uJGF{e2G7 M2Pv[FMh|ryP MojRPEBp MmjmZoxw[2u|IFHLWEBi[3SrdnH0bY9v MmD4NlU3QTd6OUm=
H460 MXLGeY5kfGmxbjDBd5NigQ>? M1PTSlMh|ryP NFrzTYw5KGh? NV70V|RM[myxY3vzJGFMXCCjY4TpeoF1cW:w MVSyOVY6Pzh7OR?=
A549 NE\CSIxHfW6ldHnvckBCe3OjeR?= Mn;rN{DPxE1? NWPR[JZnQCCq NFTLXZpjdG:la4OgcXRQWkNzLDDhcoQhTVKNLV3BVGsh[WO2aY\heIlwdiClb33ibY5m\CC5aYToJG1GUy1zNkK= MWOyOVY6Pzh7OR?=
H460 MmDmSpVv[3Srb36gRZN{[Xl? NX;vTWkzOyEQvF2= MWq4JIg> M2mwVoJtd2OtczDtWG9TSzFuIHHu[EBGWktvTVHQT{Bi[3SrdnH0bY9vKGOxbXLpcoVlKHerdHigUWVMNTF4Mh?= NE\hU2QzPTZ7N{i5PS=>
RMG1 MkDRR4VtdCCYaXHibYxqfHliQYPzZZk> M{G0XlEuOzBizszN M1nSNFczKGh? MWnk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MX:yOVUyQTF2OB?=
RMG2 M{PBZmNmdGxiVnnhZoltcXS7IFHzd4F6 MUmxMVMxKM7:TR?= Mmf2O|IhcA>? MlXk[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJIEh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ MorUNlU2OTlzNEi=
KOC7C MWPD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M1nsbFEuOzBizszN NVvBeW9jPzJiaB?= NGHhOHll\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK= NXLkSYN4OjV3MUmxOFg>
HAC2 M2jMNmNmdGxiVnnhZoltcXS7IFHzd4F6 NIjPb5kyNTNyIN88US=> M4G2UFczKGh? M{DzNoRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckBiKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= MWWyOVUyQTF2OB?=
RMG2 MWfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MUOxMVMxKM7:TR?= NXLNfIR6PDhiaB?= MXXk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MnjMNlU2OTlzNEi=
OVISE Mm\ZR4VtdCCYaXHibYxqfHliQYPzZZk> MlvmNU0{OCEQvF2= MYe0PEBp M1zkXIRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckBiKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= MnmwNlU2OTlzNEi=
SKOV3 M13uR2NmdGxiVnnhZoltcXS7IFHzd4F6 NIL6d|AyNTNyIN88US=> NGOwclE1QCCq MknT[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJIEh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ NGDZU5kzPTVzOUG0PC=>
A2780 M13kTWNmdGxiVnnhZoltcXS7IFHzd4F6 MnS3NU0{OCEQvF2= M4\te|Q5KGh? NFPMOVBl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK= MlPzNlU2OTlzNEi=
RMG1 M{TOTGFxd3C2b4Ppd{BCe3O|YYm= NGrU[Ic{OCEQvF2= M1S3dlI1KGh? NECycmdqdmS3Y3XzJIFxd3C2b4Ppdy=> NEHxN|UzPTVzOUG0PC=>
RMG2 M{LrNmFxd3C2b4Ppd{BCe3O|YYm= NHi0foE{OCEQvF2= NH;NRo0zPCCq NX7BR5BlcW6mdXPld{BieG:ydH;zbZM> M1iyXFI2PTF7MUS4
HCC1806 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFX4bmExNTFyIN88US=> MkjiOFghcA>? M4TVTmVEPTB;Mj64OQKBkcLz4pEJNE4xPyEQvF2= M13JdVI2Ojl|NUe2
MDA-MB-231  MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGf6dXQxNTFyIN88US=> NXracW1wPDhiaB?= MnjTSWM2OD1zLkGz5qCKyrIkgJmwMlA4KM7:TR?= MWSyOVI6OzV5Nh?=
GL-1 NYOxXJIzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DVPVAvOeLCk{GwNQKBkc7:TR?= M2rPWVQ5KGh? MWHJR|UxRTlwOUGg{txO MoLnNlQ5QDF3MEi=
CLBL-1 MnzwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHGTFluOC5z4pETNVAx6oDLzszN M3jRblQ5KGh? NGLNdIpKSzVyPUOzMlAh|ryP MkDSNlQ5QDF3MEi=
UL-1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXmwMlHjiJNzMEFihKnPxE1? M1naXVQ5KGh? NV;4WpkzUUN3ME23MlAyKM7:TR?= MXiyOFg5OTVyOB?=
Ema NVf4bnB5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkezNE4y6oDVMUCw5qCK|ryP MVi0PEBp NVPOT4ZOUUN3ME21PE44KM7:TR?= MUGyOFg5OTVyOB?=
PANC-1 NYD2W49OT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWqyVYl[OC1{NTFOwG0> NGny[lg4OiCq NHfIc49qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MonuNlQ2OTl5NUG=
MIA NIL0NJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TXbFAuOjVizszN M1TjVVczKGh? MUfpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NUS2NlZ1OjR3MUm3OVE>
AsPC-1 NUD6TG9ST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWq4V5NGOC1{NTFOwG0> M2PUcVczKGh? MmDybY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NVXM[I9ROjR3MUm3OVE>
PANC-1 MXTGeY5kfGmxbjDBd5NigQ>? M4nJTlAvPSEQvF2= MnPPNlQhcA>? NFOxWlJqdmirYnn0d{BCc3RuIGO2T|EtKGGwZDDFdosyNzJicHjvd5Bpd3K7bHH0bY9vyqB? MY[yOFUyQTd3MR?=
MIA M3nkXGZ2dmO2aX;uJGF{e2G7 MorrNE42KM7:TR?= M3ywd|I1KGh? M3npTYlvcGmkaYTzJGFsfCxiU{\LNUwh[W6mIFXyb|EwOiCyaH;zdIhwenmuYYTpc47DqA>? Ml7YNlQ2OTl5NUG=
AsPC-1 NIi3UY1HfW6ldHnvckBCe3OjeR?= MXywMlUh|ryP MV[yOEBp NVe2dZpycW6qaXLpeJMhSWu2LDDTOmsyNCCjbnSgSZJsOS9{IIDoc5NxcG:{eXzheIlwdsLi NHvR[IIzPDVzOUe1NS=>
U87MG NVLaSVhRS2WubDDWbYFjcWyrdImgRZN{[Xl? MljqNE0zPSEQvF2= MYmyOE06PiCq M37GWYRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckBjd3SqIHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51KG2jbn7ldi=> NILWbYczPDB4NUWyNi=>
SGC7901  MUjGeY5kfGmxbjDBd5NigQ>? M1r0c|AvPzVxMUFCpO69VQ>? MkXLOFghcA>? Mlf2[IVkemWjc3XzJJAuSWu2IDjT[ZIhPDd|KTygdE1IW0t|zsKgLHNmeiB7KTygZY5lKENvTWnDJIxmfmWuc9Mg NWWweWFxOjN7MUKyOFY>
MGC803  M3\G[WZ2dmO2aX;uJGF{e2G7 M3;UVlAvPzVxMUFCpO69VQ>? MWq0POKhcA>? NIjncI5l\WO{ZXHz[ZMheC2Da4SgLHNmeiB2N{OpMEBxNUeVS{ROtkApW2W{IEmpMEBidmRiQz3NXWMhdGW4ZXzzxsA> NVuxXoFqOjN7MUKyOFY>
TykNu M{PVbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPnTWM2OD1|LkWg{txO MonoNlM5PzdyMUK=
TykNuR M{PlWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGXTNIFKSzVyPUWuOUDPxE1? NWDQOIxFOjN6N{ewNVI>
M41 MoHJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MliwTWM2OD1{ND63JO69VQ>? M4HOdVI{QDd5MEGy
M41R NXrqZ3BYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDBeHZKSzVyPUG5Mlgh|ryP NXzjUHhXOjN6N{ewNVI>
OVCAR8 NH35TpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1n4XWlEPTB;M{GuNUDPxE1? NGPHW4QzOzh5N{CxNi=>
HeyA8 NV\NXFlCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\R[IVbUUN3ME2yOE4{KM7:TR?= MmrpNlM5PzdyMUK=
A2780CP MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DsTWlEPTB;Nz62JO69VQ>? NGTOUJczOzh5N{CxNi=>
OVCAR5 M4TPNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTZwNzFOwG0> M3fwfVI{QDd5MEGy
A2780S NVL5fXVmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTF2LkWg{txO Mm\6NlM5PzdyMUK=
MCAS MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{j1cmlEPTB;MUKuOUDPxE1? NG\hcokzOzh5N{CxNi=>
NCI-H727 NET3Z4NE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NXnyXnhrOC1zMECg{txO M37zNFI1Nzd{IHi= M3P3boRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckBjd3SqIHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51KG2jbn7ldi=> M1G2cFIzPDl7NEO3
GOT1 MVXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NVHkU44xOC1zMECg{txO NWfiUJBKOjRxN{KgbC=> M{PSWoRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckBjd3SqIHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51KG2jbn7ldi=> NEHwb5QzOjR7OUSzOy=>
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A498 NX\6fpliT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHL5[ngxNTJyIN88US=> MojOO|IhcA>? NFXMbo1qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MkPXNlE3PDRyNUC=
CWR22RV1 NWS1epVUS2WubDDWbYFjcWyrdImgRZN{[Xl? MkfONVAh|ryP M4W4c|I1KGh? MlHCbY5kemWjc3XzJJNmdnOrdHn2bZR6KG:oIHj1cYFvKEOZUkKyVnYyKGOnbHzzJJRwKHKjZHnheIlwdg>? MU[yNVQ6PjJ5Mx?=
CWR22RV1 NFnwVIxCeG:ydH;zbZMhSXO|c3H5 NEnFTHAyOCEQvF2= MoHvNlQhcA>? NVfOc2xV\W6qYX7j[ZMhemGmaXH0bY9vKGmwZIXj[YQh[XCxcITvd4l{ MX[yNVQ6PjJ5Mx?=
CWR22RV1 MmDjSpVv[3Srb36gRZN{[Xl? MVy1JO69VQ>? MYCyOEBp MYTy[YR2[2WmIIDoc5NxcG:{eXzheIlwdiCxZjDBb5Qhe2mpbnnmbYNidnSueR?= NHvzc3UzOTR7NkK3Ny=>
HepG2  MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;ofVNPPS9zMD:yNE81OCEQvF2= M{XzOlI1NzR6L{eyJIg> NIfxZ2FqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDic5RpKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= NF\Hc2IzODh2MkSyOS=>
Bel-7402 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\3UWc2NzFyL{KwM|QxKM7:TR?= NVG1WYV5OjRxNEivO|IhcA>? MUPpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCkb4ToJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MVKyNFg1OjR{NR?=
HepG2  M2DOO2Z2dmO2aX;uJGF{e2G7 NYDQd25uPS9zMD:yNEDPxE1? M3HpblI1KGh? MoLvdoV{fWy2czDpckB1cGViYXPjeY12dGG2aX;uJI9nKGOnbHygcpVu[mW{IHnuJJRp\SCJMj;NJJBp[XOn NEP6cYUzODh2MkSyOS=>
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HepG2  M4rSU2Fxd3C2b4Ppd{BCe3O|YYm= MUC1M|ExNzJyIN88US=> M3iyblI1NzR6IHi= NHjZWlNqdmS3Y3XzJIFxd3C2b4Ppd{BifCC2aHWgcI9v\y22aX3lJIV5eG:|dYLl M1;ydVIxQDR{NEK1
Bel-7402 M{jpNmFxd3C2b4Ppd{BCe3O|YYm= M{fOdFUwOTBxMkCg{txO MkGzNlQwPDhiaB?= M1HXcolv\HWlZYOgZZBweHSxc3nzJIF1KHSqZTDsc45oNXSrbXWg[Zhxd3O3cnW= NVjIfG9VOjB6NEK0NlU>
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PA-1  NF;aZnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYewMVQxKM7:TR?= NHfNUWI4OsLiaB?= NETGdlFKSzVyfkK1JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHigbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK= NUTWRpJ4OjB2MEWyPVY>
SKOV3  M{P4eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWqwMVQxKM7:TR?= MWS3NuKhcA>? NVvTd5kxUUN3MI6zNEDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIlvKGFiZH;z[UBl\XCnbnTlcpQhdWGwbnXy NWG1VWpvOjB2MEWyPVY>
A2780 NWPsUY9qT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUGwMVIxKM7:TR?= NGnJeY01QC95MjDo MXrJR|UxyqB;wrCzxsDPxG1? MnXPNlA1ODV{OU[=
A2780cis  Mlz1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\uW|AuOjBizszN M1;DRlQ5Nzd{IHi= NFn5PINKSzVywrC9xsA3yqEQvH2= MUmyNFQxPTJ7Nh?=
SKW6.4 NYTTSI9rT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnzKNk0yOMLizszN M4fJPFQ5yqCq M4HRT4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz Mn\sNlAyOzB7NkC=
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OCI M1S0TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUmyMVExyqEQvF2= NU\SSIhTPDkEoHi= MofKbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MofFNlAyOzB7NkC=
MOLM MlqyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXYNk0yOMLizszN M4LzWVQ5yqCq MWXpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> M{PLRVIxOTNyOU[w
HL-60 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEK5SJAzNTFywrFOwG0> MWe0POKhcA>? MX3pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> Mn;DNlAyOzB7NkC=
SKW6.4 MoP3RZBweHSxc3nzJGF{e3OjeR?= M{PKNlExyqEQvF2= NVLtfm01OjRxNEigbC=> NHPpZ3ZqdmS3Y3XzJIFxd3C2b4Ppd{B1cW2nLXTldIVv\GWwdHz5 MkT5NlAyOzB7NkC=
MAVER MnPURZBweHSxc3nzJGF{e3OjeR?= NX3DWmxpOTEEoN88US=> NXvod2xbOjRxNEigbC=> MWLpcoR2[2W|IHHwc5B1d3OrczD0bY1mNWSncHXu[IVvfGy7 NGTXZ3UzODF|MEm2NC=>
BJAB NWi2b4lSSXCxcITvd4l{KEG|c4PhfS=> NUnUVHhmOTEEoN88US=> MV:yOE81QCCq MWTpcoR2[2W|IHHwc5B1d3OrczD0bY1mNWSncHXu[IVvfGy7 NWXxb2M4OjBzM{C5OlA>
OCI NVTlZlFLSXCxcITvd4l{KEG|c4PhfS=> NWnST4JDOTEEoN88US=> NEnSVFAzPC92ODDo MVXpcoR2[2W|IHHwc5B1d3OrczD0bY1mNWSncHXu[IVvfGy7 NVPtcmlFOjBzM{C5OlA>
MOLM MVvBdI9xfG:|aYOgRZN{e2G7 NUjzUmFTOTEEoN88US=> M1;NVlI1NzR6IHi= NUXEO2dIcW6mdXPld{BieG:ydH;zbZMhfGmvZT3k[ZBmdmSnboTsfS=> M3\0SlIxOTNyOU[w
HL-60 NXn0OINlSXCxcITvd4l{KEG|c4PhfS=> M3nxRlExyqEQvF2= MUiyOE81QCCq NXjaTFJ1cW6mdXPld{BieG:ydH;zbZMhfGmvZT3k[ZBmdmSnboTsfS=> M3TSNFIxOTNyOU[w

... Click to View More Cell Line Experimental Data

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]
+ Expand

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.
Cell Research:[2]
+ Expand
  • Cell lines: Human glioma cell lines
  • Concentrations: 0, 15, 30 and 45 μM
  • Incubation Time: 48 hours
  • Method: Cells are incubated in the medium with 10% FCS for 48 hours with indicated concentration of Periosine. Cell viability is determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. (Cell Proliferation Kit I; Roche). The absorbance at 590 nm is recorded using the 96-well plate reader.
    (Only for Reference)
Animal Research:[3]
+ Expand
  • Animal Models: MM.1S MM cells are inoculated subcutaneously in the right flank of Beige-nude-xid (BNX) mice (5 to 6 weeks old).
  • Formulation: 0.9% NaCl solution
  • Dosages: 250 mg/kg/wk or 36 mg/kg/d
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro Ethanol 15 mg/mL (32.49 mM)
Water 8 mg/mL (17.32 mM)
DMSO Insoluble
In vivo Add solvents individually and in order:
30% propylene glycol, 5% Tween 80, 65% D5W
30 mg/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
Formula

C25H52NO4P

CAS No. 157716-52-4
Storage powder
Synonyms NSC639966

Bio Calculators

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02238496 Active, not recruiting Brain Tumor, Recurrent|Glioblastoma|Anaplastic Astrocytoma|Anaplastic Oligodendroglioma|Mixed Glioma Andrew Lassman|Pfizer|AEterna Zentaris|Columbia University July 2014 Phase 2
NCT01224730 Unknown status Cancer AEterna Zentaris January 2012 Phase 1
NCT01097018 Completed Colorectal Cancer AEterna Zentaris April 2010 Phase 3
NCT01049841 Active, not recruiting 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
NCT01051557 Active, not recruiting 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 2010 Phase 1|Phase 2
NCT01002248 Terminated Multiple Myeloma AEterna Zentaris|Dana-Farber Cancer Institute December 2009 Phase 3

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID